2. PROTAC Protein Tyrosine Kinase/RTK NF-κB
  3. PROTACs Itk NF-κB
  4. BSJ-05-037

BSJ-05-037 is an ITK PROTAC degrader that effectively targets and degrades ITK in T-cell lymphoma cell lines. BSJ-05-037 blocks the activation of the NF-κB/GATA-3 signaling pathway, inhibits PLCγ1 phosphorylation, and reduces the proliferative capacity of T-cell lymphoma cells. BSJ-05-037 enhances the sensitivity of T-cell lymphoma cells to chemotherapy. In mouse models of T-cell lymphoma, BSJ-05-037 induces ITK degradation, reduces GATA-3 expression, decreases tumor volume, and reverses chemotherapy resistance. BSJ-05-037 is applicable to research related to T-cell lymphoma.
(Pink: Itk ligand (HY-11092); Blue: Cereblon ligand (HY-103597); Black: linker (HY-W036393)).

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

BSJ-05-037

BSJ-05-037 Chemical Structure

CAS No. : 2756388-01-7

Size Price Stock Quantity
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

BSJ-05-037 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All NF-κB Isoform Specific Products:

View All Isoforms
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

BSJ-05-037 is an ITK PROTAC degrader that effectively targets and degrades ITK in T-cell lymphoma cell lines. BSJ-05-037 blocks the activation of the NF-κB/GATA-3 signaling pathway, inhibits PLCγ1 phosphorylation, and reduces the proliferative capacity of T-cell lymphoma cells. BSJ-05-037 enhances the sensitivity of T-cell lymphoma cells to chemotherapy. In mouse models of T-cell lymphoma, BSJ-05-037 induces ITK degradation, reduces GATA-3 expression, decreases tumor volume, and reverses chemotherapy resistance. BSJ-05-037 is applicable to research related to T-cell lymphoma[1][2][3]. (Pink: Itk ligand (HY-11092); Blue: Cereblon ligand (HY-103597); Black: linker (HY-W036393)).

IC50 & Target

Cereblon

 

In Vitro

BSJ-05-037 (0.001-10 μM; 2-16 h) potently induces time- and concentration-dependent degradation of ITK in DERL-2 and Hut78 cells, and this degradation is CRBN-dependent[1].
BSJ-05-037 (1 μM; 10 days) potently inhibits the proliferation of DERL-2 and Jurkat T-cell lymphoma cells[1].
BSJ-05-037 (0.025-0.5 μM; 8 h) dose-dependently inhibits the phosphorylation of PLCγ1 in DERL-2 cells[1].
BSJ-05-037 (1 μM; 24 h-3 days) blocks TCR-induced upregulation of GATA-3 and restores the sensitivity of T8ML-1 cells to Vincristine (HY-N0488A), thereby overcoming drug resistance mediated by the ITK/NF-κB/GATA-3 axis[1].
BSJ-05-037 (1 μM; 24 h-4 days) induces nearly complete ITK degradation and reduces GATA-3 levels by over 90% in Hut78 and H9 cutaneous T-cell lymphoma cells, while also enhancing the sensitivity of these cells to Vincristine during the 4-day treatment[1].

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

BSJ-05-037 Related Antibodies

Western Blot Analysis[1]

Cell Line: DERL-2、Hut78 cells
Concentration: 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 2, 4, 8, 16 h
Result: Induced potent degradation of ITK protein in a dose-dependent manner after a 16 h treatment (IC50 = 17.6~ 41.8 nM).

Cell Viability Assay[1]

Cell Line: T-cell lymphoma cell lines (DERL-2, Jurkat)
Concentration: 1 μM
Incubation Time: 10 days
Result: Reduced DERL-2 cell viability to <10% of DMSO control after 10 days.
Induced growth inhibition in Jurkat cells.

Western Blot Analysis[1]

Cell Line: DERL-2 cells
Concentration: 0.025, 0.1, 0.25, 0.5 μM
Incubation Time: 8 h
Result: Resulted in dose-dependent inhibition of PLCγ1 phosphorylation.

