CID-1067700,314042-01-8

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抑制剂描述：

产品名称：CID-1067700

产品别名：见爱必信官网

英文别名：CID-1067700

靶点：Ras

CAS：314042-01-8

纯度：98%

外观：见爱必信官网

保存方法：Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

描述：CID-1067700 is a pan GTPase inhibitor, and competitively inhibits Ras-related in brain 7 (Rab7) with a Ki of 13 nM.

溶解性：DMSO : 75 mg/mL (192.07 mM; Need ultrasonic)

体外研究：

CID-1067700 (ML282) is a pan GTPase inhibitor, and competitively inhibits Rab7 with a Ki of 13 nM. CID-1067700 shows inhibitory activity against nucleotide binding by Rab7, with Kds of 100 nM and 40 nM for BODIPY-GTP and BODIPY-GDP, respectively. With increasing concentration, CID-1067700 causes strong inhibition on binding of the BODIPY-linked nucleotides, with EC50 values of 11.22 ± 1.34 nM for BODIPY-GTP and 20.96 ± 1.34 nM for BODIPY-GDP and calculated Ki values of 12.89 nM and 19.70 nM respectively. CID-1067700 (10 μM) has no effect on the rate of release of bound BODIPY-linked nucleotide by wild type Rab7 under equilibrium binding conditions. CID-1067700 (0-40 μM) inhibits Rab7 activity, NF-κB activation as well as AID induction in B cells. Furthermore, CID-1067700 binds Rab7 with a high affinity (EC50: 10-20 nM), and blocks Class switch DNA recombination (CSR) in B cells via targeting Rab7.

体内研究：CID-1067700 (ML282; 16 mg/kg, i.p.) prevents disease development in lupus-prone mice by Rab7 inhibition, and reduces IgG-IC deposition in MRL/Faslpr/lpr mice. CID-1067700 also targets B cells and specifically impairs the CSR machinery in vivo.

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