An ATP-competitive inhibitor of the D2 domain of the p97 ATPase (IC50 = 0.11 µM; Ki = 0.22 µM); disrupts ERAD and autophagy pathways; blocks proliferation of HCT15 and SW403 colon cancer cell lines (GI50s = 0.76 and 0.5 µM

ML-240 – 1 mg

Brand:
Cayman
CAS:
1346527-98-7
Storage:
-20
UN-No:
Non-Hazardous - /

ML-240 is an ATP-competitive inhibitor of the D2 domain of the ATPase p97 (IC50 = 0.11 µM; Ki = 0.22 µM).{28269,28270} 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.{28269} 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.{28269}  

 

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Description

An ATP-competitive inhibitor of the D2 domain of the p97 ATPase (IC50 = 0.11 µM; Ki = 0.22 µM); disrupts ERAD and autophagy pathways; blocks proliferation of HCT15 and SW403 colon cancer cell lines (GI50s = 0.76 and 0.5 µM, respectively), rapidly mobilizing caspase-3 and -7 to induce apoptosis

Formal name: 2-(2-amino-1H-benzimidazol-1-yl)-8-methoxy-N-(phenylmethyl)-4-quinazolinamine

Synonyms: 

Molecular weight: 396.4

CAS: 1346527-98-7

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|ATPases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cell Biology|Cell Death|Apoptosis||Research Area|Cell Biology|Cell Signaling||Research Area|Cell Biology|Endomembrane System & Vesicular Trafficking|Autophagy||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System

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