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  4. 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.

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

YSA64

YSA64 Chemical Structure

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YSA64 Related Antibodies

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Description

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[1].

In Vitro

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.

YSA64 Related Antibodies

Western Blot Analysis[1]

Cell Line: HCT-116 colorectal cancer cells
Concentration: 0.05 μM; 0.2 μM; 0.8 μM
Incubation Time: 24 h
Result: Robustly reduced RBM39 protein levels at all tested concentrations.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUClast F CL Vss C0
Mice[1] 15 mg/kg p.o. 1.94 h 0.50 h 1193 ng/mL 2984 ng·h/mL 42.2 % / / /
Mice[1] 5 mg/kg i.v. 0.53 h / / 2355 ng·h/mL / 36 mL/min/kg 1.16 L/kg 5380 ng/mL
In Vivo

YSA64 (Compound 41) (100-200 mg/kg; p.o.; once daily; 10 days) exhibits significant in vivo antitumor efficacy in MV4-11 xenograft models, achieving up to 51.9% tumor growth inhibition, with a favorable safety profile and no observed weight loss[1].

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

Animal Model: SCID mice (male; 3-4 weeks old; subcutaneously implanted with MV4-11 cells to establish a xenograft model)[1]
Dosage: 100 mg/kg; 150 mg/kg; 200 mg/kg
Administration: p.o.; once daily; 10 days
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.
Molecular Weight

460.55

Formula

C25H24N4O3S
SMILES

CNC1=CC=C(C(COC)=C1)C2=CC=CC(S(=O)(NC3=C4NC=C(C4=C(C=C3)C)C#N)=O)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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YSA64 Related Classifications

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

YSA64YSA 64YSA-64Molecular GluesRBM39A673 Ewing sarcoma cellsacute myeloid leukemiaHCT-116 colorectal cancer cellsMV4-11 acute myeloid leukemia cellsDCAF15Cullin-RING E3 ligaseproteasomeDDB1Ewing sarcomaInhibitorinhibitorinhibit

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