CID-1067700 (ML282) is a competitive inhibitors of nucleotide binding by Ras-related GTPases with a Ki of 13 nM for Rab7. CID-1067700 (ML282) preventing BODIPY-linked GTP and GDP binding with EC50 values of 11.2 and 21 nM, respectively. CID-1067700 (0-40 μM) inhibits Rab7 activity, NF-κB activation as well as AID induction in B cells.
In vivo, CID-1067700 (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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO ≥ 60 mg/mL|
CID1067700, a late endosome GTPase Rab7 receptor antagonist, attenuates brain atrophy, improves neurologic deficits and inhibits reactive astrogliosis in rat ischemic stroke
Yuan Qin, et al. Acta Pharmacol Sin. 2019 Jun;40(6):724-736. PMID: 30315251.
Small Molecule Inhibition of Rab7 Impairs B Cell Class Switching and Plasma Cell Survival To Dampen the Autoantibody Response in Murine Lupus
Tonika Lam, et al. J Immunol. 2016 Nov 15;197(10):3792-3805. PMID: 27742832.
A competitive nucleotide binding inhibitor: in vitro characterization of Rab7 GTPase inhibition
Jacob O Agola, et al. ACS Chem Biol. 2012 Jun 15;7(6):1095-108. PMID: 22486388.
|Related Ras Products|
MLS000532223 is a selective inhibitor of Rho family GTPases, with EC50 ranging from 16 μM to 120 μM.
BI-3406 is a highly potent and selective SOS1::KRAS inhibitor (IC50=6 nM), which selectively binds to SOS1 and blocks the interaction with KRAS, irrespective of the KRAS mutation.
ZT-12-037-01 is a potent, selective, ATP-competitive STK19 inhibitor with IC50 values of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N), respectively.
BI-2852 is a potent KRAS inhibitor that binds with nanomolar affinity to a pocket.
MRTX849 (Adagrasib) is a potent, highly selective, oral available KRAS G12C inhibitor.
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