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.
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- 화학식: C25H24N4O3S
- 분자량:460.55
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보관:
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
- 순도&문서
- References
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Help & FAQs
Biological Activity
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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분자량 460.55
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YSA64 Related Classifications
HY-183755 Related Classifications
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