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

BSJ-4-116 

Cat. No.: HY-139039 Purity: 99.62%
Handling Instructions

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).

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

BSJ-4-116 Chemical Structure

BSJ-4-116 Chemical Structure

CAS No. : 2519823-34-6

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 230 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 230 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 250 In-stock
Estimated Time of Arrival: December 31
25 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 950 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1550 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

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].

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

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.
SMILES

O=C1C2=C(OCC(NCCCCCCCN3C[[email protected]@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)

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
10 mM 0.1194 mL 0.5971 mL 1.1942 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

BSJ-4-116PROTACCDKProteolysis-targeting chimeraCyclin dependent kinaseantiproliferativeKellyCDK12C1039FmutationcancerdegraderInhibitorinhibitorinhibit

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Product Name:
BSJ-4-116
Cat. No.:
HY-139039
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