SKLB06329 

SKLB06329 is a potent selective Type I PRMTs inhibitor. SKLB06329 shows good selectivity for PRMT6 (IC₅₀ = 3.86 nM) over Type II/III PRMTs (PRMT5/7) and shows no significant inhibition against various lysine methyltransferases (PKMTs). SKLB06329 significantly inhibits the proliferation of triple-negative breast cancer (TNBC) cells, induces apoptosis, and suppresses the expression of asymmetric dimethylarginine (ADMA) within cells. SKLB06329 can be used for triple-negative breast cancer research^[1].

SKLB06329 (compound B9) (6 days) inhibits the proliferation of TNBC cells, with IC₅₀ values of 29.94 μM (MDA-MB-231) and 3.93 μM (Hs578T), with efficacy comparable to MS023 (HY-19615)^[1].
SKLB06329 forms hydrogen bonds with several amino acids in PRMT1, including Glu65, Met164, and Tyr170, and thus it potently inhibits type I PRMTs^[1].
SKLB06329 (5-40 μM) significantly inhibits colony formation in MDA-MB-231 and Hs578T cells, with reduction in colony numbers and decreased cell density per colony even at 5 μM^[1].
SKLB06329 (10-80 μM, 6 days) potently induces apoptosis, and inhibits ADMA expression in a concentration-dependent manner in TNBC (MDA-MB-231 and Hs578T) cells, indicating it inhibits the methylation function of type I PRMTs intracellularly^[1].
SKLB06329 (0-80 μM, 6 days) exhibits a PRMT1-dependent anti-proliferative effect in MDA-MB-231 cells^[1].

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

399.51

C₂₀H₂₅N₅O₂S

CN(CC1=NNC2=CC=C(C=C21)C3=CC=C(C=C3)NS(=O)(C4CC4)=O)CCN

Room temperature in continental US; may vary elsewhere.

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

• [1]. Zhang Q, et al. Discovery of novel indazole derivatives as type Ⅰ PRMTs inhibitors for the treatment of triple-negative breast cancer. Eur J Med Chem. 2025 Dec 15;300:118123.  [Content Brief]