ZMF-28
ZMF-28 is a selective PAK1 inhibitor with an IC50 of 0.02 μM. ZMF-28 induces DNA damage and Apoptosis. ZMF-28 downregulates PD-L1 protein expression through post-translational regulation after inhibiting PAK1. ZMF-28 exhibits anticancer activity against triple-negative breast cancer.
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- Fòrmula: C29H31ClN6O
- Peso molecular:515.05
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
PAK1 0.02 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BT-549 | IC50 |
0.37 μM
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Antiproliferative activity against human BT-549 TNBC cells assessed by MTT viability assay.
Antiproliferative activity against human BT-549 TNBC cells assessed by MTT viability assay.
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42748864 |
| 4T1 | IC50 |
0.22 μM
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Antiproliferative activity against mouse 4T1 TNBC cells assessed by MTT viability assay.
Antiproliferative activity against mouse 4T1 TNBC cells assessed by MTT viability assay.
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42748864 |
In Vitro
ZMF-28 has antiproliferative activity against BT-549 (IC50 = 0.37 μM) and 4T1 (IC50 = 0.22 μM) cells[1].
ZMF-28 (1.0-4 μM; one week) suppresses colony formation and proliferation of BT-549 and 4T1 cells[1].
ZMF-28 (1.0-4 μM; 24 h) reverses EMT marker expression in BT-549 and 4T1 cells by increasing E-cadherin and decreasing MMP-2 and Snail[1].
ZMF-28 (1-4 μM; 24 h) downregulates PD-L1 protein post-translationally via PAK1 inhibition in BT-549 and 4T1 cells[1].
ZMF-28 (40 min) is a potent PAK1 inhibitor (IC50 = 0.02 μM) with selectivity over PAK2-PAK6[1].
ZMF-28 (1.0 μM) shows favorable selectivity for PAK1 across a 378-kinase panel[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BT-549 and 4T1 cells
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Concentration:0, 1, 2, and 4 μM
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Incubation Time:24 h
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Result:Western blot showed dose-dependent reduction of PAK1, p-PAK1S144, and PD-L1 in both BT-549 and 4T1 cells. siRNA-mediated PAK1 knockdown significantly reduced PD-L1 protein expression, comparable to the reduction observed.
Parmacokinetics
| Species | Dose | Route | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ | Tmax | CLz/F | Vz/F | Cmax |
|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 5.0 mg/kg | i.p. | 421.45 μg/L·h | 428.77 μg/L·h | 3.85 h | 4.13 h | 0.64 h | 23.48 L/h/kg | 99.16 L/kg | 167.67 μg/L |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 3-4 weeks old)[1]
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Dosage:2.5 mg/kg; 5 mg/kg
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Administration:8 days
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Result:Tumor growth was suppressed in both groups.
Slowed tumor growth and reduced final tumor weight.
Resulted in dose-dependent downregulation of PAK1, p-PAK1S144, and PD-L1, accompanied by upregulation of Bax expression in tumor tissues.
Reduced Ki-67 and PD-L1 expression levels in tumor tissues.
Chemical Information
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Peso molecular 515.05
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Fòrmula C29H31ClN6O
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SMILES
O=C1C(C2=CC=C(C=C2Cl)C3=CC=CC(C)=N3)=CC4=C(N1CCC5CCNCC5)N=C(N=C4)NC6CC6
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ZMF-28 Related Classifications
HY-189934 Related Classifications
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