2. PROTAC Cell Cycle/DNA Damage
  3. PROTACs CDK
  4. PP-C8

PP-C8 is a potent and selective PROTAC CDK12-Cyclin K degrader. PP-C8 induces CDK12-Cyclin K degradation with DC50s of 416 and 412 nM for CDK12 and Cyclin K, respectively. PP-C8 demonstrates profound synergistic antiproliferative effects with PARP inhibitor in triple-negative breast cancer (TNBC).

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PP-C8 Chemical Structure

PP-C8 Chemical Structure

CAS No. : 3032108-74-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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5 mg USD 1450 In-stock
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Based on 1 publication(s) in Google Scholar

PP-C8 Related Antibodies

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Description

PP-C8 is a potent and selective PROTAC CDK12-Cyclin K degrader. PP-C8 induces CDK12-Cyclin K degradation with DC50s of 416 and 412 nM for CDK12 and Cyclin K, respectively. PP-C8 demonstrates profound synergistic antiproliferative effects with PARP inhibitor in triple-negative breast cancer (TNBC)[1].

In Vitro

PP-C8 (0-30 μM; 24 hours; Bel-7402 and MDA-MB-231 cells) is a potent and highly selective CDK12-Cyclin K complex degrade[1].
PP-C8 (0-3 μM; 24 hours; Bel-7402 and MDA-MB-231 cells) mediated CDK12-CycK complex degradation is cereblon and UPS dependent PROTAC-MOA[1].
PP-C8 (0-3 μM; Bel-7402 and MDA-MB-231 cell lines) induces CDK12-Cyclin K degradation demonstrates superior synergistic antiproliferative activity with the PARP inhibition[1].

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

PP-C8 Related Antibodies

Western Blot Analysis[1]

Cell Line: Bel-7402 and MDA-MB-231 cells
Concentration: 0, 0.1, 0.3 ,1.0, 3.0, 10.0 and 30.0 μM
Incubation Time: 24 hours
Result: Downregulated of both CDK12 and CycK protein levels in a dose-dependent manner with DC50 of 416 nM and 412 nM.

Western Blot Analysis[1]

Cell Line: Bel-7402 and MDA-MB-231 cells
Concentration: 1 and 3 μM
Incubation Time: 24 hours
Result: Nondegraded CDK12-CycK in neither CRBN nor neither UPS depleted cell lines.
Molecular Weight

866.94

Formula

C43H51FN12O7
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

CC(N1C=NC2=C1N=C(N=C2NCC3=NC4=CC(F)=C(C=C4N3)NCCCCCCCCNC(COC5=C6C(N(C(C6=CC=C5)=O)C7CCC(NC7=O)=O)=O)=O)N8CCOCC8)C
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 : 100 mg/mL (115.35 mM; ultrasonic and warming and heat to 60°C; 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 1.1535 mL 5.7674 mL 11.5348 mL
5 mM 0.2307 mL 1.1535 mL 2.3070 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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. 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 1.1535 mL 5.7674 mL 11.5348 mL 28.8371 mL
5 mM 0.2307 mL 1.1535 mL 2.3070 mL 5.7674 mL
10 mM 0.1153 mL 0.5767 mL 1.1535 mL 2.8837 mL
15 mM 0.0769 mL 0.3845 mL 0.7690 mL 1.9225 mL
20 mM 0.0577 mL 0.2884 mL 0.5767 mL 1.4419 mL
25 mM 0.0461 mL 0.2307 mL 0.4614 mL 1.1535 mL
30 mM 0.0384 mL 0.1922 mL 0.3845 mL 0.9612 mL
40 mM 0.0288 mL 0.1442 mL 0.2884 mL 0.7209 mL
50 mM 0.0231 mL 0.1153 mL 0.2307 mL 0.5767 mL
60 mM 0.0192 mL 0.0961 mL 0.1922 mL 0.4806 mL
80 mM 0.0144 mL 0.0721 mL 0.1442 mL 0.3605 mL
100 mM 0.0115 mL 0.0577 mL 0.1153 mL 0.2884 mL
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PP-C8 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:

PP-C83032108-74-7PROTACsCDKCyclin dependent kinaseCDK12Cyclin KPROTACSynthetic lethalityTriple-negative breast cancerInhibitorinhibitorinhibit

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