CARM1-IN-5 

CARM1-IN-5 (Compound 17e) is a potent and selective inhibitor of CARM1 (IC₅₀= 2 nM). CARM1-IN-5 effectively prevents CARM1 from methylating substrate proteins by directly interacting with CARM1. CARM1-IN-5 exhibits significant antiproliferative effects on melanoma cell lines^[1].

CARM1-IN-5 is selective for CARM1. IC₅₀ is 2 ± 1 nM (CARM1), 213 ± 45 nM (PRMT1), 942 ± 78 nM (PRMT3), 64 ± 9 nM (PRMT6), 73 ± 8 nM (PRMT8), >100,000 nM ( PRMT5), >100,000 nM (PRMT7)^[1].
CARM1-IN-5 antiproliferative activity against two melanoma cell lines was IC₅₀ = 0.55 ± 0.03 μM (A375); 1.74 ± 0.07 μM (A2058)^[1].
CARM1-IN-5 (0-5 μM; 72 h) can enter A375 Cells and bind directly to CARM1. CARM1-IN-5 also can affect the level of asymmetric dimethylation of CARM1 substrates in the cellular environment by inhibiting the methyltransferase activity of CARM1^[1].


In vitro metabolic stability in Mouse Liver Microsomes^[1]

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

CARM1-IN-5 (i.p.; 10 mg/kg/day and 25 mg/kg/day; 14 days) inhibits tumor growth in BALB/c nude mice bearing subcutaneous A375 xenograft^[1].

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

431.98

C₂₂H₂₆ClN₃O₂S

CN(CC1=CC=CC=C1OCC2=CC(Cl)=C(C=C2)C3=NC=CS3)C[C@H](CNC)O

Room temperature in continental US; may vary elsewhere.

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

• [1]. Liu Z, et al. Development of (2-(Benzyloxy)phenyl)methanamine Derivatives as Potent and Selective Inhibitors of CARM1 for the Treatment of Melanoma. J Med Chem. 2024 Apr 25;67(8):6313-6326.  [Content Brief]