Glucocorticoid Receptor Antagonist/Modulator. 65 In turn, pan-BD2 inhibitors (which have higher inhibitory activity for BD2 than BD1 of BET family members) are. • GSK778 exhibits >130-fold BD1 selectivity over BD2 due to BD1 Asp144/His433 displacement (Kharenko et al. SML3234. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. 00. WGK 3. PubMed Abstract: The two tandem bromodomains of the BET (bromodomain and extraterminal domain) proteins enable chromatin binding to facilitate transcription. All Photos (1) SML3234. Copy Link. GSK778 Hydrochloride. GSK778 Hydrochloride. 1. 26 (n= 10); 40-fold. All Photos (1) Documents. , 2020). Available to order from Sigma-Aldrich. The BD1-selective inhibitor GSK778 exhibited similar transcriptional effects compared to pan-BET inhibitors in cancer cells, consistent with previous studies showing that BD1 plays the dominant role in maintaining established transcriptional programs (Picaud et al. GSK778 Hydrochloride. View and buy high purity iBET-BD1 | GSK778 from AOBIOUS, the leading supplier of life science reagents. S1F, and table S1). Copy Link. ID EN. Available to order from Sigma-Aldrich. Primary Citation of Related Structures: 6SWN, 6SWO, 6SWP, 6SWQ. Cell proliferation outcomes in naïve CD4+ T cell counts following 6 days of culture, for each of the two genotypes under the four treatment conditions (i. Available to order from Sigma-Aldrich. MOscan analysis of GSK778 indicated the binding of this compound only to BET bromodomains with strong binding to BET BD1 domains while weakly binding to BET BD2 domains. Pharmacological inhibition of BET BDs using the chemical probes JQ1 (Filippakopoulos et al. In human whole blood and MV-4–11 cells, selective inhibition of GSK778 against BD1 retains the anti-inflammatory and antiproliferative phenotype features of pan-BET inhibition. All Photos (1) Documents. GSK778 is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). For research use only. AA Blocks. All Photos (1) Documents. COO/ COA. GSK778 also displayed strong anti-cancer effects in vivo, prolonging the survival of mice carrying an aggressive form of AML at only 15 mg/kg. 5), is a highly selective BD1 inhibitor (BRD4(1), IC 50 = 41 nM) with a 143-fold selectivity over BD2. CAS# 2451862-42-1. GSK778 (iBET-BD1) is a potent and selective inhibitor of bromodomain (BRD) BD1. WGK 3. R. SML3234. Herein, GSK778 and GSK046 are referred to as iBET-BD1 and iBET-BD2, respectively. 1. Membranes were blocked with 5% milk in Tris-buffered saline (TBS) with 0. Available to order from Sigma-Aldrich. 6147. Copy Link. GSK778 Hydrochloride. All Photos (1) Documents. SML3234. from publication: Fast and Accurate. COO/ COA. They are epigenetic readers of histone acetylation with broad specificity. Open in a. SML3168. GSK778 Hydrochloride. When bound to. However, recent reports of potent and selective pan-BET BD1 and pan-BET BD2 inhibitors have been reported including ABBV-744, 21 GSK778, and GSK046. Compounds GSK778 (5) and GSK046 (6) are recently reported BET BD1-selective and BET BD2-selective small molecule inhibitors with >130-fold and >300-fold selectivity over the other corresponding bromodomains, respectively, as determined by surface plasmon resonance (SPR) assays. G-Protein-coupled Receptor Ligands. Email. Available to order from Sigma-Aldrich. SGC Toronto. nM, SPR BRD4 (BD1): pKd= 8. 1iBET-BD1 (GSK778) Following the initial report of the biological activity of iBET-BD1 and iBET-BD2, 19 Wellaway et al. ≥98% (HPLC)We would like to show you a description here but the site won’t allow us. ≥98% (HPLC)Despite their profound preclinical efficacy, the clinical utility of pan-inhibitors is limited due to observed cytotoxicicities. The structures of the two predominant metabolites (M4 and M5) of RVX-208, observed both in in vitro human and animal liver microsomal incubations, as well as in plasma from animal in vivo studies, were determined. GSK778 (iBET-BD1) potently inhibits numerous cancer cells. Before sharing sensitive information, make sure you’re on a federal government site. All Photos (1) SML3234. GSK778, a potent pan-D1 inhibitor, was reported by Gilan et al. Available to order from Sigma-Aldrich. Applications Products Services Documents Support. selective (GSK778) or BD2-selective (GSK046 and ABBV-744) BETis showed signicant IC 50 value dierences between BD1 and BD2 2,9,22,23. BD1 selective inhibitors, such as GSK778, MS-436, Olinone, and BI-2536, as well as the BD2 selective inhibitors RVX-208, RVX-297, GSK046, and ABBV-744 have been produced. Recently, inhibitors were developed that selectively target the first (BD1) and second (BD2) bromodomain of the BET proteins (iBET-BD1 [GSK778] and iBET-BD2 [GSK046]). Applications Products Services Documents Support. 