2. MAPK/ERK Pathway Apoptosis
  3. MAP3K Caspase p38 MAPK
  4. ZAK-IN-2

ZAK-IN-2 (Compound 8) is a selective, covalent ZAK inhibitor with an IC50 of 11.5 nM. ZAK-IN-2 forms a covalent bond with Cys22 in the P-loop of ZAK to inhibit its kinase activity. ZAK-IN-2 inhibits the phosphorylation of the downstream target p38. ZAK-IN-2 blocks Doxorubicin (HY-15142A)-induced cleavage of Caspase 3. ZAK-IN-2 is applicable to research related to myocardial hypertrophy.

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

ZAK-IN-2

ZAK-IN-2 Chemical Structure

CAS No. : 3033697-19-4

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ZAK-IN-2 Related Antibodies

Top Publications Citing Use of Products

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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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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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Description

ZAK-IN-2 (Compound 8) is a selective, covalent ZAK inhibitor with an IC50 of 11.5 nM. ZAK-IN-2 forms a covalent bond with Cys22 in the P-loop of ZAK to inhibit its kinase activity. ZAK-IN-2 inhibits the phosphorylation of the downstream target p38. ZAK-IN-2 blocks Doxorubicin (HY-15142A)-induced cleavage of Caspase 3. ZAK-IN-2 is applicable to research related to myocardial hypertrophy[1].

IC50 & Target[1]

p38

 

Caspase 3

 

In Vitro

ZAK-IN-2 (60 min) potently inhibits recombinant ZAK kinase with an IC50 of 11.5 nM, and exhibits high selectivity over B-rafV600E[1].
ZAK-IN-2 (0.01-10 μM; 1 h) dose-dependently inhibits ZAKα kinase activity in U2OS cells, which is verified by the reduced phosphorylation level of downstream p38[1].

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

ZAK-IN-2 Related Antibodies

Western Blot Analysis[1]

Cell Line: Human U2OS osteosarcoma cells, CRISPR-generated ZAK knockout U2OS cells
Concentration: 10 μM
Incubation Time: Undefined
Result: Prevented doxorubicin-induced caspase 3 cleavage in U2OS cells, matching the effect seen in ZAK knockout cells.
Inhibited doxorubicin-induced phosphorylation of p38 and JNK.
Prevented massive cell death induced by 24 h doxorubicin treatment in U2OS cells, matching the protection seen in ZAK knockout cells.
Molecular Weight

668.67

Formula

C33H26F2N8O4S
CAS No.
SMILES

O=C(N1CCC(C1)OC2=NNC3=C2C=C(C4=CN(C5=C(F)C(NS(=O)(C6=CC=CC(C7=CC=CC=C7)=C6)=O)=CC=C5F)N=N4)C=N3)C=C
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Purity & Documentation
References
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ZAK-IN-2 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-23033697-19-4MAP3KCaspasep38 MAPKMAP kinase kinase kinase, MEKK, MAPKKKZAKLIMK2Cys22LIMK1B-rafV600Ecaspase 3inflammatory diseasesLCKcardiac hypertrophyp38 mitogen-activated protein kinaseInhibitorinhibitorinhibit

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