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

ZAK-IN-2 (Compound 8) 是一种选择性的、共价的 ZAK 抑制剂，其 IC50 为 11.5 nM。ZAK-IN-2 可与 ZAK P 环中的 Cys22 形成共价键，从而抑制其激酶活性。ZAK-IN-2 可抑制下游靶点 p38 的磷酸化。ZAK-IN-2 可阻断 Doxorubicin (HY-15142A) 诱导的 Caspase 3 剪切。ZAK-IN-2 可用于心肌肥厚相关研究。

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ZAK-IN-2

ZAK-IN-2 Chemical Structure

CAS No. : 3033697-19-4

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ZAK-IN-2 相关抗体

Top Publications Citing Use of Products

查看 MAP3K 亚型特异性产品:

查看所有亚型
MAP3K7/TAK1 MAP3K8/COT/Tpl2 MAP3K6/ASK2 MAP3K5/ASK1 MAP3K12/DLK/Pref-1 NIK/MAP3K14

查看 Caspase 亚型特异性产品:

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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

查看 p38 MAPK 亚型特异性产品:

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

ZAK-IN-2 (60 min) 可强效抑制重组 ZAK 激酶，其 IC50 为 11.5 nM，且相较于 B-rafV600E 表现出高选择性[1]。
ZAK-IN-2 (0.01-10 μM; 1 h) 可剂量依赖性地抑制 U2OS 细胞中的 ZAKα 激酶活性，这一点可通过下游 p38 的磷酸化水平降低得到验证[1]。

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

ZAK-IN-2 相关抗体:

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.
分子量

668.67

Formula

C33H26F2N8O4S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

ZAK-IN-2 相关分类

  • 摩尔计算器

  • 稀释计算器

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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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