Western Blot Analysis[1]

Cell Line: T8ML1 cells
Concentration: 1 μM
Incubation Time: 24 h
Result: Induced potent ITK degradation and abrogated TCR-dependent upregulation of GATA-3.
Parmacokinetics
Species Dose Route T1/2 Cmax
Mice[1] 10 mg/kg i.p. 1.9 h 3.4 μM
In Vivo

BSJ-05-037 (50 mg/kg; i.p.; every 8 hours; 3 total doses/once every other day; 14 days) induces ITK degradation, reduces GATA-3 expression, inhibits PLCγ1, decreases tumor volume, and reverses chemoresistance in Hut78/H9 cutaneous T-cell lymphoma xenografts in mice[1].

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

Animal Model: NOD.Cg-PrkdcscidIl2rgtm1Wjl/SzJ (NSG) mice (9-10 weeks old)[1]
Dosage: 50 mg/kg
Administration: i.p.; every 8 hours; 3 total doses/ once every other day; 14 days
Result: Induced 99.2% degradation of ITK in xenografted tumors.
Reduced GATA-3 protein levels by >90% in treated tumors.
Reduced mean tumor volume to ~1100 mm3 by day 14 as monotherapy.
Achieved almost complete tumor stasis, with mean tumor volume reduced to ~150 mm3 by day 14 when combined with vincristine.
Enriched NF-κB pathway gene.
Downregulated GATA3, IL2, CD69, and the NF-κB regulators NFKBIA.
Resulted in an enrichment of signatures for other TCR pathways including inflammatory response,
STAT3 and STAT5 signaling, MYC targets and cell cycle regulation.
Molecular Weight

1022.20

Formula

C51H59N9O10S2
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(NC1=NC=C(SC2=CC(C(N3CCN(C(C)=O)CC3)=O)=C(OC)C=C2C)S1)C4=CC=C(N5CCN(CCCCCCCNC(COC6=C7C(C(N(C8CCC(NC8=O)=O)C7=O)=O)=CC=C6)=O)CC5)C=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (97.83 mM; Need ultrasonic; 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 0.9783 mL 4.8914 mL 9.7828 mL
5 mM 0.1957 mL 0.9783 mL 1.9566 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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (2.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 and light). 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 0.9783 mL 4.8914 mL 9.7828 mL 24.4571 mL
5 mM 0.1957 mL 0.9783 mL 1.9566 mL 4.8914 mL
10 mM 0.0978 mL 0.4891 mL 0.9783 mL 2.4457 mL
15 mM 0.0652 mL 0.3261 mL 0.6522 mL 1.6305 mL
20 mM 0.0489 mL 0.2446 mL 0.4891 mL 1.2229 mL
25 mM 0.0391 mL 0.1957 mL 0.3913 mL 0.9783 mL
30 mM 0.0326 mL 0.1630 mL 0.3261 mL 0.8152 mL
40 mM 0.0245 mL 0.1223 mL 0.2446 mL 0.6114 mL
50 mM 0.0196 mL 0.0978 mL 0.1957 mL 0.4891 mL
60 mM 0.0163 mL 0.0815 mL 0.1630 mL 0.4076 mL
80 mM 0.0122 mL 0.0611 mL 0.1223 mL 0.3057 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

BSJ-05-037 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.

Keywords:

BSJ-05-0372756388-01-7PROTACsItkNF-κBInterleukin-2 inducible T-cell kinaseIL2 inducible T-cell kinaseNuclear factor-κBNuclear factor-kappaBITK PROTACs degraderT-cell lymphomaDERL-2 cellsHut78 cellsT8ML1 cellsNSG mice
Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
BSJ-05-037
Cat. No.:
HY-185206
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (252 KB) Français - FR (252 KB) Deutsch - DE (252 KB) Norwegian - NO (252 KB) Español - ES (252 KB) Swedish - SV (252 KB) Italian - IT (252 KB) Korean - KR (252 KB) Portuguese - PT (252 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.