2. PROTAC Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Apoptosis
  3. PROTACs RAR/RXR Androgen Receptor Apoptosis Caspase MDM-2/p53
  4. WCF-598

WCF-598 is a RXRγ (Kd: 234.2 nM) PROTAC degrader. WCF-598 induces RXRγ degradation via the ubiquitin-proteasome pathway and binds directly to RXRγ. WCF-598 indirectly induces AR-V7 degradation, impairs the stability of the RXRγ-AR-V7 complex, downregulates AR-V7 levels, and inhibits the transcription of downstream target genes of AR-V7. WCF-598 induces tumor cell apoptosis, inhibits cell proliferation, activates the p53 signaling pathway, and suppresses cell cycle progression. WCF-598 can be used for the research of prostate cancer.
(Pink: RXRγ ligand (HY-182352); Blue: Cereblon ligand (HY-138793); Black: linker).

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

WCF-598

WCF-598 Chemical Structure

CAS No. : 3059574-58-9

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WCF-598 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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RXRα RXRβ RXRγ

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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

WCF-598 is a RXRγ (Kd: 234.2 nM) PROTAC degrader. WCF-598 induces RXRγ degradation via the ubiquitin-proteasome pathway and binds directly to RXRγ. WCF-598 indirectly induces AR-V7 degradation, impairs the stability of the RXRγ-AR-V7 complex, downregulates AR-V7 levels, and inhibits the transcription of downstream target genes of AR-V7. WCF-598 induces tumor cell apoptosis, inhibits cell proliferation, activates the p53 signaling pathway, and suppresses cell cycle progression. WCF-598 can be used for the research of prostate cancer[1]. (Pink: RXRγ ligand (HY-182352); Blue: Cereblon ligand (HY-138793); Black: linker).

IC50 & Target[1]

RXRγ

 

Caspase 3

 

Caspase-7

 

In Vitro

WCF-598 (96 h) potently inhibits the viability of 22Rv1 cells with an IC50 of 13.56 nM, and exhibits an IC50 of 88.46 nM against VCaP-CRPC cells[1].
WCF-598 (6.25-6400 nM; 48 h) dose-dependently degrades RXRγ protein in 22Rv1 cells and VCaP-CRPC cells[1].
WCF-598 (6.25-6400 nM; 48 h) dose-dependently degrades AR-V7 protein in 22Rv1 cells, with a DC50 of 122.0 nM after 48 h of treatment[1].
WCF-598 (100-400 nM; 14 days) potently and concentration-dependently inhibits colony formation of 22Rv1 cells[1].
WCF-598 (100-400 nM; 72 h) induces apoptosis in 22Rv1 cells in a concentration-dependent manner, which is evidenced by increased levels of cleaved PARP and caspase-7, as well as enhanced Caspase-3/7 activity[1].
WCF-598 (100-400 nM; 48 h) activates p53-related pathways and inhibits cell cycle-related pathways in 22Rv1 cells in a concentration-dependent manner[1].

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

WCF-598 Related Antibodies

Western Blot Analysis[1]

Cell Line: 22Rv1, VCaP-CRPC
Concentration: 6.25, 12.5, 25, 50, 100, 200, 400, 800, 1600, 3200, 6400 nM
Incubation Time: 48 h
Result: Induced dose-dependent degradation of RXRγ in both cell lines, with DC50 values of 24.82 nM (22Rv1, maximal degradation 92.79%) and 27.15 nM (VCaP-CRPC, maximal degradation 82.01%).

Apoptosis Analysis[1]

Cell Line: 22Rv1
Concentration: 100, 200, 400 nM
Incubation Time: 72 h
Result: Induced concentration-dependent apoptosis in 22Rv1 cells, demonstrated by increased levels of cleaved-PARP and caspase-7, and significantly elevated Caspase-3/7 activity at all tested concentrations.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t MRT0-t F Vz CL
Rat[1] 3.0 mg/kg i.v. 3.85 h 0.08 h 39187.77 ng/mL 17400.36 ng·h/mL 0.86 h / 0.98 L/kg 2.91 mL/min/kg
Rat[1] 10.0 mg/kg p.o. 2.43 h 0.83 h 117.71 ng/mL 243.45 ng·h/mL 2.09 h 0.42 % / /
Rat[1] 5.0 mg/kg i.p. 7.69 h 5.33 h 743.64 ng/mL 6649.49 ng·h/mL 8.66 h 22.93 % / /
In Vivo

WCF-598 (10-20 mg/kg; i.p.; daily administration; 17 days) dose-dependently inhibits the growth of 22Rv1 castration-resistant prostate cancer (CRPC) xenografts in NOD-SCID mice[1].

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

Animal Model: NOD-SCID (male, 4 weeks old, injected subcutaneously with 22Rv1 CRPC cells)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: i.p.; daily; 17 days
Result: Achieved a tumor growth inhibition (TGI) value of 45.46% at 10 mg/kg.
Achieved a tumor growth inhibition (TGI) value of 61.18% at 20 mg/kg.
Significantly downregulated RXRγ protein levels in tumor tissues at both doses.
Induced degradation of androgen receptor (AR) and androgen receptor splice variant 7 (AR-V7) proteins in tumor tissues at both doses.
Caused no significant changes in mouse body weight during treatment.
Resulted in normal morphology and function of major organs (heart, liver, spleen, lung, kidney) per histopathological analysis.
Molecular Weight

894.11

Formula

C54H63N5O7
CAS No.
SMILES

O=C(CCCCCCCCCCCOC1=CC=CC2=C1CN(C2=O)C3CCC(NC3=O)=O)NC4=CC5=C(N(C6=CC7=C(C=C6C(C8=CC=C(C=C8)C(O)=O)=N5)C(C)(C)CCC7(C)C)C)C=C4
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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WCF-598 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:

WCF-5983059574-58-9WCF598WCF 598PROTACsRAR/RXRAndrogen ReceptorApoptosisCaspaseMDM-2/p53Retinoic acid receptorsRetinoid X receptorscastration-resistant prostate cancerp53 signaling pathwayCRPC cellsubiquitin-proteasome pathwayapoptosisRXRγAR-V7VCaP-CRPC cellsnuclear receptors22Rv1 cellsInhibitorinhibitorinhibit

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