ADSS2-IN-1
ADSS2-IN-1 is a ADSS2 inhibitor. ADSS2-IN-1 inhibits de novo AMP biosynthesis by targeting ADSS2, downregulates AMPK activity and promotes mitophagy in drug-resistant cells. ADSS2-IN-1 alone induces mild apoptosis in acute myeloid leukemia cells, and acts synergistically with BH3 mimetics to enhance the apoptotic effect. ADSS2-IN-1 restores the sensitivity of drug-resistant acute myeloid leukemia cells and reduces disease burden in immunocompetent mouse models. ADSS2 antagonist-1 can be used for the research of acute myeloid leukemia.
For research use only. We do not sell to patients.
- CAS No.: 375394-74-4
- Formula: C11H11N5
- Molecular Weight:213.24
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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- References
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Biological Activity
ADSS2-IN-1 (Compound 3) (2.5-10 μM; 72 h) acts synergistically with Venetoclax (HY-15531) to reduce cell viability when co-treated with BH3 mimetic-resistant P1-R, P2-R and P3-R AML cells[1].
ADSS2-IN-1 exhibits strong synergistic activity with BH3 mimetics (Venetoclax or S63845 (HY-100741)) in P4 acute myeloid leukemia (AML) cells, with a ZIP synergy score > 10, but shows no synergistic effect with the menin inhibitor Ziftomenib (HY-132001)[1].
ADSS2-IN-1 (2.5-10 μM; 72 h) enhances the Venetoclax-mediated reduction in cell viability and decreases the IC50 of Venetoclax when co-treatmented MA9/p53-KD mouse AML cells[1].
ADSS2-IN-1 alone induces mild apoptosis; in combination with Venetoclax, it triggers robust apoptosis in primary Venetoclax-resistant AML patient cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BH3 mimetic-resistant acute myeloid leukemia (AML) cell lines (P1-R, P2-R, P3-R cells)
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Concentration:2.5 μM, 5 μM, 10 μM
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Incubation Time:72 h
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Result:Synergistically eliminated BH3 mimetic-resistant P1-R, P2-R, and P3-R AML cells when combined with Venetoclax.
Showed minimal effect on cell viability when used alone.
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Cell Line:Double-hit murine AML cells (MA9/p53-KD cells)
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Concentration:2.5 μM, 5 μM, 10 μM
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Incubation Time:72 h
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Result:Enhanced Venetoclax-mediated reduction of cell viability in MA9/p53-KD cells when co-treated with Venetoclax.
Lowered the Venetoclax IC50 value in MA9/p53-KD cells when co-treated with Venetoclax.
ADSS2-IN-1 (100 mg/kg; i.p.; once daily; 5 times per week for 4 weeks) is well tolerated in wild-type C57BL/6 mice, with no toxicity detected in key organs or hematopoietic compartments[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 CD45.1 (male and female, non-irradiated wild-type recipients injected with MA9/p53-KD cells)[1]
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Dosage:100 mg/kg
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Administration:i.p.; once daily; 5 consecutive days; 3 weeks
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Result:Reduced leukemia burden as measured by bioluminescent radiance (short-term 5-day treatment).
Modestly increased total and CD69+ T cells in bone marrow (short-term 5-day treatment).
Reduced leukemia burden measured by bioluminescent radiance (long-term 3-week treatment).
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Animal Model:C57BL/6 (male and female, wild-type)[1]
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Dosage:100 mg/kg
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Administration:i.p.; once daily; 5 times per week; 4 weeks
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Result:Showed no significant changes in body weight.
Showed no significant changes in bone marrow hematopoietic progenitor or mature lineage cell frequencies.
Showed no detectable histology abnormalities in kidney, liver, and spleen.
Chemical Information
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CAS No. 375394-74-4
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Molecular Weight 213.24
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Formula C11H11N5
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SMILES
CC1=NN(C(N)=C1)C2=NC3=C(N2)C=CC=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ADSS2-IN-1 Related Classifications
HY-W264185 Related Classifications
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