1. PROTAC
    Cell Cycle/DNA Damage
  2. PROTAC
    CDK
  3. PROTAC CDK2/9 Degrader-1

PROTAC CDK2/9 Degrader-1 

Cat. No.: HY-130709
Handling Instructions

PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with CRBN ligand.

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

PROTAC CDK2/9 Degrader-1 Chemical Structure

PROTAC CDK2/9 Degrader-1 Chemical Structure

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Description

PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with CRBN ligand[1].

IC50 & Target

CDK2

62 nM (DC50)

CDK9

33 nM (DC50)

Cereblon

 

In Vitro

PROTAC CDK2/9 Degrader-1 (0.25-3 μM; 48 hours) induces cell cycle blockage at the G2/M phase[1].
PROTAC CDK2/9 Degrader-1 (500 nM; 2-24 hours) down-regulates the Mcl-1 protein level in PC-3 cells[1].
PROTAC CDK2/9 Degrader-1 effectively degrades CDK2/9 in cell lines MCF-7, HCT-116 and 22Rv1, which all have high CDK2/9 expression[1].
PROTAC CDK2/9 Degrader-1 inhibits both CDK2 and CDK9, with IC50 as 7.42 nM and 14.50 nM, respectively[1].

Cell Cycle Analysis[1]

Cell Line: PC-3 cells
Concentration: 500 nM
Incubation Time: 2, 4, 8, 16, 24 hours
Result: Down-regulated the Mcl-1 protein level in PC-3 cells.

Western Blot Analysis[1]

Cell Line: PC-3 cells
Concentration: 0.25, 1, 3 μM
Incubation Time: 48 hours
Result: Induced cell cycle blockage at the G2/M phase.
Molecular Weight

815.84

Formula

C₄₀H₄₁N₁₃O₇

SMILES

O=C(C1=NNC=C1NC2=C3C(NC=C3)=NC=N2)NC4=CC=C(CN5CCN(C(CCC(NCCNC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)=O)=O)CC5)C=C4

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

PROTAC CDK2/9 Degrader-1PROTACCDKProteolysis-targeting chimeraCyclin dependent kinasecellcycleprostatecancertumorPC-3Mcl-1c-MycarrestInhibitorinhibitorinhibit

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Product name:
PROTAC CDK2/9 Degrader-1
Cat. No.:
HY-130709
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