2. MAPK/ERK Pathway TGF-beta/Smad Stem Cell/Wnt Cytoskeleton
  3. JNK TGF-beta/Smad Cadherin
  4. JNK3-IN-10

JNK3-IN-10 是一种不可透过血脑屏障的 JNK3 抑制剂 (IC50=0.257 nM)，对 JNK1 的选择性超过 400 倍。JNK3-IN-10 可阻断 TGF-β1 下游的 JNK3 介导信号通路，抑制 TGF-β1 诱导的 c-Jun 磷酸化，减少促纤维化标志物的表达，并可恢复上皮蛋白 E-钙粘蛋白 (E-cadherin) 的表达。JNK3-IN-10 具有低细胞毒性、抗纤维化、细胞保护和肾脏保护作用，可缓解白蛋白尿、肾小球硬化和足细胞足突融合。JNK3-IN-10 可用于慢性肾脏病、肾小球硬化、阿霉素诱导的肾病的研究。

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JNK3-IN-10

JNK3-IN-10 Chemical Structure

CAS No. : 3085181-00-3

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JNK3-IN-10 相关抗体

Top Publications Citing Use of Products

查看 JNK 亚型特异性产品:

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JNK1 JNK2 JNK3 JNK

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JNK3-IN-10 is a blood-brain barrier-impermeable JNK3 inhibitor (IC50=0.257 nM) with over 400-fold selectivity over JNK1. JNK3-IN-10 blocks the JNK3-mediated signaling pathway downstream of TGF-β1, inhibits TGF-β1-induced phosphorylation of c-Jun, reduces the expression of pro-fibrotic markers, and restores the expression of the epithelial protein E-cadherin. JNK3-IN-10 exhibits low cytotoxicity, anti-fibrotic, cytoprotective and renoprotective effects, and alleviates albuminuria, glomerulosclerosis and podocyte foot process fusion. JNK3-IN-10 can be used for the research of chronic kidney disease, glomerulosclerosis and adriamycin-induced nephropathy[1].

IC50 & Target[1]

hJNK3

0.257 nM (IC50)

体外研究
(In Vitro)

JNK3-IN-10 (Compound 14bg) (1 μM; 预孵育 20 min, 与 ATP 共孵育 2 h) 对 JNK1、JNK2 和 p38α 的选择性分别为 84 倍、472 倍和 194 倍，且在 1 μM 浓度下的脱靶激酶活性极低[1]。
JNK3-IN-10 (1 μM; 30 min; 37 °C) 在人肝微粒体中表现出中等微粒体稳定性，37 °C 孵育 30 分钟后仍有 64.63% 的残留[1]。
JNK3-IN-10 具有较低的血脑屏障 (BBB) 通透性，其 Pe 值为 0.52×10-6 cm/s，被归类为 BBB 非通透性化合物[1]。
JNK3-IN-10 (5 μM; 预孵育 1 h) 可抑制 TGF-β1 诱导的分化人足细胞中 c-Jun 磷酸化、促纤维化标志物 (PAI-1、COL1α1) 表达，且不降低细胞活力[1]。

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

JNK3-IN-10 相关抗体:

ELISA Assay[1]

Cell Line: Differentiated human podocytes
Concentration: 5 μM
Incubation Time: 1 h pretreatment
Result: Suppressed TGF-β1-induced phosphorylation of c-Jun.
Showed no cytotoxicity, with cell viability remaining at control levels.

Western Blot Analysis[1]

Cell Line: Differentiated human podocytes
Concentration: 5 μM
Incubation Time: 1 h pretreatment
Result: Attenuated TGF-β1-induced upregulation of PAI-1 and COL1α1.
Restored E-cadherin expression to near-basal levels.
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-t Cmax T1/2 CL Bioavailability
Mice[1] 1 mg/kg i.v. 614 ng·h/mL 1115.01 ng/mL 0.21 h 204 mL/min/kg /
Mice[1] 3 mg/kg p.o. 392 ng·h/mL 378 ng/mL 0.34 h / 21.3 %
Mice[1] 1 mg/kg i.p. 718 ng·h/mL 136 ng/mL 1.14 h 129.63 mL/min/kg /
体内研究
(In Vivo)

JNK3-IN-10 (Compound 14bg) (2-6 mg/kg; i.p.; 每周 3 次; 2 w) 可显著缓解阿霉素 (HY-15142A) 诱导的雄性 BALB/c 小鼠肾损伤、白蛋白尿、肾小球硬化及足细胞损伤，且无全身毒性[1]。

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

Animal Model: BALB/c (male, 8 weeks old, chronic kidney disease induced by single intravenous injection of Adriamycin at 12 mg/kg)[1]
Dosage: 2 mg/kg; 6 mg/kg
Administration: i.p.; three times per week; 2 weeks
Result: Significantly restored serum albumin levels and tended to reduce blood urea nitrogen (BUN) levels compared to untreated Adriamycin-injected mice.
Reduced urinary albumin-to-creatinine ratio, collagen-positive area, and glomerulosclerosis scores.
Decreased podocyte foot process effacement and preserved glomerular basement membrane structure.
Reduced Adriamycin-induced phosphorylation of c-Jun, suppressed upregulation of α-SMA and Col1α1, and partially restored E-cadherin expression in renal cortical tissues.
Downregulated fibrotic (α-SMA, Col1α1) and epithelial-mesenchymal transition-associated transcripts, with a trend toward recovery of podocyte-specific markers (E-cadherin, synaptopodin).
Showed no systemic toxicity.
分子量

559.47

Formula

C24H24Cl2N8O2S
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

JNK3-IN-10 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:

JNK3-IN-103085181-00-3JNKTGF-beta/SmadCadherinc-Jun N-terminal kinaseTransforming growth factor betaJNK3E-cadherinp38αJNK2JNK1adriamycin-induced nephropathyTGF-β1c-Junglomerulosclerosischronic kidney diseaseInhibitorinhibitorinhibit

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