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

ZAK-IN-1 Chemical Structure

CAS No. : 2362525-64-0

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Based on 1 publication(s) in Google Scholar

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].

Cellular Effect
Cell Line Type Value Description References
Sf9 IC50
4 nM
Compound: 6p
Inhibition of N-terminal GST-tagged recombinant human full-length ZAK expressed in baculovirus infected Sf9 insect cells using MBP as substrate after 30 mins by ADP-Glo assay
Inhibition of N-terminal GST-tagged recombinant human full-length ZAK expressed in baculovirus infected Sf9 insect cells using MBP as substrate after 30 mins by ADP-Glo assay
[PMID: 31244114]
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[1].

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.
Appearance

Solid

Color

White to off-white

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

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (178.72 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7872 mL 8.9358 mL 17.8715 mL
5 mM 0.3574 mL 1.7872 mL 3.5743 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7872 mL 8.9358 mL 17.8715 mL 44.6788 mL
5 mM 0.3574 mL 1.7872 mL 3.5743 mL 8.9358 mL
10 mM 0.1787 mL 0.8936 mL 1.7872 mL 4.4679 mL
15 mM 0.1191 mL 0.5957 mL 1.1914 mL 2.9786 mL
20 mM 0.0894 mL 0.4468 mL 0.8936 mL 2.2339 mL
25 mM 0.0715 mL 0.3574 mL 0.7149 mL 1.7872 mL
30 mM 0.0596 mL 0.2979 mL 0.5957 mL 1.4893 mL
40 mM 0.0447 mL 0.2234 mL 0.4468 mL 1.1170 mL
50 mM 0.0357 mL 0.1787 mL 0.3574 mL 0.8936 mL
60 mM 0.0298 mL 0.1489 mL 0.2979 mL 0.7446 mL
80 mM 0.0223 mL 0.1117 mL 0.2234 mL 0.5585 mL
100 mM 0.0179 mL 0.0894 mL 0.1787 mL 0.4468 mL
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ZAK-IN-1 Related Classifications

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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