YSA64
YSA64 is an orally active RBM39-targeting molecular glue. YSA64 promotes degradation via formation of a DCAF15/DDB1 ternary complex, dependent on Cullin-RING E3 ligase and proteasome activity. YSA64 can be used for the research of acute myeloid leukemia and Ewing sarcoma.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C25H24N4O3S
- Masse moléculaire:460.55
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Stockage:
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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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
YSA64 (Compound 41) (4 days) potently inhibits HCT-116 colorectal cancer cell proliferation with an IC50 of 166 nM[1].
YSA64 (0.05-0.8 μM; 24 h) induces robust degradation of RBM39 in HCT-116 colorectal cancer cells[1].
YSA64 (4 days) inhibits proliferation of multiple cancer cell lines with varying potency, showing highest activity in A673 Ewing sarcoma (IC50 = 125.3 nM) and MV4-11 acute myeloid leukemia (IC50 = 111.7 nM) cells[1].
YSA64 (24 h) induces robust degradation of RBM39 and CEP192 in A673 Ewing sarcoma cells[1].
YSA64-induced RBM39 degradation in A673 Ewing sarcoma cells requires intact proteasome and Cullin-RING E3 ligase activity[1].
YSA64 (24 h) induces dose-dependent degradation of RBM39 and CEP192 in MV4-11 acute myeloid leukemia cells following 24 h incubation, with RBM39 degradation potency comparable to E7820[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116 colorectal cancer cells
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Concentration:0.05 μM; 0.2 μM; 0.8 μM
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Incubation Time:24 h
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Result:Robustly reduced RBM39 protein levels at all tested concentrations.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID mice (male; 3-4 weeks old; subcutaneously implanted with MV4-11 cells to establish a xenograft model)[1]
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Dosage:100 mg/kg; 150 mg/kg; 200 mg/kg
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Administration:p.o.; once daily; 10 days
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Result:Achieved a tumor growth inhibition (TGI) value of 51.9% at 200 mg/kg.
Yielded unspecified tumor inhibition at 100 mg/kg.
Achieved a tumor growth inhibition rate of 44.1% at 150 mg/kg.
Caused no overt toxicity or weight loss at any tested dose.
Chemical Information
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Masse moléculaire 460.55
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Formule C25H24N4O3S
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SMILES
CNC1=CC=C(C(COC)=C1)C2=CC=CC(S(=O)(NC3=C4NC=C(C4=C(C=C3)C)C#N)=O)=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YSA64 Related Classifications
HY-183755 Related Classifications
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