Art. -Nr.: HY-162706

BSJ-5-63

Name: BSJ-5-63
Brand: MedChemExpress
SKU: HY-162706
Price: 195.00 USD
Availability: InStock
Rating: 5 (1 reviews)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

BSJ-5-63 is a potent CDK12, CDK7, CDK9 PROTAC degrader. BSJ-5-63 BSJ-5-63 decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, Cyclin K. BSJ-5-63 decreases the mRNA expression of BRCA1, BRCA2. BSJ-5-63 shows anticancer activity and has the potential for the research of prostate cancer.
(Pink: CDK12 and CDK7 and CDK9 ligand (HY-150948); Blue: VHL ligand (HY-112078); Black: linker (HY-W140827)).

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Reinheit: 99.97%
CAS. Nr.: 2519823-37-9
Formel: C₅₂H₇₄ClN₉O₆S₂
Molecular Weight:1020.78

Speicherung:

Store at room temperature 3 years.

In solvent -80°C, 2 years , -20°C, 1 year

BSJ-5-63 Chemical Structure

CAS. Nr.: 2519823-37-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

BSJ-5-63 is a potent CDK12, CDK7, CDK9 PROTAC degrader. BSJ-5-63 BSJ-5-63 decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, Cyclin K. BSJ-5-63 decreases the mRNA expression of BRCA1, BRCA2. BSJ-5-63 shows anticancer activity and has the potential for the research of prostate cancer^[1]. (Pink: CDK12 and CDK7 and CDK9 ligand (HY-150948); Blue: VHL ligand (HY-112078); Black: linker (HY-W140827)).

IC₅₀ & Target^[1]

CDK12

CDK7

CDK9

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle CDK Isoform-spezifische Produkte anzeigen :

In Vitro

BSJ-5-63 (0-1000 nM; 8 h) decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, Cyclin K in a dose-dependent manner^[1].
BSJ-5-63 (0-1000 nM; 8, 16, 24 h) decreases the mRNA expression of BRCA1, BRCA2 in a dose and time dependent manner^[1].

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

Western Blot Analysis^[1]

Cell Line:

LNCaP, C4-2B, 22Rv1 cells
Concentration:

62.5, 125, 250, 500, 1000 nM
Incubation Time:

8 h
Result:

Decreased the protein expression of CDK12, CDK7, CDK9, P-RNAPII Ser2, P-RNAPII Ser5, P-RNAPII Ser7, RNAPII, Cyclin K in a dose-dependent manner.

RT-PCR^[1]

Cell Line:

LNCaP, C4-2B, 22Rv1 cells
Concentration:

62.5, 125, 250, 500, 1000 nM
Incubation Time:

8, 16, 24 h
Result:

Decreased the mRNA expression of BRCA1, BRCA2 in a dose and time dependent manner.

In Vivo

BSJ-5-63 (50 mg/kg; i.p.; daily for 12 days) shows anticancer activity in mice^[1].

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

Animal Model:

4-5 weeks, Male ICR-SCID mice (22Rv1 cells)^[1]
Dosage:

50 mg/kg
Administration:

I.p.; daily for 12 days
Result:

Significantly inhibited the growth of 22Rv1 tumors and tumor weight was significantly reduced and increased in the number of apoptotic cells, daily administration resulted in approximately 10% weight loss in mice.

Chemical Information

CAS. Nr. 2519823-37-9
Appearance Solid
Molecular Weight 1020.78
Formel C₅₂H₇₄ClN₉O₆S₂
Color White to off-white
SMILES

O=S(C1=CC=CC=C1NC2=NC(N[C@H]3CN(CCCCCCCCCCC(N[C@@H](C(C)(C)C)C(N4C[C@H](O)C[C@H]4C(N[C@@H](C)C5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)CCC3)=NC=C2Cl)(C(C)C)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Store at room temperature 3 years

In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Journal Impact Factor

bioRxiv

Defective Microhomology-Mediated End-joining in SMARCB1-Deficient Tumors. [Abstract]

2025 Nov 21:2025.11.20.689563. PMID: 41332615

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (97.96 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

0.9796 mL

4.8982 mL

9.7964 mL

5 mM

0.1959 mL

0.9796 mL

1.9593 mL

10 mM

0.0980 mL

0.4898 mL

0.9796 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 90% Corn Oil

Solubility: ≥ 5 mg/mL (4.90 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 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 (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Gui F, et al. Acute BRCAness Induction and AR Signaling Blockage through CDK12/7/9 Degradation Enhances PARP Inhibitor Sensitivity in Prostate Cancer. bioRxiv [Preprint]. 2024 Jul 10:2024.07.09.602803. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	0.9796 mL	4.8982 mL	9.7964 mL	24.4911 mL
	5 mM	0.1959 mL	0.9796 mL	1.9593 mL	4.8982 mL
	10 mM	0.0980 mL	0.4898 mL	0.9796 mL	2.4491 mL
	15 mM	0.0653 mL	0.3265 mL	0.6531 mL	1.6327 mL
	20 mM	0.0490 mL	0.2449 mL	0.4898 mL	1.2246 mL
	25 mM	0.0392 mL	0.1959 mL	0.3919 mL	0.9796 mL
	30 mM	0.0327 mL	0.1633 mL	0.3265 mL	0.8164 mL
	40 mM	0.0245 mL	0.1225 mL	0.2449 mL	0.6123 mL
	50 mM	0.0196 mL	0.0980 mL	0.1959 mL	0.4898 mL
	60 mM	0.0163 mL	0.0816 mL	0.1633 mL	0.4082 mL
	80 mM	0.0122 mL	0.0612 mL	0.1225 mL	0.3061 mL

Bioz

Keywords

BSJ-5-63

1 Cited Publications

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BSJ-5-63

Publications Citing Use of MedChemExpress (MCE) BSJ-5-63

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BSJ-5-63 Related Classifications

HY-162706 Related Classifications

Bioz