2. PROTAC Cell Cycle/DNA Damage
  3. PROTACs CDK
  4. BSJ-5-63

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: ligand for target protein (HY-150948); black: linker (HY-W140827); Blue: E3 ligase ligand (HY-112078)).

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

BSJ-5-63

BSJ-5-63 Chemical Structure

CAS No. : 2519823-37-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
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Customer Review

Based on 1 publication(s) in Google Scholar

BSJ-5-63 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE BSJ-5-63

View All PROTACs Isoform Specific Products:

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

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View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

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: ligand for target protein (HY-150948); black: linker (HY-W140827); Blue: E3 ligase ligand (HY-112078))[1].

IC50 & Target[1]

CDK12

 

CDK7

 

CDK9

 

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.

BSJ-5-63 Related Antibodies

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.
Molecular Weight

1020.78

Formula

C52H74ClN9O6S2
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Store at room temperature 3 years

In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9796 mL 4.8982 mL 9.7964 mL
5 mM 0.1959 mL 0.9796 mL 1.9593 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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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: ≥ 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

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).
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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
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BSJ-5-63 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-5-632519823-37-9PROTACsCDKCyclin dependent kinaseRNAPIICyclin Kanticancerprostate cancerLNCaPC4-2B22Rv1 cellsInhibitorinhibitorinhibit

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