Chemical Structure : SIAIS361034
货号: PC-23129Not For Human Use, Lab Use Only.
SIAIS361034 is a potent, selective PROTAC degrader of Bcl-xL, selectively degrades Bcl-xL and significantly inhibits the Hh pathway activity SIAIS361034 with IC50 of 120 nM.
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SIAIS361034 is a potent, selective PROTAC degrader of Bcl-xL, selectively degrades Bcl-xL and significantly inhibits the Hh pathway activity SIAIS361034 with IC50 of 120 nM.
SIAIS361034 binds to Bcl-xL and Bcl-2 with Ki values of 37.27 nM and 15.09 nM, respectively, but exhibits little affinity to Mcl-1.
SIAIS361034 potently degrades Bcl-xL via CRBN E3 ubiquitin ligase and ubiquitin proteasome system.
SIAIS361034 significantly degrades Bcl-xL and did not change the levels of Bcl-2 and Mcl-1.
SIAIS361034 inhibits the Hh signaling pathway by disabling Bcl-xL/Sufu interaction.
SIAIS361034 possesses the ability of combating resistance to Smo inhibitors caused by Smo mutations and Gli2 amplification.
SIAIS361034 10 mg/kg oral (p.o.) administration retards hair growth in a depilatory model by inhibiting the Hh pathway activity.
分子量 | 1159.78 | |
分子式 | C58H66ClF3N8O8S2 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Shaoqing Zhang, et al. Theranostics. 2022 Oct 24;12(17):7476-7490.
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