1 in RR-multiple myeloma CC-94280 HIGHLIGHTS FROM DRUG DISCOVERY ARTICLES PUBLISHED ONLINE | MAR. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. GSK778 (iBET-BD1) potently inhibits numerous cancer cells. GSK778 phenocopies the effects of pan- BET inhibitors in cancer models. 00. Storage Class Code. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models[1]. Your information is safe with us. VI EN. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. On the basis of sequence homology, BCPs are classified into eight different subgroups (families). 5 (LPS-PBMC assay) ≤ 10 µM. GSK778: GSK778 (iBET-BD1) is a strong BD1 bromodomain inhibitor of the BET proteins, with IC50 value of 75 nM for BRD2 BD1, 41 nM for BRD3 BD1, 41 nM for BRD4 BD1, and 143 nM for BRDT BD1. GSK778 hydrochloride hydrochloride phenocopies the effects of pan-BET inhibitors in cancer models[1]. * Please kindly note that our products are not to be used for therapeutic purposes and cannot be sold to patients. The bromodomain (BD) is a ~110 amino acid motif that binds to acetyl-lysine modifications on histone and non-histone proteins (Dhalluin et al. Their affinities for the individual bromodomains of the BET family were initially determined by TR-FRET (Fig. The calculations of the energy contributions of individual residues demonstrate that residues corresponding to (BD1, BD2) generate significant energy difference in binding of SG3-179, GSK778, and. 1. GSK778 Hydrochloride. Catalog Number: AA01KEG7. Applications Products Services Documents Support. 2451862-42-1: Formula: C 30 H 33 N 5 O 3: Formula Wt. Available to order from Sigma-Aldrich. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. 65 ABBV-744 shows potent anti-proliferative effects against. GSK778 (iBET-BD1) is a potent and selective inhibitor of the BD1 bromine domain of the BET protein,IC50 The values are 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1). COO/ COA. comThe calculations of the energy contributions of individual residues demonstrate that residues corresponding to (BD1, BD2) generate significant energy difference in binding of SG3-179, GSK778, and. Serum alanine aminotransferase (ALT)/aspartate aminotransferase (AST) < 2. All Photos (1) Documents. Fig. Immunoblots. ≥98% (HPLC) All Photos (1)GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778. Open in a separate window. Recombinant IL-1β (Peprotech, Cranbury, NJ) was reconstituted RPMI at 0. Resolution:Description GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Chemical Structure GSK778. 5 upper limit of normal (ULN) Total bilirubin < 1. GSK778. Solubility: Soluble in DMSO. GSK778 Hydrochloride. GSK778: CAS Registry Number: 2451862-42-1: Molecular Weight: 511. SML3234. Modukuri a,1, Zhifeng Yu , Zhi Tan , Hai Minh Tab,1, Melek Nihan Ucisik a. Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months). (B). Discovery of potent BET bromodomain 1 stereoselective inhibitors using DNA-encoded chemical library selections Ram K. Available to order from Sigma-Aldrich. Available to order from Sigma-Aldrich. ≥98% (HPLC) All Photos (1)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. COO/ COA. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models[1]. Anti-Radixin antibody produced in rabbit. The oldest compound, RVX-208 based on a quinazolinone chemical core, exhibited a selectivity of 20-fold with K D values of 4100 nMComprar GSK778 hydrochloride na CymitQuimica a partir de 187,0 €I-BET151 (GSK1210151A), iBET-BD1 (GSK778) and iBET-BD2 (GSK046) were provided by GlaxoSmithKline plc (GSK, London, UK). Copy Link. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC 50 s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Open in a separate window. