ML-240

ML-240 is an ATP-competitive inhibitor of the D2 domain of the ATPase p97 (IC50 = 0.11 µM, Ki = 0.22 µM). It disrupts the endoplasmic reticulum-associated degradation (ERAD) and autophagy pathways, preventing the degradation of p97-dependent proteasome substrates (IC50 = 0.9 µM) and causing accumulation of ubiquitin conjugates in nuclear membrane and cytosolic compartments at 5-10 µM. ML-240 has also been shown to block proliferation of HCT15 and SW403 colon cancer cell lines (GI50s = 0.76 and 0.5 µM, respectively) and to rapidly mobilize caspase-3 and -7, inducing apoptosis.Formal Name: 2-(2-amino-1H-benzimidazol-1-yl)-8-methoxy-N-(phenylmethyl)-4-quinazolinamine. CAS Number: 1346527-98-7. Molecular Formula: C23H20N6O. Formula Weight: 396.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMSO: 1 mg/ml, DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml. lambdamax: 254, 304 nm. SMILES: COC1=C2C(C(NCC3=CC=CC=C3)=NC(N4C(C=CC=C5)=C5N=C4N)=N2)=CC=C1. InChi Code: InChI=1S/C23H20N6O/c1-30-19-13-7-10-16-20(19)27-23(28-21(16)25-14-15-8-3-2-4-9-15)29-18-12-6-5-11-17(18)26-22(29)24/h2-13H,14H2,1H3,(H2,24,26)(H,25,27,28). InChi Key: NHAMBLRUUJAFOY-UHFFFAOYSA-N.