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Art. -Nr.: HY-183755

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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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₂₅H₂₄N₄O₃S
Molecular Weight:460.55

Speicherung:

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

YSA64 Chemical Structure

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

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	T_1/2	T_max	C_max	AUC_last	F	CL	V_ss	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.

Chemical Information

Molecular Weight 460.55
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Lyu X, et al. Discovery and characterization of YSA64, a RBM39 degrader with in vivo efficacy and potent cellular activity in pediatric Ewing sarcoma A673. Eur J Med Chem. 2026;314:118921. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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