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. their selectivity. Copy Link. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. SML3234. showed that BD(1)-specific GSK778 phenocopied the effects of pan-BET BRD inhibitors, while GSK046 and its orally bioavailable GSK620 derivative had minimal impact on cell viability while impairing the induction, but not the maintenance, of transcriptional programs [133]. Copy Link. CA EN. SML3234. 3; Cell. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. CAS#: 2451862-42-1. If not otherwise indicated, cells were pretreated with I-BET151, iBET-BD1,. GD EN. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. In recent years, members of the bromodomain and. SML3234. ZA EN. GSK778 Hydrochloride. All Photos (1) Documents. By Louis Gilman. The RNA. GM6001. Available to order from Sigma-Aldrich. Recently, inhibitors were developed that selectively target the first (BD1) and second (BD2) bromodomain of the BET proteins (iBET-BD1 [GSK778] and iBET-BD2 [GSK046]). Available to order from Sigma-Aldrich. *. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. IL EN. Safety Information. The calculations of the energy contributions of individual residues demonstrate that residues corresponding to (BD1, BD2) generate significant energy difference in binding of SG3-179, GSK778, and. 5. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. K. K. GSK778 Hydrochloride. Comparison of the binding modes of CDD-956 with BD1, CDD-1302 with BRDT-BD2 , and iBET-BD1 (GSK778) with BRD4-BD1 (Fig. GSK778 Hydrochloride. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Copy Link. Find here details of companies selling GSK778, for your purchase requirements. Address: 1633 Old Bayshore Highway Suite 280 Burlingame, CA 94010. 6SWN, 6SWO, 6SWP, 6SWQ. Glatiramer acetate generates anti-inflammatory Th2 cells, which produce neurotrophic factors. 2451862-42-1: GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively; GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. 11 - Combustible Solids. COO/ COA. MS40229, and GSK77830. GSK778 Hydrochloride. The distinct families are. Available to order from Sigma-Aldrich. Email. , 2020), which is accordant to a previous reported BD1-specific inhibitor (Ma et al. , Suite 700 Toronto, ON, M5G 1L7 Canada +1 416-946-0237. AA Blocks. 27,42 The second-generation BRD4 inhibitors are mainly synthesized by proteolysis targeting chimera (PROTAC) technology. 0. , 2016). (A) Schematic of the BET Bromodomain proteins and chemical structures. ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. 9. In humans, 61 bromodomains, each composed of ∼110 amino acids forming four antiparallel α helices (αZ, αA, αB, and αC) and two hydrophobic (ZA and BC) loops, in 46 different proteins have been described. WGK. Email. AR EN. 15 Gilan et al. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. Available to order from Sigma-Aldrich. GSK778 Hydrochloride. GSK778. Domain-Selective Targeting (BD1 or BD2 Targeting) The BET protein family of BCPs comprise the ubiquitously expressed BRD2, BRD3, and BRD4 and the testis-restricted BRDT, all of which harbor two highly conserved tandem bromodomains, BD1 and BD2, allowing them to. All Photos (1) Documents. Available to order from Sigma-Aldrich. GSK778 inhibits proliferation, induces a cell cycle arrest and apoptosis . GSK778, also known as iBET-BD1, is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). 125 nM (MV-4−11 cells) ≤. Available to order from Sigma-Aldrich. 4. GSK778 reduces the production of anti-keyhole limpet. However, many compounds reported in the literature and routinely. Applications Products Services Documents Support. More than 7 days of UK778 history is available with an upgrade to a Silver (90 days), Gold (1 year), or Business (3 years) subscription. First of all, GSK778 (iBET-BD1) is a potent and selective inhibitor of bromodomain (BRD) BD1. IC₅₀ & Target BRD2 BD1 75 nM (IC50) BRD3 BD1 41 nM. The authors found that in mouse models of various cancers, BD1 inhibition is. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. All. SGC chemical probes are open-access. 