MRT199665

• CAT Number: I017418
• CAS Number: 1456858-57-3
• Molecular Formula: C₂₈H₃₁N₅O₂
• Molecular Weight: 469.58
• Purity: ≥95%
• IUPAC Name: 7-[(1S)-4-hydroxy-2,3-dihydro-1H-inden-1-yl]-5,5-dimethyl-2-[3-(pyrrolidin-1-ylmethyl)anilino]pyrrolo[2,3-d]pyrimidin-6-one
• InChI: InChI=1S/C28H31N5O2/c1-28(2)22-16-29-27(30-19-8-5-7-18(15-19)17-32-13-3-4-14-32)31-25(22)33(26(28)35)23-12-11-21-20(23)9-6-10-24(21)34/h5-10,15-16,23,34H,3-4,11-14,17H2,1-2H3,(H,29,30,31)/t23-/m0/s1
• InChIKey: OFIFLUFVENTCNZ-QHCPKHFHSA-N
• SMILES: CC1(C2=CN=C(N=C2N(C1=O)C3CCC4=C3C=CC=C4O)NC5=CC=CC(=C5)CN6CCCC6)C

MRT199665 (Cat No.:I017418) is a small molecule inhibitor that targets the WDR5-MLL interaction, which is essential for the activity of the MLL family of histone methyltransferases. By inhibiting this interaction, MRT199665 prevents the methylation of histone H3 lysine 4 (H3K4) and the expression of genes that promote cancer cell proliferation and survival. Preclinical studies have shown that MRT199665 has potent antitumor activity in leukemia and solid tumor models.

Reference

[1]. Clark K, et al. Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proc Natl Acad Sci U S A. 2012 Oct 16;109(42):16986-91.[2]. Brown FC, et al. MEF2C Phosphorylation Is Required for Chemotherapy Resistance in Acute Myeloid Leukemia. Cancer Discov. 2018 Apr;8(4):478-497.[3]. Hutchinson LD, et al. Salt-inducible kinases (SIKs) regulate TGFβ-mediated transcriptional and apoptotic responses.Cell Death Dis. 2020 Jan 22;11(1):49.