MS3-123

MS3-123 (Compound 17zh) shows potent inhibition against PRMT1 (IC₅₀ = 11.4 nM) with high selectivity over other PRMT family members (17 to 439 fold), labels only a limited set of off-target cysteines at 50 μM, and exhibits weak activity against multiple other methyltransferases (G9a, EHMT1, MLL1, SMYD2, SETD8, EZH2, SUV39H1) (IC₅₀ > 10 μM), demonstrating an excellent selectivity profile^[1].
MS3-123 covalently binds to PRMT1 through a time-dependent inhibition mechanism (KI = 1.52 × 10⁴ M^-1s^-1)^[1].
MS3-123 induces thermal stabilization of PRMT1 protein (ΔTm = 2.0°C)^[1].
MS3-123 (130 μM; 1 h) covalently modifies PRMT1 at Cys119, forming a covalent complex with a mass shift of +419.2 Da^[1].
The alkyne-functionalized probe of MS3-123 (100-260 μM; 1 h) effectively labels and pulls down PRMT1 protein in recombinant protein and MCF-7 cell lysates^[1].
MS3-123 (0.2-3 μM; 12-84 h) concentration- and time-dependently reduces H4R3me2a and total ADMA levels in MCF-7 and MDA-MB-231 cells, with IC₅₀ values of 0.78 μM and 0.56 μM for H4R3me2a reduction at 72 h, respectively; and significantly reduces EZH2 protein levels and AKT phosphorylation in MCF-7 cells^[1].
MS3-123 (72 h) exhibits antiproliferative activity against MCF-7 and MDA-MB-231 cells, with GI₅₀ values of 4.40 μM and 4.76 μM, respectively, and shows low toxicity against normal mammary epithelial MCF-10A cells (GI₅₀ > 60 μM)^[1].
MS3-123 (0.3-3 μM; 8-day treatment) dose-dependently inhibits colony formation in MCF-7 and MDA-MB-231 cells, with near-complete inhibition observed at 3 μM^[1].
MS3-123 (0.75 μM) in combination with Gemcitabine (HY-17026) reduces the GI₅₀ in MCF-7 cells from 3.03 μM to 0.75 μM, demonstrating a synergistic effect, with a similar trend observed in MDA-MB-231 cells^[1].
MS3-123 (3-6 μM; 24 h) significantly inhibits the migration of MCF-7 and MDA-MB-231 cells^[1].
MS3-123 (3-6 μM; 24 h) dose-dependently inhibits the invasion of MDA-MB-231 cells, with inhibition rates of approximately 35.0% and 57.4%, respectively^[1].
MS3-123 (2-4 μM; 72 h) dose-dependently inhibits the invasion of MCF-7 cells, with inhibition rates of approximately 47.9% and 70.1%, respectively^[1].
MS3-123 (6-12 μM; 24 h) dose-dependently induces S-phase cell cycle arrest in MCF-7 and MDA-MB-231 cells, characterized by a significant increase in the S-phase cell population and a corresponding decrease in the G0/G1 and G2/M phase cell populations^[1].
MS3-123 (15-25 μM; 48 h) dose-dependently induces apoptosis in MCF-7 and MDA-MB-231 cells^[1].
MS3-123 (1.25 μM; 0-45 min) shows a metabolic half-life of 62.1 minutes in human liver microsomes and exhibits no significant inhibition against major CYP450 enzymes (IC₅₀ > 50 μM)^[1].
MS3-123 (250 μM; 0-180 min) shows a half-life of 80.9 minutes in a GSH reactivity assay under physiological pH conditions, indicating low intrinsic reactivity^[1].
MS3-123 (1 μM; 5 h) exhibits a human plasma protein binding rate of 34.7% and a free fraction of 65^[1].

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