5 ± 0. In addition, while GSK778 phenocopied I-BET151 in terms of antiproliferative effects on a range of human cancer cells, GSK046 was less effective. The two novel ‘iBET’ molecules display the. Recombinant IL-1β (Peprotech, Cranbury, NJ) was reconstituted RPMI at 0. ABBV-744 is highly selective for BD2 of BRD2, BRD3 and BRD4, 64 exhibiting several hundred-fold higher affinity for the BD2 over BD1. GSK778 (iBET-BD1) is a strong BD1 bromodomain inhibitor of the BET proteins, with IC50 value of 75. Adequate renal, hepatic, pulmonary and cardiac function defined as: Creatinine clearance (as estimated by Cockcroft Gault) > 60 mL/min. Storage Class Code. CPI-0610 is another second-generation BET inhibitor with a molecular structure similar. All Photos (1) SML3234. Copy Link. CAS: 2451862-42-1 (free base) Chemical Name: GSK778 2HCl; 4-(2-(Methoxymethyl)-1-((R)-1-phenylethyl)-8-(((S)-pyrrolidin-3-yl)methoxy)-1H. Applications Products Services Documents Support. GSK778 Hydrochloride. R3653. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Safety Information. +86-21-51987688Crystal structure of GSK778 complexed with BRD4-BD1 (Fig. comBET structure and function. Copy Link. Description: GSK778, also known as iBET-BD1, is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). S1F. WGK. Theoretical Analysis Hodoodo Cat#: H408120 Name: GSK778 CAS#: 2451862-42-1By surface plasmon resonance binding assay, GSK778 is > 130-fold selective for BD1, whereas GSK046 is > 300-fold selective for BD2 [26]. Copy Link. The imidazoquinolinone 8-position of iBET151 was identified as orienting towards the. 2451862-42-1. Instead, a unique effect of BD2-selective antagonism was revealed with GSK046 affecting the induction of gene expression more so than the expression of steady-state genes, in contrast to GSK778 . GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Purity : >98% (HPLC)Description: GSK778, also known as iBET-BD1, is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). Probe criteria. GSK778 offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model. Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months). Safety Information. 00. Copy Link. iBET-BD1 dihydrochloride . The distinct families are indicated by Roman numbers (I–VIII) in circles and. Available to order from Sigma-Aldrich. SML3234. Available to order from Sigma-Aldrich. Inhibitor/agonist potency: goal is < 50 nM (IC 50, K D) Surpasses criterion: :BET mutant TR-FRET assay: BRD2 (BD1) pIC 50 = 7. Email. You can also browse global suppliers,vendor,prices,Price,manufacturers of GSK484(1652591-81-5). 6SWN, 6SWO, 6SWP, 6SWQ. rednibar) and I. Available to order from Sigma-Aldrich. ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. ksg@ahjnirp. SERP Rating Probe GSK778 is in the process of SERP review. Available to order from Sigma-Aldrich. GSK778, also known as iBET-BD1, is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). PubMed Abstract: The two tandem bromodomains of the BET (bromodomain and extraterminal domain) proteins enable chromatin binding to facilitate transcription. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. It reduces relapse rate and disease progression in Multiple Sclerosis. We would like to show you a description here but the site won’t allow us. MM EN. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. All Photos (1) SML3234. COO/ COA. All Photos (1) Documents. GSK778 phenocopies the. Copy Link. 27, 42. GSK778 hydrochloride | C30H34ClN5O3 | CID 168013350 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological. Louis Gilman July 17, 2023. Dagrocorat. The BD2 selective inhibitor RVX-208 could significantly decrease atherosclerosis in hyperlipidemic apolipoprotein E-deficient mice 14 , and increase high-density lipoprotein cholesterol as well as apolipoprotein A-1 in monkeys 15 . GSK778 : Catalog Number: M10828: CAS Number: 2451862-42-1: 1. Email. FRAP, BAZ2A: 1000 1-25719566: 10 GSK2801. 2h 04m. Copy Link. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. 14 GSK778, another pan-D1-selective inhibitor (Figure 1A), was recently reported. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778. Available to order from Sigma-Aldrich. Not for human use. Figure 4. Código de clase de almacenamiento. GlaxoSmithKline; BRD2, BRD3, BRD4, BRDT (BD2) GSK046; pIC50 = 7. 