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

ZAK-IN-1 是一种口服有效且选择性的 亮氨酸拉链和不育α基序激酶 ZAK 抑制剂，其 IC50 为 4 nM，KD 为 8 nM。ZAK-IN-1 对 403 种野生型激酶显示出优异的选择性。 ZAK-IN-1 能够阻断 p38/GATA-4 和 JNK/c-Jun 信号通路，并可显著抑制心肌肥大。ZAK-IN-1 可用于肥厚型心肌病 (HCM) 的研究。

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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 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

ZAK-IN-1 (Compound 6p) (0-10 μg/mL, 24 h) 在 H9c2 细胞中通过阻断 p38/GATA-4 和 JNK/c-Jun 信号通路，有效抑制由 ZAKα 过表达引发的心肌细胞肥大。

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

ZAK-IN-1 相关抗体:

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.
药代动力学
(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
体内研究
(In Vivo)

ZAK-IN-1 (Compound 6p) (0-10 mg/kg, p.o., 每日 1 次共 8 周) 在自发性高血压大鼠模型中展现了良好的抗心肌肥大效果[1]。

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.
分子量

559.55

Formula

C27H19F2N7O3S
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-1 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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