2. Epigenetics Metabolic Enzyme/Protease
  3. Methionine Adenosyltransferase (MAT)
  4. ZS34

ZS34 is a potent, orally active, and selective MAT2A inhibitor with an IC50 of 13.7 nM, displaying minimal hERG and UGT1A1 liabilities. ZS34 selectively suppresses the growth of methylthioadenosine phosphorylase (MTAP)-deficient cancer cells by inhibiting SAM synthesis, reducing SDMA levels, and inducing DNA damage. ZS34 exhibits antitumor efficacy in a HCT116 MTAP-/- xenograft mouse model. ZS34 can be used for the research of MTAP-deficient cancer.

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ZS34

ZS34 Chemical Structure

CAS No. : 3106086-17-0

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ZS34 Related Antibodies

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Description

ZS34 is a potent, orally active, and selective MAT2A inhibitor with an IC50 of 13.7 nM, displaying minimal hERG and UGT1A1 liabilities. ZS34 selectively suppresses the growth of methylthioadenosine phosphorylase (MTAP)-deficient cancer cells by inhibiting SAM synthesis, reducing SDMA levels, and inducing DNA damage. ZS34 exhibits antitumor efficacy in a HCT116 MTAP-/- xenograft mouse model. ZS34 can be used for the research of MTAP-deficient cancer[1].

IC50 & Target[1]

MAT2A

13.7 nM (IC50)

In Vitro

ZS34 (10 days) inhibits the proliferation of MTAP deficiency cells (NCI-H838, NCI-H1437, MCF-7, MDA-MB-231 and MIA PaCa-2 cells) with IC50s of 1.70, 386, 38.1, 37.2, and 115 nM, respectively, exhibiting selectivity over MTAP proficiency cells (A-375, AsPC-1, DU145, NCI-H460 and NCI-H520) with IC50s >10000 nM[1].
ZS34 (10 days) exhibits potent antiproliferative effects against HCT116 MTAP-null cells (IC50 = 124 nM) but weak activity against WT HCT116 cells (IC50 > 10000 nM), demonstrating excellent selectivity inhibition with a selective indices (SI) exceeding 80.6[1].
ZS34 (0-10 μM; 96 h) selectively induces DNA damage in MTAP-deficient HCT116 cells through MAT2A inhibition[1].
ZS34 binds to the allosteric site of the MAT2A dimer, forming hydrogen bonds with Arg313 and a coordinated water molecule, and engaging in π-π stacking with Phe20, Trp274, and Phe18, while its ortho-methyl group participates in a CH-π interaction with Phe333[1].

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

ZS34 Related Antibodies

Western Blot Analysis[1]

Cell Line: HCT116 (MTAP-/-) and HCT116 (WT)
Concentration: 0, 0.1, 1 μM
Incubation Time: 96 h
Result: Induced a dose-dependent decrease in the SDMA level, in HCT116 MTAP-/- cells, but not in HCT116 WT cells.
Induced a marked increase in γH2AX levels, a marker of DNA damage, in HCT116 MTAP-/- cells, but not in HCT116 WT cells.

Immunofluorescence[1]

Cell Line: HCT116 (MTAP-/-) and HCT116 (WT)
Concentration: 0.1, 1, 10 μM
Incubation Time: 96 h
Result: led to a marked increase in γH2AX levels in HCT116 MTAP-/-cells compared to the control, but not in HCT116 WT cells.
Parmacokinetics
Species Dose Route T1/2 Cmax AUCinf F Tmax MRTINF_obs ClF_obs Vss_obs
Mice[1] 10 mg/kg p.o. 2.53 h 8049 ng/mL 17549 ng·h/mL 148 % 0.33 h 2.35 h / /
Mice[1] 5 mg/kg i.v. 1.02 h / 5946 ng·h/mL / / 0.88 h 15.6 mL/min/kg 792 mL/kg
In Vivo

ZS34 (10 and 30 mg/kg, p.o., daily for 30 days) demonstrats robust in vivo antitumor efficacy and a favorable safety profile in the HCT116 MTAP-/- xenograft moues model[1].
ZS34 (400 mg/kg, p.o., single dose) shows no obvious toxicity in mice[1].

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

Animal Model: Female ALB/c nude mice subcutaneously inoculated with HCT116 MTAP-/- cells[1]
Dosage: 10, 30 mg/kg
Administration: p.o., daily for 30 days
Result: Significantly suppressed tumor growth, with tumor growth inhibition (TGI) values of 57.3% and 89.0% at 10 and 30 mg/kg, respectively.
Showed a tendency to cause tumor regression at 30 mg/kg.
Reduced SAM levels in tumors.
Showed no significant body weight loss compared to control.
Animal Model: ICR mice[1]
Dosage: 400 mg/kg
Administration: p.o., single dose
Result: Was well tolerated at this high dose.
Molecular Weight

339.78

Formula

C18H14ClN3O2
CAS No.
SMILES

O=C1N(C2=C(C(NC)=N1)C3=C(C(Cl)=C2)C=CO3)C4=CC=CC=C4C
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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ZS34 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:

ZS343106086-17-0ZS 34ZS-34Methionine Adenosyltransferase (MAT)S-adenosylmethionine Synthetasemethylthioadenosine phosphorylase (MTAP)-deficient cancer cellsSAM synthesisSDMADNA damageHCT116 MTAP-/- xenograft mouse modelInhibitorinhibitorinhibit

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