UM-002 | BRD4 inhibitor | Probechem Biochemicals

Chemical Structure : UM-002

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UM-002 (UM002)

货号: PC-72676Not For Human Use, Lab Use Only.

UM-002 is a highly potent, selective, brain penetrant BRD4 bromodomain inhibitor with IC50 of 8.8 and 2.4 nM for BRD4-1 and BRD4-2, respectively.

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生物&药学活性

UM-002 is a highly potent, selective, brain penetrant BRD4 bromodomain inhibitor with IC50 of 8.8 and 2.4 nM for BRD4-1 and BRD4-2, respectively.
UM-002 is more potent than JQ1 at inhibiting BRD2-1, BRD4-1, and BRD4-2.
UM-002 reduces GBM cell proliferation more than JQ1, or the brain penetrant BET inhibitor MK-8628.
UM-002 not affect the enzymatic activity of histone deacetylases, histone acetyltransferases.
UM-002 inhibits GBM cell proliferation in vitro with EC50 of 0.13 and 0.24 uM for GBM22 cells and GBM39 cells, repectively.
UM-002 reduces proliferation of GBM cells co-cultured with cerebral brain organoids, reduces the expression of cell-cycle related genes in vivo and reduces the expression of invasion related genes within the non-proliferative cells present in tumors.

物理化学性质&存储条件

分子量	417.897
分子式	C23H20ClN5O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-(3-(2-(3-chlorophenyl)propan-2-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl)-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one

参考文献

1. Anna M Jermakowicz, et al. Sci Rep. 2021 Dec 3;11(1):23370.

UM-002 (UM002)

生物&药学活性

物理化学性质&存储条件

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UM-002 (UM002)

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