GSK778
CAS No. 2451862-42-1
GSK778 ( iBET-BD1 )
Catalog No. M28843 CAS No. 2451862-42-1
GSK778 is a potent and selective inhibitor of BD1 bromodomain such as BRD2 BD1 (IC50s = 75 nM), BRD3 BD1 (IC50s = 41 nM), BRD4 BD1 (IC50s = 41 nM), and BRDT BD1 (IC50s = 143 nM). GSK778 inhibits proliferation, induces a cell cycle arrest and apoptosis.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
Size | Price / USD | Stock | Quantity |
5MG | 299 | Get Quote |
|
10MG | 478 | Get Quote |
|
25MG | 896 | Get Quote |
|
100MG | Get Quote | Get Quote |
|
200MG | Get Quote | Get Quote |
|
500MG | Get Quote | Get Quote |
|
1G | Get Quote | Get Quote |
|
Biological Information
-
Product NameGSK778
-
NoteResearch use only, not for human use.
-
Brief DescriptionGSK778 is a potent and selective inhibitor of BD1 bromodomain such as BRD2 BD1 (IC50s = 75 nM), BRD3 BD1 (IC50s = 41 nM), BRD4 BD1 (IC50s = 41 nM), and BRDT BD1 (IC50s = 143 nM). GSK778 inhibits proliferation, induces a cell cycle arrest and apoptosis.
-
DescriptionGSK778 is a potent and selective inhibitor of BD1 bromodomain such as BRD2 BD1 (IC50s = 75 nM), BRD3 BD1 (IC50s = 41 nM), BRD4 BD1 (IC50s = 41 nM), and BRDT BD1 (IC50s = 143 nM). GSK778 inhibits proliferation, induces a cell cycle arrest and apoptosis.(In Vitro):GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. GSK778 inhibits BRD BD2 receptors such as BRD2 BD2 (IC50 = 3950 nM), BRD3 BD2 (IC50 = 1210 nM ), BRD4 BD2 (IC50 = 5843 nM), and BRDT BD2 (IC50 = 17451 nM). GSK778 (0.001-10 μM; 5 days) has a more pronounced effect on the growth and viability of MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells. GSK778 (1000 nM; 12 days) reduces the clonogenic capacity of primary human AML cells. GSK778 (0.01-10 μM; 72 hours) inhibited the production of effector cytokines including IFNγ, IL-17A and IL-22 and the proliferative activity of human primary CD4+ T cells.(In Vivo):GSK778 (15?mg/kg/BID; s.c. for 14 days) reduces the production of anti-keyhole limpet hemocyanin (KLH) IgM and is well tolerated. GSK778 (15?mg/kg/BID; i.p. for 30 days) offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model. The Cmax, Tmax and AUC∞ values are 85 ng/mL, 1.48 h and 132 ng.h/mL, respectively.
-
SynonymsiBET-BD1
-
PathwayChromatin/Epigenetic
-
TargetEpigenetic Reader Domain
-
RecptorVHL
-
Research Area——
-
Indication——
Chemical Information
-
CAS Number2451862-42-1
-
Formula Weight511.6
-
Molecular FormulaC30H33N5O3
-
Purity>98% (HPLC)
-
Solubility——
-
SMILESC[C@H](c1ccccc1)n1c2c(cc(c(-c3c(C)onc3C)c3)OC[C@@H]4CNCC4)c3ncc2nc1COC
-
Chemical Name——
Shipping & Storage Information
-
Storage(-20℃)
-
ShippingWith Ice Pack
-
Stability≥ 2 years
Reference
1.Crew, Andrew P, et al. MDM2-BASED MODULATORS OF PROTEOLYSIS AND ASSOCIATED METHODS OF USE. US20170008904A1.
molnova catalog
related products
-
3-methyl-1,2,3,4-tet...
3-methyl-1,2,3,4-tetrahydroquinazolin-2-one is a inhibitor of BRD4 .
-
BET bromodomain inhi...
It is a BET bromodomain inhibitor.
-
UMB298
UMB298 is a potent and selective CBP/P300 bromodomain inhibitor. UMB298 inhibits BRD4 with IC50 of 5193nM.