2. MAPK/ERK Pathway NF-κB Immunology/Inflammation Metabolic Enzyme/Protease
  3. p38 MAPK Keap1-Nrf2 Reactive Oxygen Species (ROS)
  4. SH494

SH494 是一种 p38 MAPK 抑制剂和 Nrf2 通路激活剂。SH494 可抑制 RANKL 诱导的 p38 磷酸化，破坏与破骨细胞生成相关的 MAPK 级联反应。SH494 能够激活 Nrf2 通路，上调下游靶基因并诱导细胞保护酶的表达。SH494 可减少细胞内 ROS 的积累并使线粒体膜电位 (ΔΨm) 恢复正常。SH494 可降低卵巢切除小鼠的破骨细胞活性并缓解其骨质疏松症状。SH494 可用于骨质疏松症的研究。

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SH494

SH494 Chemical Structure

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SH494 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 Akt1 p38α p38β MAPK13 p38δ p38γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SH494 is a p38 MAPK inhibitor and Nrf2 pathway activator. SH494 inhibits RANKL-induced phosphorylation of p38 and disrupts the MAPK cascade associated with osteoclastogenesis. SH494 activates the Nrf2 pathway, upregulates downstream target genes and induces the expression of cytoprotective enzymes. SH494 reduces intracellular ROS accumulation and restores mitochondrial membrane potential (ΔΨm) to normal. SH494 decreases osteoclast activity and alleviates osteoporosis symptoms in ovariectomized mice. SH494 can be used for research on osteoporosis[1].

体外研究
(In Vitro)

SH494 (0.01-1 μM; 7 days) 可强效抑制 RANKL 诱导的小鼠骨髓巨噬细胞 (BMMs) 破骨细胞分化，其 IC50 为 8.4 nM，在浓度≥0.1 μM、作用 7 天的条件下可实现完全抑制[1]。
SH494 (0.01-1 μM; 7 days) 呈剂量依赖性抑制 RANKL 诱导的小鼠骨髓巨噬细胞 (BMMs) 中 F-肌动蛋白环的形成[1]。
SH494 (0.01-1 μM; 1-5 days) 可呈剂量依赖性和时间依赖性下调经 RANKL 和 M-CSF 处理的小鼠骨髓巨噬细胞 (BMMs) 中破骨细胞生成关键基因的 mRNA 表达[1]。
SH494 (0.01-1 μM; 72 h) 可剂量依赖性地抑制小鼠骨髓巨噬细胞 (BMMs) 中关键破骨细胞生成标志物 (c-Fos、Ctsk、Mmp9) 的蛋白表达[1]。
SH494 (1 μM; 5-30 min) 可在 RANKL 刺激后 5、10 和 30 min 时抑制小鼠骨髓巨噬细胞 (BMMs) 中由 RANKL 诱导的 p38 MAPK 磷酸化[1]。
SH494 (0.01-1 μM; 48-72 h) 可降低 RANKL 诱导的小鼠骨髓巨噬细胞 (BMMs) 内 ROS 积累，并在 48 h 后恢复其线粒体膜电位；同时通过上调 Cat、Gclc 和 HO-1 的表达，以及增加 Nrf2 的核定位来激活 Nrf2 通路[1]。

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

SH494 相关抗体:

Real Time qPCR[1]

Cell Line: mouse bone marrow-derived macrophages (BMMs)
Concentration: 0.01 μM (48 h), 0.1 μM (48 h), 1 μM (48 h; 1, 3, 5 days)
Incubation Time: 48 h (concentration-dependent analysis); 1, 3, 5 days (time course with 1 μM SH494)
Result: Dose-dependently downregulated the mRNA expression of key osteoclastogenic markers: Nfatc1, Trap, Ctsk, Mmp9, and c-Fos after 48 h.
Over a 5-day time course, 1 μM SH494 abrogated RANKL-induced upregulation of Nfatc1, Trap, Ctsk, and c-Fos throughout differentiation.

Western Blot Analysis[1]

Cell Line: mouse bone marrow-derived macrophages (BMMs)
Concentration: 0.01 μM, 0.1 μM, 1 μM
Incubation Time: 72 h
Result: Dose-dependently reduced the protein levels of c-Fos, Ctsk, and Mmp9 in RANKL-stimulated BMMs.

Western Blot Analysis[1]

Cell Line: mouse bone marrow-derived macrophages (BMMs)
Concentration: 1 μM
Incubation Time: pretreated, then incubated with RANKL for 5, 10, 30 min
Result: Markedly inhibited RANKL-induced phosphorylation of p38 at all tested time points.
药代动力学
(Parmacokinetics)
Species Dose Route Tmax Cmax AUC0-t AUC0-∞ Vz CL T1/2 F
Mice[1] 1.0 mg/kg i.v. 0.083 h 1093 ng/mL 396 ng·h/mL 399 ng·h/mL 674 mL/kg 42 mL/min/kg 0.32 h /
Mice[1] 10.0 mg/kg p.o. 0.333 h 1162 ng/mL 1061 ng·h/mL 1067 ng·h/mL / / 0.66 h 26.8 %
体内研究
(In Vivo)

SH494 (1-5 mg/kg；腹腔注射；每日一次；6 周) 可呈剂量依赖性地预防小鼠去卵巢诱导的骨丢失[1]。

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

Animal Model: C57BL/6 (8-week-old female; osteoporosis induced by bilateral ovariectomy)[1]
Dosage: 1 mg/kg; 5 mg/kg
Administration: i.p.; once daily; 6 weeks
Result: Increased bone volume fraction (BV/TV) by 40.66%, trabecular number (Tb.N) by 28.35%, and bone surface density (BS/TV) by 33.43% relative to vehicle-treated OVX mice at 5 mg/kg.
Dose-dependently prevented OVX-induced bone microstructural deterioration, with the 5 mg/kg dose showing improvement in Tb.N and BS/TV comparable to positive control teriparatide.
Preserved trabecular architecture and reduced osteoclast numbers in treated groups.
Showed no systemic or organ-specific toxicity, with stable body weights and normal histology of major organs.
分子量

494.63

Formula

C31H34N4O2
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

SH494 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:

SH494SH 494SH-494p38 MAPKKeap1-Nrf2Reactive Oxygen Species (ROS)TraposteoclastogenesisNfatc1CtskRANKLc-FosNrf2 pathwayMmp9mouse BMMsInhibitorinhibitorinhibit

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