2. Apoptosis Cell Cycle/DNA Damage
  3. MDM-2/p53 Topoisomerase Bcl-2 Family Caspase Cyclin G-associated Kinase (GAK)
  4. ZM484

ZM484 is a potent dual p53-MDM2/TOP1 inhibitor that exhibits antiproliferative and antitumor activity both in vitro and in vivo. ZM484 effectively upregulates p53 and MDM2 proteins and maintains TOP1 inhibitory activity by the release of camptothecin (CPT) and a potent p53-MDM2 inhibitor. ZM484 induces cell cycle arrest and apoptosis by regulating the expression of key apoptosis- and cycle-related proteins, including caspase-3, Bcl-2, and Cyclin B1. ZM484 can be used for colorectal cancer research.

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

ZM484

ZM484 Chemical Structure

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ZM484 Related Antibodies

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Topoisomerase Topo I Topo II

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

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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

ZM484 is a potent dual p53-MDM2/TOP1 inhibitor that exhibits antiproliferative and antitumor activity both in vitro and in vivo. ZM484 effectively upregulates p53 and MDM2 proteins and maintains TOP1 inhibitory activity by the release of camptothecin (CPT) and a potent p53-MDM2 inhibitor. ZM484 induces cell cycle arrest and apoptosis by regulating the expression of key apoptosis- and cycle-related proteins, including caspase-3, Bcl-2, and Cyclin B1. ZM484 can be used for colorectal cancer research[1].

In Vitro

ZM484 (72 h) shows potent antiproliferative activity against three cancer cell lines HCT116, SJSA-1, and A549 with IC50 values of 0.03, 0.97, and 0.11 μM, respectively[1].
ZM484 (1.56-50 μM, 72 h) exhibits minimal cytotoxicity towards the noncancerous MRC-5 cell line[1].
ZM484 (3.125-100 μM, 30 min) shows no hemolytic activity at a concentration of 100 μM[1].
ZM484 (50 μM, 0-24 h) maintains an amount concentration of over 95% within 24 h, and exhibits excellent stability even in acidic buffer solutions with pH values of 2 or 5[1].
ZM484 (25-100 nM, 8 days) significantly reduces the colony formation ability of HCT116 cells[1].
ZM484 (0.195-200 μM, 15 min) inhibits TOP1 activity in a concentration-dependent manner, retaining efficacy at concentrations as low as 0.195 μM[1].
ZM484 (50-100 nM, 4 h) upregulates p53 and MDM2 protein levels in a concentration-dependent manner[1].
ZM484 (10-40 nM, 24 h) effectively induces cell cycle arrest in HCT116 cells in the S and G2 phases[1].
ZM484 (10-640 nM, 48 h) exhibits a potent, concentration-dependent proapoptotic effect in HCT116 cells, which is concomitant with a dose-dependent decrease in the expression levels of caspase-3, Bcl-2[1].

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

ZM484 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: HCT116 cells
Concentration: 25, 50, and 100 nM
Incubation Time: 8 days
Result: Significantly reduced the colony formation ability of HCT116 cells at concentrations of 25, 50, and 100 nM.

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 50 and 100 nM
Incubation Time: 4 h
Result: Increased p53 and MDM2 protein levels in a concentration-dependent manner.
Exhibited more activity than Idasanutlin (HY-15676) at 50 and 100 nM for p53 protein upregulation.

Cell Cycle Analysis[1]

Cell Line: HCT116 cells
Concentration: 10 and 40 nM
Incubation Time: 24 h
Result: Induced a dose-dependent increase in the S phase (29.8 % and 43.3 % at 10 and 40 nM, respectively) and G2 phase (20.9 % and 28.3 %) cell populations.

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 40, 160, and 640 nM
Incubation Time: 48 h
Result: Induced significant apoptosis in a concentration-dependent manner, with apoptotic rates of 11.6 %, 16.8 %, and 25.8 % at concentrations of 40, 160, and 640 nM, respectively.
Induced apoptosis more effectively than Idasanutlin or the vehicle control.
Decreased the expression levels of caspase-3, Bcl-2 in a dose-dependent manner.
In Vivo

ZM484 (10 mg/kg, i.p., every other day for 12 days) exhibits significant tumor growth inhibition in a HCT116 xenograft model[1].

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

Animal Model: Female BALB/c nude mice (4-6 weeks) subcutaneously injected with HCT116 cells[1]
Dosage: 10 mg/kg
Administration: i.p., every other day for 12 days
Result: Exhibited the highest tumor growth inhibition (TGI of 81.07 %) among the tested groups, surpassing the positive controls Idasanutlin (25 mg/kg, i.g., qd, TGI = 68.59 %) and Irinotecan (HY-16562) (50 mg/kg, i.p., qw, TGI = 64.01 %).
Molecular Weight

1374.35

Formula

C67H72Cl2F2N6O15S2
SMILES

O=C1C2=C(C=C3C4=NC5=CC=CC=C5C=C4CN31)[C@](OC(OCCSSCCOC(CCOCCOCCOCCOCCNC(C6=CC(OC)=C(NC([C@@H]([C@@H]([C@]7(C8=C(C=C(C=C8)Cl)F)C#N)C9=CC=CC(Cl)=C9F)N[C@H]7CC(C)(C)C)=O)C=C6)=O)=O)=O)(C(OC2)=O)CC
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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ZM484 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:

ZM484ZM 484ZM-484MDM-2/p53TopoisomeraseBcl-2 FamilyCaspaseCyclin G-associated Kinase (GAK)Auxilin 2p53MDM2TOP1antiproliferativeantitumorcell cycle arrestCPTapoptosiscaspase-3Bcl-2Cyclin B1colorectal cancerHCT116SJSA-1A549HCT116 xenograft modelInhibitorinhibitorinhibit

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