UNC0379

SET domain-containing protein 8 (SET8) is a methyltransferase that selectively mono-methylates histone H4 at lysine residue 20, an event proven to have an important role in chromatin structure and transcriptional activation. It is also a regulator of p53, mono-methylating lysine 382 of the tumor suppressor. UNC0379 is a substrate-competitive inhibitor of the lysine methyltransferase SET8 (IC50 = 7.3 µM, Kd = 18.3 µM). It is selective for SET8 over 15 other methyltransferases, including G9a and GLP (IC50s = >100 µM).Formal Name: 6,7-dimethoxy-2-(1-pyrrolidinyl)-N-[5-(1-pyrrolidinyl)pentyl]-4-quinazolinamine. CAS Number: 1620401-82-2. Molecular Formula: C23H35N5O2. Formula Weight: 413.6. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 10 mg/ml. lambdamax: 210, 249, 345 nm. SMILES: COC1=C(OC)C=C(N=C(N2CCCC2)N=C3NCCCCCN4CCCC4)C3=C1. InChi Code: InChI=1S/C23H35N5O2/c1-29-20-16-18-19(17-21(20)30-2)25-23(28-14-8-9-15-28)26-22(18)24-10-4-3-5-11-27-12-6-7-13-27/h16-17H,3-15H2,1-2H3,(H,24,25,26). InChi Key: WEXCGGWTIDNVNT-UHFFFAOYSA-N.