1. Metabolic Enzyme/Protease Apoptosis
  2. Adenosine Deaminase Apoptosis
  3. ADAR1-IN-1

ADAR1-IN-1 is a potent ADAR1 inhibitor. ADAR1-IN-1 significantly suppressed DU-145 cell proliferation (IC50 = 1.11 μM), clonogenicity, migration, and invasion, arrests cell cycle, and induces apoptosis. ADAR1-IN-1 safely and effectively inhibits tumor growth. ADAR1-IN-1 can be used for the study of prostate cancer (PCa).

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

ADAR1-IN-1

ADAR1-IN-1 Chemical Structure

CAS No. : 2734853-87-1

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Description

ADAR1-IN-1 is a potent ADAR1 inhibitor. ADAR1-IN-1 significantly suppressed DU-145 cell proliferation (IC50 = 1.11 μM), clonogenicity, migration, and invasion, arrests cell cycle, and induces apoptosis. ADAR1-IN-1 safely and effectively inhibits tumor growth. ADAR1-IN-1 can be used for the study of prostate cancer (PCa)[1].

In Vitro

ADAR1-IN-1 (Compound C12) (1-3 μM, 1-4 days) significantly inhibits the growth and colony formation of DU-145 cells at a concentration of 1 μM, with maximal inhibition observed at 3 μM[1].
ADAR1-IN-1 (1-3 μM, 24 h) dose-dependently inhibits the migration and invasion of DU-145 cells by [1].
ADAR1-IN-1 (1-3 μM, 24-48 h) significantly arrests DU-145 cells in the G0/G1 phase and induces apoptosis in a dose-dependent manner[1].
ADAR1-IN-1 (1-3 μM, 48 h) induces a downregulation of N-cadherin and vimentin and a upregulation of p53[1].
ADAR1-IN-1 (72 h) exhibits significant proliferation inhibition against androgen receptor-dependent VCaP cells, castration-resistant 22Rv1 cells, and AR-negative PC-3 cells with IC50 values of 1.76 μM, 1.79 μM, and 0.72 μM, respectively[1].

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

Cell Migration Assay [1]

Cell Line: DU-145 cells
Concentration: 1, 2 and 3 μM
Incubation Time: 24 h
Result: Dose-dependently inhibited the migration.

Cell Cycle Analysis[1]

Cell Line: DU-145 cells
Concentration: 1, 2 and 3 μM
Incubation Time: 24 h
Result: Arrested cells in the G0/G1 phase.

Apoptosis Analysis[1]

Cell Line: DU-145 cells
Concentration: 1, 2 and 3 μM
Incubation Time: 24 h
Result: Induced apoptosis in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: DU-145 cells
Concentration: 1, 2 and 3 μM
Incubation Time: 48 h
Result: Induced a concentration-dependent downregulation of N-cadherin and vimentin. Decreased CDk6 and c-MYC, and increased p53.
In Vivo

ADAR1-IN-1 (Compound C12) (15-30 mg/kg, i.p., twice daily for 19 days) has potent antitumor efficacy and safety properties in DU-145 and 22Rv1 xenograft mice models[1].

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

Animal Model: DU-145 and 22Rv1 xenograft models established in male BALB/c nude mice[1]
Dosage: 15 and 30 mg/kg
Administration: Intraperitoneal injection (i.p.), twice daily for 19 days
Result: Significantly inhibited tumor growth with tumor growth inhibition (TGI) rates of 41.8% and 52.8%, respectively in DU-145 model and 46.4% and 59.0%, respectively in 22Rv1 model.
No obvious lesions were observed in the main organs of the mice.
Molecular Weight

493.39

Formula

C17H15F4N5O6S

CAS No.
SMILES

O[C@@H]1[C@H](O)[C@@H](COS(=O)(C2=CC=C(C=C2)C(F)(F)F)=O)O[C@H]1N3C4=NC(F)=NC(N)=C4N=C3

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

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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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ADAR1-IN-1
Cat. No.:
HY-175243
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