Art. -Nr.: HY-139039

BSJ-4-116

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

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).
(Pink: CDK12 ligand (HY-150948); Blue: Cereblon ligand (HY-41547); Black: linker).

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Reinheit: 99.87%
CAS. Nr.: 2519823-34-6
Formel: C₄₀H₄₉ClN₈O₈S
Molecular Weight:837.38

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

BSJ-4-116 Chemical Structure

CAS. Nr.: 2519823-34-6

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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]. (Pink: CDK12 ligand (HY-150948); Blue: Cereblon ligand (HY-41547); Black: linker).

IC₅₀ & Target^[1]

CDK12

6 nM (IC₅₀)

Cereblon

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle CDK Isoform-spezifische Produkte anzeigen :

In Vitro

BSJ-4-116 (10-10000 nM; 72 hours) exhibits potent antiproliferative effects in Kelly CDK12^C1039F^[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 CDK12^C1039F 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.

Cell Proliferation Assay^[1]

Cell Line:

Parental Kelly and CDK12^C1039F 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 CDK12^C1039F cells compared with the parental cell line.

Western Blot Analysis^[1]

Cell Line:

Parental and CDK12^C1039F (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.

Chemical Information

CAS. Nr. 2519823-34-6
Appearance Solid
Molecular Weight 837.38
Formel C₄₀H₄₉ClN₈O₈S
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (4)

All Bio/Physico-chemical AssayRT-PCRCell Proliferation/Viability AssayIF

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Journal Impact Factor

Nat Commun

Transcriptional and epigenetic rewiring by the NUP98::KDM5A fusion oncoprotein directly activates CDK12. [Abstract]

2025 May 19;16(1):4656. PMID: 40389480

BSJ-4-116 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 19;16(1):4656. [Abstract]

RNA-seq data of dTAG-NUP98::KDM5A cells treated with BSJ-4-116 (100 nM, 4h) compared to DMSO showing log2(FC) values of selected DNA damage repair genes.

BSJ-4-116 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 19;16(1):4656. [Abstract]

Viability assay of primary human NUP98-rearranged AML cells, healthy donor BM MNC and CD34+ progenitors treated with indicated concentrations of BSJ-4-116 (0.1 nM-10 μM) for 3 days.

BSJ-4-116 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 19;16(1):4656. [Abstract]

Representative images of γH2A.X immunofluorescence staining of dTAG-GFPNUP98::KDM5A cells treated with BSJ-4-116 (100 nM, 4h).
J Cell Mol Med

Inactivation of CDK12 Enhances Mitochondrial Efficiency to Suppress DNA Damage. [Abstract]

2026 Apr;30(7):e71101. PMID: 41896195
bioRxiv

2025 Nov 20.
bioRxiv

A functional map of CDK-drug interactions at single amino acid resolution. [Abstract]

2025 Nov 3:2025.11.02.685764. PMID: 41279360

BSJ-4-116 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Nov 3:2025.11.02.685764. [Abstract]

Scatterplot of median gRNA enrichment (log2 fold-change) in the presence of BSJ-4-116 relative to DMSO-treated control. Each dot represents a gRNA, filtered to exclude gRNAs below 10% sensor editing and with a base mean count ≤ 100. Hits labelled with FDR < 0.1 & LFC ≥ 2. ABE screen results shown in purple; CBE in blue. Regions shaded blue indicate ATP binding site residues.

BSJ-4-116 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Nov 3:2025.11.02.685764. [Abstract]

Visualization of the top resistance variants in BSJ-4–116- and HQ461-treated cell pools. Maximum likelihood estimate of sensor editing rate shown as amino acid logo plot.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (119.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

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)}

In Vivo:

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

Stock Solution Working Solution

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.

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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Jiang B, et al. Discovery and resistance mechanism of a selective CDK12 degrader. Nat Chem Biol. 2021;17(6):675-683. [Content Brief]

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.

Complete Stock Solution Preparation Table

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

Keywords

BSJ-4-116

4 Cited Publications

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BSJ-4-116

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

PROTAC Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Publications Citing Use of MedChemExpress (MCE) BSJ-4-116

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BSJ-4-116

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

PROTAC Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Publications Citing Use of MedChemExpress (MCE) BSJ-4-116

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BSJ-4-116 Related Classifications

HY-139039 Related Classifications