2. MAPK/ERK Pathway
  3. MAP3K
  4. ZAK-IN-1

ZAK-IN-1 is an orally active and selective selective leucine-zipper and sterile‑α motif kinase (ZAK) inhibitor with IC50 of 4 nM and KD of 8 nM. ZAK-IN-1 exhibits excellent selectivity against a panel of 403 wild-type kinases. ZAK-IN-1 blocks p38/GATA-4 and JNK/c-Jun signaling and shows promising anti antihypertrophic cardiomyopathy (HCM) efficacy. ZAK-IN-1 can be used for the study of HCM.

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ZAK-IN-1 Chemical Structure

ZAK-IN-1 Chemical Structure

CAS No. : 2362525-64-0

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ZAK-IN-1 Related Antibodies

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Description

ZAK-IN-1 is an orally active and selective selective leucine-zipper and sterile‑α motif kinase (ZAK) inhibitor with IC50 of 4 nM and KD of 8 nM. ZAK-IN-1 exhibits excellent selectivity against a panel of 403 wild-type kinases. ZAK-IN-1 blocks p38/GATA-4 and JNK/c-Jun signaling and shows promising anti antihypertrophic cardiomyopathy (HCM) efficacy. ZAK-IN-1 can be used for the study of HCM[1].

In Vitro

ZAK-IN-1 (Compound 6p) (0-10 μg/mL, 24 h) could effectively suppress hypertrophy induced by ZAKα overexpression by blocking p38/GATA-4 and JNK/c-Jun signaling in H9c2 cells.

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

ZAK-IN-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: H9c2 cells
Concentration: 0, 2.5, 5, 10 μg/mL
Incubation Time: 24 h
Result: Dose dependently inhibited the phosphorylated ZAKα but had no detectable impact on the ZAKα expression level.
Blocked the cardiac hypertrophy induced by AngII and Doxycycline (HY-N0565) .
Dose dependently decreased the expression of brain natriuretic peptide (BNP).
Suppressed the elevation of p-JNK and p-p38 and hypertrophic transcription factors p-GATA-4 and p-c-Jun.
Parmacokinetics
Species Dose Route Indicator value
Rat 10 mg/kg p.o. Cmax 16372.2 μg/L
Rat 2.5 mg/kg i.v. AUC0-∞ 27866.1 μg/L·h
Rat 10 mg/kg p.o. T1/2 1.7 h
Rat 2.5 mg/kg i.v. AUC0-t 27424.4 μg/L·h
Rat 10 mg/kg p.o. AUC0-t 71572.6 μg/L·h
Rat 2.5 mg/kg i.v. T1/2 1.6 h
Rat 10 mg/kg p.o. AUC0-∞ 71790.9 μg/L·h
Rat 2.5 mg/kg i.v. Cmax 34151.6 μg/L
Rat 10 mg/kg p.o. Bioavailability 65.3 %
Rat 2.5 mg/kg i.v. CL 91.9 L/h/kg
In Vivo

ZAK-IN-1 (Compound 6p) (0-10 mg/kg, p.o., once daily for 8 weeks) displays promising anti-HCM effect in the mice SHR model[1].

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

Animal Model: Spontaneous hypertensive rats (SHR) model established by SD male rats (180-220 g) [1]
Dosage: 0, 2.5, and 10 mg/kg
Administration: Oral administration (p.o.), once daily for 8 weeks
Result: Suppressed the whole heart and the left ventricle mass elevation and rescued the hypertrophic symptoms in a dose-dependent manner.
Suppressed the phosphorylation of ZAK down-stream signaling JNK, p38, c-Jun, p-GATA-4, and protein levels of hypertrophic markers BNP and ANP in a dose-dependent manner.
Molecular Weight

559.55

Formula

C27H19F2N7O3S
CAS No.
SMILES

FC1=CC=C(NS(C2=CC=CC(C3=CC=CC=C3)=C2)(=O)=O)C(F)=C1N4N=NC(C5=CN=C(NN=C6OC)C6=C5)=C4
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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ZAK-IN-1 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:

ZAK-IN-12362525-64-0MAP3KMAP kinase kinase kinase, MEKK, MAPKKKAntihypertrophic cardiomyopathyHypertensive rat (SHR) modelH9c2Inhibitorinhibitorinhibit

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