RelB inhibitor RS47

Chemical Structure : RelB inhibitor RS47

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货号: PC-24073Not For Human Use, Lab Use Only.

规格	价格	库存	数量
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote

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生物&药学活性

RelB inhibitor RS47 is a potent and specific small molecule targeting RelB (MST, binding Kd=1.1 uM) to inhibit non-canonical NF-κB signaling pathway, with no inhibitory effect on canonical NF-κB signaling pathway.
RS47 inhibitsHCT116 cell viability with IC50 of 1.28 uM, also significantly suppresses the viability of colorectal cancer cell lines (RKO) and breast cancer cell line (MDA-MB-231).
RS47 blocks non-canonical NF-κB signaling pathway through interacting with RelB, RS47 could pull down endogenous RelB protein in HCT116 cells directly, but not NIK and p100.
RS47 interrupts RelB binding to its target DNA, thus inhibiting expression of genes induced by BAFFactivated non-canonical NF-κB signaling pathway.
RS47 represses BAFF-induced survival of primary B lymphoma cells significantly.
RS47 suppresses human colorectal cancer (CRC) cells proliferation and promote cells apoptosis, promotes human B lymphoma cells apoptosis in vitro.
RS47 inhibits tumorigenesis of human B lymphoma from PDX in xenograft model.

物理化学性质&存储条件

分子量	354.43
分子式	C18H18N4O2S
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	(E)-2-(1-(2-(5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-yl)hydrazineylidene)ethyl)benzene-1,4-diol

参考文献

1. Li C, et al. Mol Ther. 2025 Feb 4:S1525-0016(25)00085-1.