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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-STAT-BMA097
BMA097

Chemical Structure : BMA097

CAS No.: 2045392-40-1

BMA097 (BMA-097)

货号: PC-24628Not For Human Use, Lab Use Only.

BMA097 is a small molecule STAT3 inhibitor with IC50 of 1.8 uM in STAT3-dependent luciferase assays, binds directly to the SH2 domain of STAT3 and specifically inhibits STAT3 Tyr705 phosphorylation and activation.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

BMA097 is a small molecule STAT3 inhibitor with IC50 of 1.8 uM in STAT3-dependent luciferase assays, binds directly to the SH2 domain of STAT3 and specifically inhibits STAT3 Tyr705 phosphorylation and activation.
BMA097 inhibited the expression of STAT3 target genes, cyclin D1 and Bcl-xL.
BMA097 suppresses Tyr705 phosphorylation and activation of STAT3, but not the phosphorylation of Ser727, also has little effect on the level of total STAT3.
BMA097 treatment reduced IL-6-induced phosphorylation and activation of STAT3 in serum-starved MDA-MB-231 cells.
BMA097 inhibits STAT3 activation (phosphorylation and dimerization) and translocation into nucleus.
BMA097 does not inhibit STAT3 upstream kinase JAK2.
BMA097 inhibits survival and induces apoptosis of breast cancer cells, with IC50 of 0.9, 1.8, and 3.9 μM, respectively for MDA-MB-231, MDA-MB-468, and MCF7 (72 h).
BMA097 (10 and 40 mg/kg) suppresses growth of xenograft tumors and STAT3 activation in vivo.

物理化学性质&存储条件

分子量 461.53
分子式 C28H23N5O2
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

2,3-bis[1-(3-cyanopropyl)-1H-indol-3-yl]maleimide

参考文献

1. Xia Li, et al. Oncogene. 2018 May;37(18):2469-2480.

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