1. Protein Tyrosine Kinase/RTK
  2. Btk
  3. JS25

JS25 is a selective and covalent inhibitor of BTK that inactivates BTK with an IC50 value of 5.8 nM by chelating Tyr551. JS25 inhibits cancer cells proliferation, pronounces cell death, and promotes murine xenograft model of Burkitt’s lymphoma. JS25 effectively crosses the blood-brain barrier.

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JS25 Chemical Structure

JS25 Chemical Structure

CAS No. : 2411771-95-2

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5 mg USD 515 In-stock
10 mg USD 870 In-stock
25 mg USD 1740 In-stock
50 mg USD 2950 In-stock
100 mg USD 5000 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

JS25 is a selective and covalent inhibitor of BTK that inactivates BTK with an IC50 value of 5.8 nM by chelating Tyr551. JS25 inhibits cancer cells proliferation, pronounces cell death, and promotes murine xenograft model of Burkitt’s lymphoma. JS25 effectively crosses the blood-brain barrier[1].

IC50 & Target

IC50: 5.8 nM (BTK), 49.0 nM (BMX), 440 nM (ITK), 190 nM (TXK), 220 nM (TEC), 2.60 μM (BLK)[1]

In Vitro

JS25 (0-50 μM; 72 h) inhibits the proliferation of myeloid and lymphoid B-cell cancer cell lines. JS25 shows inhibitory capability against BTK, BMX, ITK, TXK, TEC, and BLK with IC50s of 28.5 nM, 49.0 nM, 0.44 μM, 0.19 μM, 0.22 μM, and 2.60 μM, respectively; shows little inhibition against other BTK pathway-related proteins (EGFR, ERBB2, and JAK3), with IC50>3 μM. JS25 presents a more favorable selectivity profile than Ibrutinib (HY-10997) and Acalabrutinib (HY-17600)[1].
JS25 (10 μM; 0, 4, 15 h) degrades BTK and inhibits both the catalytic activity and the expression of BTK in tumor cells[1].
JS25 (10 μM; 72 h) inhibits the tumor growth of Burkitt’s lymphoma and induces selective ex vivo cytotoxicity in primary diffuse large B-cell lymphoma (DLBCL) samples[1].

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

In Vivo

JS25 (10 mg/kg and 20 mg/kg; i.p.; every 2 days, for 14 d) inhibits tumor growth and results a significant reduction in their secondary tumor formation in murine xenograft model of Burkitt’s lymphoma[1].
JS25 (1, 2.5, and 5 μM; injection; every day for 2 days) decreases tumor burden in zebrafish patient-derived xenografts of chronic lymphocytic leukemia, wich efficacy is better than Ibrutinib (HY-10997)[1].

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

Animal Model: Female adult BALB/c/NSG mice with Raji cells (s.c.)[1]
Dosage: 10 mg/kg and 20 mg/kg
Administration: Intraperitoneal injection; every 2 days for 14 days
Result: Caused a 30-40% reduction of the subcutaneous tumor and an overall reduction in the percentage of metastasis and secondary tumor formation.
Molecular Weight

524.59

Formula

C29H24N4O4S

CAS No.
Appearance

Solid

Color

Light yellow to light brown

SMILES

C=CC(NC1=CC(C)=CC(N2C(C=CC3=C2C4=C(N=C3)C=C(C=C4)C5=CC=C(C=C5)NS(C)(=O)=O)=O)=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (38.13 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9063 mL 9.5313 mL 19.0625 mL
5 mM 0.3813 mL 1.9063 mL 3.8125 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9063 mL 9.5313 mL 19.0625 mL 47.6563 mL
5 mM 0.3813 mL 1.9063 mL 3.8125 mL 9.5313 mL
10 mM 0.1906 mL 0.9531 mL 1.9063 mL 4.7656 mL
15 mM 0.1271 mL 0.6354 mL 1.2708 mL 3.1771 mL
20 mM 0.0953 mL 0.4766 mL 0.9531 mL 2.3828 mL
25 mM 0.0763 mL 0.3813 mL 0.7625 mL 1.9063 mL
30 mM 0.0635 mL 0.3177 mL 0.6354 mL 1.5885 mL
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JS25 Related Classifications

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.

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Product Name:
JS25
Cat. No.:
HY-151808
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