Chemical Structure : SIAIS361034
CAS No.:
2641287-90-1
SIAIS361034
(SIAIS 361034)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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1159.78
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Formula
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C58H66ClF3N8O8S2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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4-(4-((4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((4-((3-(4-(5-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)pent-4-yn-1-yl)piperazin-1-yl)propyl)amino)-3-((trifluoromethyl)sulfonyl)phenyl)sulfonyl)benzamide
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References
1. Shaoqing Zhang, et al. Theranostics. 2022 Oct 24;12(17):7476-7490.
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