2. PROTAC Cell Cycle/DNA Damage
  3. PROTACs CDK
  4. BSJ-4-116

BSJ-4-116 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. BSJ-4-116 downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation). BSJ-4-116 exhibits potent antiproliferative effects, alone and in combination with the poly(ADP-ribose) polymerase inhibitor Olaparib (HY-10162).

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BSJ-4-116 Chemical Structure

BSJ-4-116 Chemical Structure

CAS No. : 2519823-34-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 212 In-stock
Solution
10 mM * 1 mL in DMSO USD 212 In-stock
Solid
1 mg USD 63 In-stock
5 mg USD 140 In-stock
10 mg USD 230 In-stock
25 mg USD 490 In-stock
50 mg USD 770 In-stock
100 mg USD 1150 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

BSJ-4-116 Related Antibodies

Top Publications Citing Use of Products

Customer Validation

These results were obtained using AlphaLISA™ SureFire® Ultra™ assays

View All PROTACs Isoform Specific Products:

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

View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

BSJ-4-116 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. BSJ-4-116 downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation). BSJ-4-116 exhibits potent antiproliferative effects, alone and in combination with the poly(ADP-ribose) polymerase inhibitor Olaparib (HY-10162)[1].

IC50 & Target[1]

CDK12

6 nM (IC50)

Cereblon

 

In Vitro

BSJ-4-116 (10-10000 nM; 72 hours) exhibits potent antiproliferative effects in Kelly CDK12C1039F[1].
BSJ-4-116 (50?nM; 6-24?hours) decreases the level of CDK12 protein, regardless of the mutational status of the cell line[1].
BSJ-4-116 inhibits the growth of T-ALL cells (Jurkat and MOLT-4 cells) and sensitizes them to PARP inhibition[1].
BSJ-4-116 regulates DDR genes via poly(adenylation). BSJ-4-116 overcomes CDK12C1039F mutation. BSJ-4-116 represents the first example of resistance to a bivalent degrader molecule that is a consequence of an acquired point mutation in the target protein[1].

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

BSJ-4-116 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Parental Kelly and CDK12C1039F cells
Concentration: 10-10000 nM
Incubation Time: 72 hours
Result: Antiproliferative activity of BSJ-4-116 is independent of the mutational status, and the degrader compounds exhibited improved GR50 (growth rate inhibition) values in Kelly CDK12C1039F cells compared with the parental cell line.

Western Blot Analysis[1]

Cell Line: Parental and CDK12C1039F (KellyCDK12CF)-expressing Kelly cells
Concentration: 50 nM
Incubation Time: 6-24 hours
Result: Led to the same level of CDK12 protein level decrease, regardless of the mutational status of the cell line.
Molecular Weight

837.38

Formula

C40H49ClN8O8S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=C(OCC(NCCCCCCCN3C[C@@H](CCC3)NC4=NC=C(Cl)C(NC5=C(C=CC=C5)S(C(C)C)(=O)=O)=N4)=O)C=CC=C2C(N1C6C(NC(CC6)=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (298.55 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 1.1942 mL 5.9710 mL 11.9420 mL
5 mM 0.2388 mL 1.1942 mL 2.3884 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. 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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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (2.48 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.08 mg/mL (2.48 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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).
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. 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 1.1942 mL 5.9710 mL 11.9420 mL 29.8550 mL
5 mM 0.2388 mL 1.1942 mL 2.3884 mL 5.9710 mL
10 mM 0.1194 mL 0.5971 mL 1.1942 mL 2.9855 mL
15 mM 0.0796 mL 0.3981 mL 0.7961 mL 1.9903 mL
20 mM 0.0597 mL 0.2986 mL 0.5971 mL 1.4928 mL
25 mM 0.0478 mL 0.2388 mL 0.4777 mL 1.1942 mL
30 mM 0.0398 mL 0.1990 mL 0.3981 mL 0.9952 mL
40 mM 0.0299 mL 0.1493 mL 0.2986 mL 0.7464 mL
50 mM 0.0239 mL 0.1194 mL 0.2388 mL 0.5971 mL
60 mM 0.0199 mL 0.0995 mL 0.1990 mL 0.4976 mL
80 mM 0.0149 mL 0.0746 mL 0.1493 mL 0.3732 mL
100 mM 0.0119 mL 0.0597 mL 0.1194 mL 0.2986 mL
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BSJ-4-116 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-4-1162519823-34-6PROTACsCDKCyclin dependent kinaseantiproliferativeKellyCDK12C1039FmutationcancerdegraderInhibitorinhibitorinhibit

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