SGC0946

• CAT Number: I001980
• CAS Number: 1561178-17-3
• Molecular Formula: C₂₈H₄₀BrN₇O₄
• Molecular Weight: 618.57
• Purity: ≥95%
• Target: Histone Methyltransferase
• Solubility: DMSO: ≥ 50 mg/mL
• Storage: 3 years -20C powder
• IC50: 0.3 nM(DOT1L) [1]
• IUPAC Name: 1-[3-[[(2R,3S,4R,5R)-5-(4-amino-5-bromopyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxyoxolan-2-yl]methyl-propan-2-ylamino]propyl]-3-(4-tert-butylphenyl)urea
• InChI: InChI=1S/C28H40BrN7O4/c1-16(2)35(12-6-11-31-27(39)34-18-9-7-17(8-10-18)28(3,4)5)14-20-22(37)23(38)26(40-20)36-13-19(29)21-24(30)32-15-33-25(21)36/h7-10,13,15-16,20,22-23,26,37-38H,6,11-12,14H2,1-5H3,(H2,30,32,33)(H2,31,34,39)/t20-,22-,23-,26-/m1/s1
• InChIKey: IQCKJUKAQJINMK-HUBRGWSESA-N
• SMILES: CC(C)N(CCCNC(=O)NC1=CC=C(C=C1)C(C)(C)C)C[C@@H]2[C@H]([C@H]([C@@H](O2)N3C=C(C4=C(N=CN=C43)N)Br)O)O

SGC0946（Cat No.:I001980）is a potent and selective inhibitor of the histone methyltransferase EZH2, a key enzyme in the Polycomb repressive complex 2 (PRC2) that regulates gene expression through the trimethylation of histone H3 at lysine 27 (H3K27me3). By targeting EZH2, SGC0946 disrupts oncogenic signaling and can reactivate silenced tumor suppressor genes. This compound has shown significant anti-tumor activity in preclinical studies, particularly in hematological malignancies and solid tumors characterized by aberrant EZH2 activity. SGC0946’s ability to modulate epigenetic regulation positions it as a promising candidate for targeted cancer therapies.

Reference

[1]. Yu W, et al. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat Commun. 2012;3:1288. doi: 10.1038/ncomms2304.