PROTAC CARM1 degrader-1 hydrochloride

CARM1 degrader-1 (compound 3b) (6.25-500 nM, 0.1-10 μM; 1-48 h) hydrochloride potently degrades CARM1 in MCF7 cells with a DC₅₀ of 8.1 nM and 97% maximal degradation, achieving significant degradation within 2 h and sustaining it for up to 48 h^[1].
CARM1 degrader-1 (0.5 μM; 24 h) hydrochloride degrades CARM1 in MCF7 cells in a CARM1-binding-, VHL-, proteasome-, and neddylation-dependent manner^[1].
CARM1 degrader-1 (0.01-10 μM, 25 nM; 4-24 h) hydrochloride exerts highly selective degradation of CARM1 over PRMT1, PRMT6, and PRMT5 in MCF7 cells, with minimal off-target proteome effects^[1].
CARM1 degrader-1 (0.1-10 μM, 0.5 μM; 2-48 h) hydrochloride potently inhibits asymmetric dimethylation of CARM1 substrates BAF155 and PABP1 in MCF7, BT474, and MDA-MB-231 breast cancer cells, with at least 100-fold greater functional potency than the CARM1 inhibitor TP-064 in MCF7 cells^[1].
CARM1 degrader-1 (0.5 μM; 20 h) hydrochloride potently inhibits migration of MDA-MB-231 triple-negative breast cancer cells^[1].
CARM1 degrader-1 hydrochloride potently degrades CARM1 in MCF10A normal human mammary epithelial cells^[1].
CARM1 degrader-1 hydrochloride (7 days) does not inhibit proliferation of MCF7, MCF10A, or MDA-MB-231 cells^[1].

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