CAS NO: | 314042-01-8 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | CID-1067700 (ML282) is a panGTPaseinhibitor, and competitively inhibits Ras-related in brain 7 (Rab7) with aKiof 13 nM. | ||||||||||||||||
IC50& Target | Ki: 13 nM (Rab7)[1] | ||||||||||||||||
体外研究 (In Vitro) | CID-1067700 (ML282) is a pan GTPase inhibitor, and competitively inhibits Rab7 with a Kiof 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 EC50values of 11.22 ± 1.34 nM for BODIPY-GTP and 20.96 ± 1.34 nM for BODIPY-GDP and calculated Kivalues 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[1]. 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[2]. | ||||||||||||||||
体内研究 (In Vivo) | 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/lprmice. CID-1067700 also targets B cells and specifically impairs the CSR machinery in vivo[2]. | ||||||||||||||||
分子量 | 390.48 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C18H18N2O4S2 | ||||||||||||||||
CAS 号 | 314042-01-8 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 12.5 mg/mL(32.01 mM;Need ultrasonic) 配制储备液
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