2. PROTAC Cell Cycle/DNA Damage Apoptosis
  3. PROTACs CDK Caspase
  4. PROTAC CDK2/4/6 Degrader-2

PROTAC CDK2/4/6 Degrader-2 is a CDK2/4/6 PROTAC degrader. PROTAC CDK2/4/6 Degrader-2. PROTAC CDK2/4/6 Degrader-2 can be converted into the prodrug PROTAC CDK2/4/6 Degrader-1 (HY-171826) through a one-step reaction with chloromethyl pivalate. PROTAC CDK2/4/6 Degrader-2 degrades CDK2/4/6 and their complex in malignant melanomas cells. PROTAC CDK2/4/6 Degrader-2 induces cell cycle arrest and cell apoptosis in various cancer cells, in particular for melanomas. PROTAC CDK2/4/6 Degrader-2 can be used for malignant melanomas research.
(Pink: CDK2 and CDK4 and CDK6 ligand (HY-168440); Blue: Cereblon ligand (HY-10984); Black: linker).

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

PROTAC CDK2/4/6 Degrader-2

PROTAC CDK2/4/6 Degrader-2 Chemical Structure

CAS No. : 2541626-49-5

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Based on 1 publication(s) in Google Scholar

PROTAC CDK2/4/6 Degrader-2 Related Antibodies

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Description

PROTAC CDK2/4/6 Degrader-2 is a CDK2/4/6 PROTAC degrader. PROTAC CDK2/4/6 Degrader-2. PROTAC CDK2/4/6 Degrader-2 can be converted into the prodrug PROTAC CDK2/4/6 Degrader-1 (HY-171826) through a one-step reaction with chloromethyl pivalate. PROTAC CDK2/4/6 Degrader-2 degrades CDK2/4/6 and their complex in malignant melanomas cells. PROTAC CDK2/4/6 Degrader-2 induces cell cycle arrest and cell apoptosis in various cancer cells, in particular for melanomas. PROTAC CDK2/4/6 Degrader-2 can be used for malignant melanomas research[1]. (Pink: CDK2 and CDK4 and CDK6 ligand (HY-168440); Blue: Cereblon ligand (HY-10984); Black: linker).

IC50 & Target[1]

CDK2

 

CDK3

 

CDK6

 

Caspase 3

 

CDK4

 

In Vitro

PROTAC CDK2/4/6 Degrader-2 (compound 3) (72 h) exhibits prominent anti-proliferative activity against B16F10 and A375, with IC50s of 0.09861 and 0.1659 μM, respectively[1].
PROTAC CDK2/4/6 Degrader-2 (0-2000 nM, 0-12 h) mediates CDK2/4/6 protein degradation and impairs downstream Rb signaling activation by hijacking the E3 ubiquitin ligase CRBN in B16F10 and A375 cells[1].
PROTAC CDK2/4/6 Degrader-2 (50-500 nM, 7 days) exerts significant anti-proliferative activity in B16F10 and A375 cells[1].
PROTAC CDK2/4/6 Degrader-2 (125-1000 nM,48 h) significantly induces apoptosis of A375 and B16F10 cells in a dose-dependent manner in B16F10 and A375 cells[1].
PROTAC CDK2/4/6 Degrader-2 (0-2000 nM, 48 h) induces caspase-dependent apoptosis via the common P53/Bcl-2/Bax apoptotic pathway in B16F10 and A375 cells[1].
PROTAC CDK2/4/6 Degrader-2 (25-1000 nM ,48 h) induces cell cycle arrest via the degradation of cell cycle-related proteins CDK2/4/6 in A375 and B16F10 cells[1].

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

PROTAC CDK2/4/6 Degrader-2 Related Antibodies

Western Blot Analysis[1]

Cell Line: B16F10 and A375 cells
Concentration: 0, 62.5, 100, 125, 250, 500, 1000 and 2000 nM
Incubation Time: 0, 3, 6, 9 and 12 h
Result: Induced significant intracellular cleavage of all CDK 2, CDK 4 and CDK 6 proteins in both concentration-dependent and time dependent manners.
Mitigated downstream p-Rb signaling pathway activation of melanoma cells.
Induced CDK2/4/6 protein degradation via the proteasomal pathway at 100 nM and 6 h.

Cell Proliferation Assay[1]

Cell Line: B16F10 and A375
Concentration: 50, 100, 250, 500 nM
Incubation Time: 7 days
Result: Exerted a remarkable inhibiting effect on colony formation in A375 and B16F10 in low nano molar concentration.

Apoptosis Analysis[1]

Cell Line: B16F10 and A375 cells
Concentration: 125, 250, 500, 1000 nM
Incubation Time: 48 h
Result: Significantly induced apoptosis.

Western Blot Analysis[1]

Cell Line: B16F10 and A375 cells
Concentration: 0, 62.5, 125, 250, 500, 1000 and 2000 nM
Incubation Time: 48 h
Result: Upregulated casepase-3 and cleaved PARP protein expression.
Also significantly induced up-regulation of the pro-protein level of P-53 and Bax.
Downregulated the anti-apoptotic protein level of Bcl-2.

Cell Cycle Analysis[1]

Cell Line: B16F10 and A375 cells
Concentration: 0, 25, 50, 100, 250, 500, 1000 nM
Incubation Time: 48 h
Result: Increased accumulation of A375 cell population in G0/G1 phase, but G2/M phase for B16F10 cell.
Parmacokinetics
Species Dose Route Cmax Tmax AUC0-24
Rat[1] 10 mg/kg i.v. 59851 ng/mL 0.75 h 1607045 ng/mL
Rat[1] 200 mg/kg p.o. 692268 ng/mL 0.25 h 822803.9967 ng/mL
Molecular Weight

747.84

Formula

C40H45N9O6
CAS No.
SMILES

O=C(C1=CC=C(NC2=NC3=C(C=C(N3C4CCCC4)C(N(C)C)=O)C=N2)C=C1)NCCCCCCNC5=CC=CC(C(N6C7C(NC(CC7)=O)=O)=O)=C5C6=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC CDK2/4/6 Degrader-2 Related Classifications

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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.

Keywords:

PROTAC CDK2/4/6 Degrader-22541626-49-5PROTACsCDKCaspaseCyclin dependent kinaseCDK2/4/6PROTACdegraderprodrugmalignant melanomasapoptosisInhibitorinhibitorinhibit

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