1. Metabolic Enzyme/Protease
  2. ATP Citrate Lyase
  3. EVT0185

EVT0185 is an orally active ATP citrate lyase (ACLY) inhibitor. EVT0185 is converted to a CoA thioester in the liver by SLC27A2 and interacts with the CoA-binding site of ACLY. EVT0185-CoA inhibits ACLY activity with an IC50 of 2.5 μM. EVT0185 can phenocopy the immune and antitumour effects of genetic ACLY deletion. EVT0185 can increases tumour-infiltrating B cells and chemokine CXCL13 levels. EVT0185 can be used for the research of cancer, such as hepatocellular carcinoma (HCC).

For research use only. We do not sell to patients.

EVT0185

EVT0185 Chemical Structure

CAS No. : 2588489-03-4

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Description

EVT0185 is an orally active ATP citrate lyase (ACLY) inhibitor. EVT0185 is converted to a CoA thioester in the liver by SLC27A2 and interacts with the CoA-binding site of ACLY. EVT0185-CoA inhibits ACLY activity with an IC50 of 2.5 μM. EVT0185 can phenocopy the immune and antitumour effects of genetic ACLY deletion. EVT0185 can increases tumour-infiltrating B cells and chemokine CXCL13 levels. EVT0185 can be used for the research of cancer, such as hepatocellular carcinoma (HCC)[1].

In Vitro

EVT0185 inhibits lipogenesis with an IC50 of 0.46 μM in hepatocytes[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

EVT0185 (30-100 mg/kg, i.g., for 1 month) reduces tumour burden in MASH-HCC mice models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Metabolic dysfunction-associated steatohepatitis (MASH)-driven hepatocellular carcinoma (HCC) mice models[1]
Dosage: 30 and 100 mg/kg
Administration: Orally gavaged, 1 month
Result: Reduced tumor numbers in liver.
Reduced tumour surface area and lipid accumulation.
Elevated levels of AFP.
Increased B cells and B cell chemoattractant CXCL13 levels.
Increased cleaved caspase 3 levels and reduced Ki67 levels.
Molecular Weight

362.50

Formula

C22H34O4

CAS No.
SMILES

O=C(O)C(C)(C)CCCCC1=CC=C(CCCCC(C)(C(O)=O)C)C=C1

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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EVT0185
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HY-175606
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