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首页-小分子抑制剂&激动剂-Autophagy-GW296115
GW296115

Chemical Structure : GW296115

CAS No.: 118458-58-5

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GW296115 (GW-296115)

货号: PC-25750Not For Human Use, Lab Use Only.

GW296115 is a potent inhibitor of brain-specific serine/threonine protein kinases BRSK2 with IC50 of 8.4 nM and 21 nM for BRSK2 and BRSK1 respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

GW296115 is a potent inhibitor of brain-specific serine/threonine protein kinases BRSK2 with IC50 of 8.4 nM and 21 nM for BRSK2 and BRSK1 respectively.
GW296115 also inhibits DRAK2 (IC50 = 5.5 nM), PHKG1 (IC50 = 20 nM),, DRAK1 (IC50 = 28 nM), and DCAMKL3 (IC50 = 89 nM).
GW296115 engages BRSK2 in cells with an IC50 of 107 nM.
GW296115 also is an inhibitor of platelet-derived growth factor receptor-β (PDGFRβ), inhibits the autophosphorylation of the cytoplasmic domain of PDGFR both in vitro (IC50 = 1.8 uM) and in insect cells (IC50 = 2.0 uM).
GW296115 (1 uM) does not impact cell growth when profiled against 60 cancer cell lines.
GW296115 downregulates BRSK2-driven phosphorylation and downstream signaling.
GW296115 markedly reduces nutrient-deprivation stress-mediated autophagy, cell growth, and metastatic potential, and enhanced breast cancer cell apoptosis.
BRSK2, a marker of aggressive metastatic disease in breast cancer patients, is crucial in regulating autophagy.

物理化学性质&存储条件

分子量 385.38
分子式 C22H15N3O4
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

3,9-dimethoxy-12,13-dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione

参考文献

1. Tamir TY, et al. Sci Rep. 2020 Sep 28;10(1):15826.

2. Maiti A, et al. Sci Rep. 2025 Nov 19;15(1):40651.

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