1. Cell Cycle/DNA Damage PROTAC
  2. CDK PROTACs DNA/RNA Synthesis
  3. YJ9069

YJ9069 is a selective CDK12/CDK13 PROTAC degrader with an IC50 of 22.22 nM for in VCaP cells. CDK12/13 degradation rapidly triggers gene-length-dependent transcriptional elongation defects, leading to DNA damage and cell-cycle arrest. YJ9069 effectively inhibits proliferation in subsets of prostate cancer cells and significantly suppresses prostate tumor growth. (Pink: CDK12/CDK13 degradation agent (HY-168658); Black: Linker (HY-W015967); Blue: ligand for E3 ligase (HY-103596)).

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

YJ9069 Chemical Structure

YJ9069 Chemical Structure

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Based on 1 publication(s) in Google Scholar

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Description

YJ9069 is a selective CDK12/CDK13 PROTAC degrader with an IC50 of 22.22 nM for in VCaP cells. CDK12/13 degradation rapidly triggers gene-length-dependent transcriptional elongation defects, leading to DNA damage and cell-cycle arrest. YJ9069 effectively inhibits proliferation in subsets of prostate cancer cells and significantly suppresses prostate tumor growth. (Pink: CDK12/CDK13 degradation agent (HY-168658); Black: Linker (HY-W015967); Blue: ligand for E3 ligase (HY-103596))[1].

IC50 & Target[1]

CDK12

 

CDK13

 

Molecular Weight

850.92

Formula

C46H46N10O7

Appearance

Solid

Color

White to off-white

SMILES

O=C(NCC1=CC=CC=C1)N(C2=CN=C(N3CCN(C(COC4=C5C(C(N(C6CCC(NC6=O)=O)C5=O)=O)=CC=C4)=O)CC3)C=C2)[C@H](CC7)CC[C@@H]7NC8=NC=C9C(C=CC=C9)=N8

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (58.76 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1752 mL 5.8760 mL 11.7520 mL
5 mM 0.2350 mL 1.1752 mL 2.3504 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
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 Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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 (sealed storage, away from moisture and light). 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 1.1752 mL 5.8760 mL 11.7520 mL 29.3800 mL
5 mM 0.2350 mL 1.1752 mL 2.3504 mL 5.8760 mL
10 mM 0.1175 mL 0.5876 mL 1.1752 mL 2.9380 mL
15 mM 0.0783 mL 0.3917 mL 0.7835 mL 1.9587 mL
20 mM 0.0588 mL 0.2938 mL 0.5876 mL 1.4690 mL
25 mM 0.0470 mL 0.2350 mL 0.4701 mL 1.1752 mL
30 mM 0.0392 mL 0.1959 mL 0.3917 mL 0.9793 mL
40 mM 0.0294 mL 0.1469 mL 0.2938 mL 0.7345 mL
50 mM 0.0235 mL 0.1175 mL 0.2350 mL 0.5876 mL
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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.

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Product Name:
YJ9069
Cat. No.:
HY-168556
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