CM-272 is a first-in-class reversible dual small molecule inhibitor against G9a and DNMTs in hematological malignancies. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC50s of 8 nM, 382 nM, 85 nM, 1200nM and 2 nM, respectively.
|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.
|Related Histone Methyltransferase Products|
EZM0414 is a potent, selective, oral bioavailable SETD2 inhibitor (IN SETD2 biochemical analysis, IC50=18 nM; In cell analysis, IC50=34 nM). EZM0414 can be used to study relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma.
GNA002 is a potent, selective, covalent EZH2 inhibitor with an IC50 of 1.1 μM against EZH2. GNA002 can specifically and covalently bind Cys668 in the EZH2-SET domain to induce EZH2 degradation through COOH terminal of ubiquitination mediated by Hsp70 interacting protein (CHIP). GNA002 effectively reduced EZH2-mediated H3K27 trimethylation and reactivated tumor suppressor genes silenced by Polycomb repressor complex 2 (PRC2).
Pf-06726304 is an effective selective EZH2 inhibitor. Pf-06726304 inhibited wild type and Y641N mutant EZH2 with Ki of 0.7 and 3.0 nM, respectively. Pf-06726304 has strong anti-tumor growth activity.
Cpi-169 (CPI 169 R-Enantiomer) is a novel and effective EZH2 inhibitor, capable of inhibiting the activity of EZH2 WT, EZH2 Y641N and EZH1 with IC50 value of 0.24 nM, respectively. 0.51 nM and 6.1 nM.
EI1 (KB-145943) is a novel and effective EZH2 inhibitor, capable of acting on EZH2 (WT) and EZH2 (Y641F) with IC50 values of 15 nM and 13 nM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.