CDK/HDAC-IN-3 

CDK/HDAC-IN-3 is an orally active HDACs/CDKs dual inhibitor. CDK/HDAC-IN-3 has potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2 and HDAC3 with IC₅₀ values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28nM and 82.87 nM. CDK/HDAC-IN-3 can be used for the acute myeloid leukemia (AML) ^[1].

IC50: 98.32 nM (CDK9), 98.85 nM (CDK12), 100 nM (CDK13), 62.12 nM (HDAC1), 93.28nM (HDAC2) and 82.87 nM (HDAC3), 0.72 μM (U937 cell), 1.43μM (HL-60 cell), 1.63μM (SKNO-1 cell) and 0.89 μM (Kaumi-1 cell)^[1].

CDK/HDAC-IN-3 (compound 33a) (1μM) has potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2 and HDAC3 with IC₅₀ values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28nM and 82.87 nM, respectively^[1].
CDK/HDAC-IN-3 (0.5 μM, 1.0 μM) significantly induces differentiation of leukemic stem-like cells and inhibits AML proliferation^[1].
CDK/HDAC-IN-3 (0.5 μM, 1.0 μM, 2.0 μM) significantly induced differentiation of LSCs^[1].
CDK/HDAC-IN-3 has inhibitory effect for U937, HL-60, SKNO-1 and Kaumi-1 cell with IC₅₀ values of 0.72 μM, 1.43μM, 1.63μM and 0.89 μM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CDK/HDAC-IN-3 (compound 33a) (i.v., p.o.; 5, 25 mg/kg) has relatively adequate oral bioavailability^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

509.34

C₂₄H₁₈Cl₂N₆O₃

2944087-54-9

NC1=C(C=CC=C1)NC(C2=CC=C(C=C2)NC(C3=NNC=C3NC(C4=C(C=CC=C4Cl)Cl)=O)=O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Liu Y, et al. Discovery of novel and bioavailable histone deacetylases and cyclin-dependent kinases dual inhibitor to impair the stemness of leukemia cells. Eur J Med Chem. 2023;249:115140.  [Content Brief]