1. GPCR/G Protein
  2. Ras
  3. ZT-12-037-01

ZT-12-037-01 

Cat. No.: HY-122866
Handling Instructions

ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC50 of 24 nM.

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

ZT-12-037-01 Chemical Structure

ZT-12-037-01 Chemical Structure

CAS No. : 2328073-61-4

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Description

ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC50 of 24 nM[1].

In Vitro

ZT-12-037-01 (3 μM; 14 days) significantly inhibits mutant NRAS-STK19-driven melanocyte colony formation and proliferation[1].
ZT-12-037-01 (0-3 μM) has an inhibitory effects of ZT-12-037-01 on STK19WT and STK19D89N-activated NRAS phosphorylation in HPMs[1].

Cell Proliferation Assay[1]

Cell Line: CDK4 (R24C) melanocyte cells; hTERT melanocyte cells; p53DD melanocyte cells
Concentration: 3 μM
Incubation Time: 14 days
Result: Inhibited melanocyte proliferation.

Western Blot Analysis[1]

Cell Line: STK19WT and STK19D89N
Concentration: 0 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM
Incubation Time:
Result: Inhibited NRAS phosphorylation.
In Vivo

ZT-12-037-01 (injection subcutaneously; 25-50 mg/kg; once daily; 21 days) inhibits growth of SK-MEL-2 xenograft melanoma and the sections of tumors indicates induction of apoptosis by increasing cleaved caspase-3[1].

Animal Model: SK-MEL-2 xenograft melanoma nude mice with hTERT/p53DD/CDK4(R24C) melanocytes[1]
Dosage: 25 mg/kg; 50 mg/kg
Administration: Injected subcutaneously; 21 days
Result: Inhibited growth of SK-MEL-2 xenograft melanoma.
Molecular Weight

385.50

Formula

C₂₁H₃₁N₅O₂

CAS No.

2328073-61-4

SMILES

COC1=CC2=NC(NC3CC3)=NC(NC4CCN(C(C)C)CC4)=C2C=C1OC

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 8.33 mg/mL (21.61 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5940 mL 12.9702 mL 25.9403 mL
5 mM 0.5188 mL 2.5940 mL 5.1881 mL
10 mM 0.2594 mL 1.2970 mL 2.5940 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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ZT-12-037-01
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HY-122866
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