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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PROTAC CDK2/4/6 Degrader-2 Related Antibodies

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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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

 

Cellular Effect
Cell Line Type Value Description References
A-375 IC50
0.1659 μM
Compound: 3
Cytotoxicity against human A375 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human A375 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 33256948]
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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