2. MAPK/ERK Pathway Stem Cell/Wnt
  3. ERK
  4. ERK5-IN-4

ERK5-IN-4 (compound 34b) 是细胞外信号相关激酶 5 (ERK5) 的选择性抑制剂。ERK5-IN-4 抑制剂在 HEK293 细胞中抑制 ERK5 全长激酶 和截断 ERK5 (ERK5ΔTAD) 激酶活性的 IC50 分别为 77 nM 和 300 nM。

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ERK5-IN-4 Chemical Structure

ERK5-IN-4 Chemical Structure

CAS No. : 1888305-17-6

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ERK5-IN-4 相关抗体

Top Publications Citing Use of Products

查看 ERK 亚型特异性产品:

查看所有亚型
ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ERK5-IN-4 (compound 34b) is a potent and selective inhibitor of extracellular signal-related kinase 5 (ERK5). ERK5-IN-4 inhibits ERK5 (full-length) and truncated ERK5 (ERK5 ΔTAD) kinase activity in HEK293 cells with an IC50 of 77 nM and 300 nM, respectively[1].

IC50 & Target

ERK5

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A498 GI50
22.3 nM
Compound: 34b
Antiproliferative activity against human A498 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay
Antiproliferative activity against human A498 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay
[PMID: 35468293]
HEK293 GI50
19.6 μM
Compound: 34b
Antiproliferative activity against HEK293 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay
Antiproliferative activity against HEK293 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay
[PMID: 35468293]
MDA-MB-231 GI50
26.6 nM
Compound: 34b
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay
[PMID: 35468293]
SJSA-1 GI50
25 nM
Compound: 34b
Antiproliferative activity against human SJSA-1 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay
Antiproliferative activity against human SJSA-1 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay
[PMID: 35468293]
体外研究
(In Vitro)

ERK5-IN-4 (compound 34b) is selective against MAP3K, p38 (IC50>30 μM) and BRD4 (IC50>20 μM), in contrast to many reported ERK5 inhibitors[1].
ERK5-IN-4 (0-100 μM; 72 h) suppresses ERK5 kinase activity in HEK293 cells and (0-1 μM; 72 h) induces paradoxical activation of ERK5 transcriptional activity, thus resulting in C-terminal transcriptional activation domain (TAD) separated from the nuclear localization sequence (NLS) and results ERK5 nuclear translocation[1].
ERK5-IN-4 inhibits cancer cells with GI50 of 19.6 μM (HEK293), 22.3 μM (A498), 25 μM (SJSA-1), 26.6 μM (MDA-MB-231) following a 72 h incubation[1].
ERK5-IN-4 exhibits kinome selectivity Kd of 1.2 μM, 0.29 μM, 0.046 μM, 0.061 μM, 0.18 μM, 0.38 μM, 1.3 μM, 0.42 μM, 0.22 μM, 2.8 μM against ABL1-nonphosphorylated, AURKA, CSF1R, DCAMKL1 (DCLK1), ERK5 (MAPK7), FGFR1, JAK3 (JH1domain-catalytic), KIT, LRRK2, MEK5 (MAP2K5)[1].

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

ERK5-IN-4 相关抗体:

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3 μM
Incubation Time: 1 h
Result: Resulted upper phospho-ERK5 band with EGF stimulation and inhibition.
体内研究
(In Vivo)

ERK5-IN-4 (compound 34b) (p.o.; 10 mg/kg) has low clearance and an oral bioavailability of 42% in the mouse[1].

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

Animal Model: Pharmacokinetic Parameters for ERK5-IN-4[1]
Dosage:
Administration:
Result:
Route Dose (mg/kg) Cl (mL/min/kg) Vd (L/kg) t1/2 (min) BA (%)
i.v. or p.o. 10 14 0.6 80 42
分子量

381.19

Formula

C16H11Cl2FN4O2
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

ERK5-IN-4 相关分类

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  • 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:

ERK5-IN-41888305-17-6ERKExtracellular signal regulated kinasesHEK293HeLaextracellular signal-relatedkinaseERK5 ΔTADpharmacokineticInhibitorinhibitorinhibit

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