Description
ML-240 is an ATP-competitive inhibitor of the D2 domain of the p97 ATPase (IC₅₀ = 110 nM). It disrupts the endoplasmic reticulum-associated degradation 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.
ML-240 is an ATP-competitive inhibitor of the D2 domain of the p97 ATPase (IC₅₀ = 110 nM). It disrupts the endoplasmic reticulum-associated degradation 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.
Alternate Name/Synonyms: 2-(2-Amino-1H-benzimidazole-1-yl)-8-methoxy-N-(phenylmethyl)-4-quinazolinamine
Appearance: White Solid
Formulation: N/A
CAS Number: 1346527-98-7
Structure Available?: Yes
Peptide sequence: N/A
Salt Form: No
Molecular Formula: C₂₃H₂₀N₆O
Molecular Weight: 396.44
Cell-Permeable?: Yes
Purity: ≥98% by HPLC
Solubilities: DMSO (>5 mg/ml)
Handling: Protect from air and light
Country of Origin: USA
Tag Line: An ATP-competitive inhibitor of the D2 domain of the p97 ATPase
MDL Number: N/A
PubChem CID: 49830258
SMILES: COC1=CC=CC2=C1N=C(N=C2NCC3=CC=CC=C3)N4C5=CC=CC=C5N=C4N
InChi: 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
Additional Information
Storage Condition: |
-20°C |
Shipping Condition: |
Gel Pack |
Shelf Life: |
36 months |