2. MAPK/ERK Pathway
  3. p38 MAPK
  4. (R)-STU104

(R)-STU104 是一种有效且具有口服活性的 TAK1 与 MKK3 蛋白质互作抑制剂，对 TNF-α 和 MKK3 磷酸化的 IC50 分别为 0.58 μM 和 4.0 μM。(R)-STU104 通过与 MKK3 结合，阻断 TAK1 磷酸化 MKK3，抑制 TAK1/MKK3/p38/MnK1/MK2/elF4E 信号通路。(R)-STU104 可用于溃疡性结肠炎的研究。

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(R)-STU104 Chemical Structure

(R)-STU104 Chemical Structure

CAS No. : 2767124-77-4

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(R)-STU104 相关抗体

Top Publications Citing Use of Products

查看 p38 MAPK 亚型特异性产品:

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

(R)-STU104 is a potent and orally active TAK1-MKK3 interaction inhibitor with IC50s of 0.58 μM and 4.0 μM for TNF-α and MKK3 phosphorylation. (R)-STU104 suppresses the TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathways through binding with MKK3 and disrupting the TAK1 phosphorylating MKK3. (R)-STU104 can be used for researching ulcerative colitis[1].

IC50 & Target

IC50: 0.58 μM (TNF-α), 4.0 μM (MKK3 phosphorylation)[1]
体外研究
(In Vitro)

(R)-STU104 attenuates phosphorylation levels of Mnk1, MK2, and elF4E, leading to the downregulation of TNF-α expression and production[1].

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

(R)-STU104 相关抗体:
体内研究
(In Vivo)

(R)-STU104 (1, 3 and 10 mg/kg; IG for 7 days) ameliorates the symptoms of DSS-induced experimental colitis in mice, and significantly inhibits inflammatory cytokine protein[1].
Pharmacokinetic Parameters of (R)-STU104 in male C57 mice[1].

IV (5 mg/kg) PO (30 mg/kg)
Tmax (h) 0.083
AUC0-t (μg/L·h) 7249 9895
AUC0-∞ (μg/L·h) 8635 16991
MRT0-∞ (h) 7.32 12.52
Cmax (ng/mL) 2920 2290
t1/2 (ng/mL) 9.29 8.67
VZ (L/kg) 7.76 3.68
CLZ (ng/mL) 0.58 0.29
F (%) 33%

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

Animal Model: C57BL/6 mice (dextran sodium sulfate (DSS)-induced acute ulcerative colitis)[1]
Dosage: 1, 3 and 10 mg/kg
Administration: IG, for 7 days
Result: Ameliorated the symptoms of DSS-induced experimental colitis, and significantly inhibited inflammatory cytokine protein TNF-α, IL-1β, IL-6, and IL-23.
分子量

298.33

Formula

C18H18O4
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

(R)-STU104 相关分类

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  • 稀释计算器

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  • 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:

(R)-STU1042767124-77-4p38 MAPKTAK1MKK3TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathwaysulcerative colitisdextran sodium sulfateInhibitorinhibitorinhibit

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产品名称：
(R)-STU104
目录号：
HY-150612
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