11 - Combustible Solids. Fax: +1 510. Preis und Verfügbarkeit anzeigen. But, how does GSK778 work on the target? Let’s discuss it in detail. GSK778 Hydrochloride. gov means it’s official. to produce antitumor effects in vivo. ≥98% (HPLC)Comparison of the binding modes of CDD-956 with BD1, CDD-1302 with BRDT-BD2 , and iBET-BD1 (GSK778) with BRD4-BD1 (Fig. GSK778 Catalog No. HY-136570 10mg GSK778 CAS: 2451862-42-1 GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Visit ChemicalBook To find more GSK484(1652591-81-5) information like chemical properties,Structure,melting point,boiling point,density,molecular formula,molecular weight, physical properties,toxicity information,customs codes. CAS: 2451862-42-1 (free base) Chemical Name: GSK778 2HCl; 4-(2-(Methoxymethyl)-1-((R)-1-phenylethyl)-8-(((S)-pyrrolidin-3-yl)methoxy)-1H. For research use only. 00. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. 999. The subsequent development and application of GSK778 (BD1 selective) and GSK046 (BD2 selective) revealed that inhibition of BD2 was ineffective in displacing BET proteins from chromatin. 10 µM; GSK791. All Photos (1) Documents. At. Applications Products Services Documents Support. Copy Link. Fig. This approachGSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Copy Link. We do not sell to patients. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. 0; BRD4 (BD2) pKd = 5. (A) Schematic of the BET Bromodomain proteins and chemical structures. They are useful assets for example, in phenotypic assays, or as a starting point for medicinal chemistry campaigns. Applications Products Services Documents Support. BE EN. 06 (n = 8); (BD2) 5. GSK778. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC 50 s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Le GSK778 montre également de forts effets anti-cancéreux in vivo, prolongeant la survie de souris atteintes de leucémies myéloïdes aiguë [422, 423]. Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months). 5 (LPS-PBMC assay) ≤ 10 µM. 5 GSK778 (BD1) ↓. All Photos (1) Documents. Glioblastoma multiforme (GBM) is the most common and aggressive malignant primary brain tumor in adult humans, characterized by a poor prognosis despite the existence of multimodal therapy []. toronto@thesgc. Available to order from Sigma-Aldrich. SML3234. 33DFTG (TD139) $21. ChemicalBook 致力于为化学行业用户提供FREEBASE的性质、化学式、分子式、比重、密度,同时也包括FREEBASE的沸点、熔点、MSDS、用途、作用、毒性、价格、生产厂家、用途、上游原料、下游产品等信息。GSK778 phenocopied the effects of pan-BET inhibitors in cancer models. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Molecular Formula: C30H33N5O3. 61: Molecular Formula: C 30 H 33 N 5 O 3. SML3234. Available to order from Sigma-Aldrich. GSK778 hydrochloride hydrochloride phenocopies the effects of pan-BET inhibitors in cancer models[1]. MedKoo CAT#: 408120. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. BD1 selective inhibitors, such as GSK778, MS-436, Olinone, and BI-2536, as well as the BD2 selective inhibitors RVX-208, RVX-297, GSK046, and ABBV-744 have been produced. 6swn: n-terminal bromodomain of human brd4 with ibet-bd1 (gsk778)GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. Your information is safe with us. GSK778 phenocopies the. 11 - Combustible Solids. GSK789 was derived from a series of naphthyridone ATAD2 inhibitors. Applications Products Services Documents Support. WGK 3. TC EN. 1. Last but not the least, GSK778 offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model. (A) Schematic of the BET bromodomain proteins and chemical structures. Applications Products Services Documents Support. GSK778 phenotyping the role of pan-BET inhibitors in cancer models. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Not for human use. Nevertheless, it was more efficacious in a broad range of cancers and inflammatory pathologies [25]. Heat Shock Protein Research Products. Available to order from Sigma-Aldrich. Copy Link. GSK778 phenotyping the role of pan-BET inhibitors in cancer models. Preis und Verfügbarkeit anzeigen. 3 Details of the supplier of the safety data sheet; Company: Abmole Bioscience Inc. Applications Products Services Documents Support. Phone: +1 510. BRD4. Copy Link. Comprar GSK778 na CymitQuimica. SML3234. Fig.