2. Vitamin D Related/Nuclear Receptor Epigenetics
  3. Androgen Receptor Histone Acetyltransferase
  4. JZY3032

JYZ3032 is an orally active super inhibitor of androgen receptor (AR) and p300/CBP. JYZ3032 redirects the catalytic activity of p300 and locks the complex in a transcriptionally inactive state, thereby inhibiting AR-driven transcription and proliferation. JYZ3032 induces deep and durable tumor regression in castration-resistant and patient-derived xenograft models, and exhibits good tolerability. JYZ3032 can be used in research related to metastatic castration-resistant prostate cancer and prostate cancer.

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

JZY3032

JZY3032 Chemical Structure

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JZY3032 Related Antibodies

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CBP/p300 GCN5/PCAF TIP60 MOZ/MORF HBO1

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Description

JYZ3032 is an orally active super inhibitor of androgen receptor (AR) and p300/CBP. JYZ3032 redirects the catalytic activity of p300 and locks the complex in a transcriptionally inactive state, thereby inhibiting AR-driven transcription and proliferation. JYZ3032 induces deep and durable tumor regression in castration-resistant and patient-derived xenograft models, and exhibits good tolerability. JYZ3032 can be used in research related to metastatic castration-resistant prostate cancer and prostate cancer[1].

IC50 & Target

p300

 

In Vitro

JYZ3032 (1.0 nM; 120 h) potently inhibits the growth of 22Rv1 prostate cancer cells with an IC50 of 1.0 nM and 69% maximum growth inhibition[1].
JYZ3032 (100 nM, Serial dilutions; 4 h pulse treatment, total 120 h) exhibits durable, sustained growth inhibitory activity in VCaP and LNCaP prostate cancer cells, with a 4-hour pulse treatment yielding comparable efficacy to continuous exposure[1].
JYZ3032 potently suppresses enhancer-associated histone acetylation marks in VCaP prostate cancer cells but not in AR-negative Kelly neuroblastoma cells, demonstrating lineage selectivity[1].

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

JZY3032 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: 22Rv1 prostate cancer cells
Concentration: 1.0 nM
Incubation Time: 120 h
Result: Inhibited 22Rv1 cell growth with an IC50 of 1.0 nM and a maximum inhibition (Imax) of 69%.

Cell Proliferation Assay[1]

Cell Line: VCaP, LNCaP, CWR-R1 prostate cancer cells
Concentration: Serial dilutions
Incubation Time: 120 h
Result: Exhibited potent cytotoxicity across all tested AR-positive prostate cancer cells, with superior activity relative to the combined treatment with AR-LBD inhibitor JZY3221 and p300/CBP BRD inhibitor GNE-049.
Activity was comparable to or better than the p300/CBP dual degrader CBPD-409 (HY-158113).
Parmacokinetics
Species Dose Route T1/2 Cmax AUC0-24 Vss CL Bioavailability
Mice[1] 5.0 mg/kg p.o. 5.1 h 284 ng/mL 2952 ng·h/mL / / 18.5 %
Mice[1] 2.0 mg/kg i.v. 5.0 h 5906 ng/mL 6394 ng·h/mL 1.3 L/kg 5.2 mL/min/kg /
In Vivo

JYZ3032 (30 mg/kg; i.p.) induces tumor regression in 75% of castrated male NSG mice bearing VCaP castration-resistant prostate cancer xenografts[1].
YZ3032 (60 mg/kg; p.o.) also achieves significant tumor inhibition with good tolerance[1].
JYZ3032 induces complete tumor regression and 100% survival for at least 35 days in NSG mice bearing patient-derived prostate cancer xenografts of MDA-PCa-183, significantly inhibits tumor growth in the MDA-PCa-146-12 model, and exhibits good tolerance[1].

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

Animal Model: NSG (male, castrated)[1]
Dosage: 30 mg/kg (i.p.); 60 mg/kg (p.o.)
Administration: i.p.; p.o.
Result: Induced tumor regression in 75% (12 of 16) of treated tumors.
Achieved robust tumor suppression that outperformed a combination of a p300 bromodomain inhibitor and an AR-LBD inhibitor.
Increased AR-p300 proximity in treated tumors.
Reduced ERG, PSA, MYC, Ki67, H3K27ac, and H2BK20ac signals in treated tumors.
Left AR, p300, and CBP levels unchanged.
Caused no significant changes in body weight, serum liver/kidney function, or hematologic parameters.
Molecular Weight

974.58

Formula

C52H62ClF2N13O2
SMILES

CN1N=CC(C2=CC3=C(N(C4=NN([C@H](CC5)CC[C@@H]5CN(CC6)CCN6C(C=C7)=NN=C7C(N[C@H]8CC[C@@H](CC8)N(C)C9=CC=C(C(Cl)=C9)C#N)=O)C%10=C4CN(C(C)=O)CC%10)CCC3)C=C2C(F)F)=C1
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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JZY3032 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:

JZY3032JZY 3032JZY-3032Androgen ReceptorHistone AcetyltransferaseHATsHATpatient-derived organoidsHEK293 cellsp300/CBPLNCaPmetastatic castration-resistant prostate cancerAR-positive prostate cancer cells22Rv1VCaPcastration-resistant prostate cancerandrogen receptorInhibitorinhibitorinhibit

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