2. PROTAC Cell Cycle/DNA Damage Apoptosis
  3. PROTACs CDK Apoptosis
  4. WWZ-11-098

WWZ-11-098 is a selective CDK6 PROTAC degrader with DC50 of 2.6 nM. WWZ-11-098 induces degradation of CDK6 in a CRBN-dependent manner, while sparing CDK1, CDK2, CDK4, and CDK9. WWZ-11-098 induces apoptosis, G1-S cell cycle arrest and shows anti-proliferative activity in cancer cells. WWZ-11-098 exhibits antitumor efficacy in a xenograft model without signs of toxicity. WWZ-11-098 can be used for the research of leukemia.
(Pink: CDK6 ligand (HY-181501); Blue: Cereblon E3 ligase ligand; Black: linker).

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

WWZ-11-098

WWZ-11-098 Chemical Structure

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Based on 1 publication(s) in Google Scholar

WWZ-11-098 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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Description

WWZ-11-098 is a selective CDK6 PROTAC degrader with DC50 of 2.6 nM. WWZ-11-098 induces degradation of CDK6 in a CRBN-dependent manner, while sparing CDK1, CDK2, CDK4, and CDK9. WWZ-11-098 induces apoptosis, G1-S cell cycle arrest and shows anti-proliferative activity in cancer cells. WWZ-11-098 exhibits antitumor efficacy in a xenograft model without signs of toxicity. WWZ-11-098 can be used for the research of leukemia[1]. (Pink: CDK6 ligand (HY-181501); Blue: Cereblon E3 ligase ligand; Black: linker).

IC50 & Target[1]

CDK6

2.6 nM (DC50)

In Vitro

WWZ-11-098 ( 5 days) potently inhibits the proliferation of MOLT-4 cells (IC50 = 70 nM) and MV4-11 cells (IC50 = 0.13 μM)[1].
WWZ-11-098 (10 nM-10 μM; 3-24 h) potently and selectively degrades CDK6 in MOLT-4 cells with a DC50 of 2.6 nM, achieving over 98% degradation at 100 nM for 24 h, while sparing CDK1, CDK2, CDK4, and CDK9, via a CRBN-dependent mechanism[1].
WWZ-11-098 (100-200 nM; 48 h) induces G1-S cell cycle arrest and induces apoptosis in MOLT-4 cells[1].

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

WWZ-11-098 Related Antibodies

Western Blot Analysis[1]

Cell Line: MOLT-4 cells
Concentration: 10, 100 nM, 10 μM
Incubation Time: 3, 6, 9, 12, 24 h
Result: Achieved 98% degradation of CDK6 at 100 nM for 24 h.
Induced dose-dependent CDK6 degradation with a DC50 of 2.6 nM and a Dmax exceeding 99%, with no hook effect up to 10 μM.
Depleted over 80% of CDK6 within 3 h of treatment with 100 nM.
Showed rescued CDK6 degradation by pre-treatment with CDK2/4/6 inhibitor, MG132 (HY-13259), confirming CRBN-dependent activity via the ubiquitin-proteasome pathway.

Cell Cycle Analysis[1]

Cell Line: MOLT-4 cells
Concentration: 100, 200 nM
Incubation Time: 48 h
Result: Induced G1-S cell cycle arrest in MOLT-4 cells, with a stronger effect than control compounds at equivalent concentrations.

Apoptosis Analysis[1]

Cell Line: MOLT-4 cells
Concentration: 100, 200 nM
Incubation Time: 48 h
Result: Significantly promoted apoptosis in MOLT-4 cells, with superior efficacy compared to control compounds.
Parmacokinetics
Species Dose Route T1/2 Cmax Tmax AUC0-∞ AUC0-t F C0 CL
Mice[1] 5 mg/kg i.v. 2.64 ± 0.899 h 11833 ± 1242 ng/mL 0.0833 ± 0.000 h 7821 ± 1464 ng·h/mL 7766 ± 1393 ng·h/mL / 17358 ± 2227 ng/mL 655 ± 123 mL/h/kg
Mice[1] 20 mg/kg p.o. 0.293 ± 0.0441 h 294 ± 155 ng/mL 0.250 ± 0.00 h 203 ± 97.4 ng·h/mL 201 ± 97.5 ng·h/mL 0.647 ± 0.31 % / /
In Vivo

WWZ-11-098 (10 mg/kg; i.v.; daily; 21 consecutive days) drives robust, well-tolerated tumor growth inhibition in MOLT-4 xenografts mice model[1].

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

Animal Model: Nude mice (male, 4-6 weeks old, 18-22 g, MOLT-4 cell line xenograft model)[1]
Dosage: 10 mg/kg
Administration: 21 days
Result: Induced sustained degradation of CDK6 and corresponding reductions of phosphorylated retinoblastoma protein (p-RB) in tumor tissues 6 hours after final dose at day 3.
Significantly suppressed MOLT-4 xenograft tumor growth, with marked reductions in both tumor volume and final tumor weight.
Caused no significant body weight loss throughout the study.
Molecular Weight

828.90

Formula

C39H47F3N8O7S
SMILES

COC1=C(C=C(C=C1)C(N2[C@H](CN(C[C@@H]2C)C3=CC=C(C=C3)S(=O)(N4CCC(CC4)NC5=NC=C(C(OC6CCCC6)=N5)C(F)(F)F)=O)C)=O)N7CCC(NC7=O)=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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WWZ-11-098 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:

WWZ-11-098PROTACsCDKApoptosisCyclin dependent kinaseCRBNacute lymphoblastic leukemiaCereblonCDK6G1-S cell cycle arrestMOLT-4 cellsleukemiaInhibitorinhibitorinhibit

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