SP600125 

SP600125 (GMP) is SP600125 (HY-12041) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC₅₀s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 induces the transformation of bladder cancer cells from autophagy to apoptosis^[1][2][3].

SP600125 (GMP) 是 JNK2 的 ATP 竞争性抑制剂，K_i 值为 0.19 μM。SP600125 (GMP) 在 Jurkat T 细胞中抑制 c-Jun 的磷酸化，IC₅₀ 为 5 μM 至 10 μM。在 CD4⁺ 细胞中，例如从人脐带血或外周血中分离的 Th0 细胞，SP600125 (GMP) 阻断细胞活化和分化并抑制炎症基因 COX-2、IL-2、IL-10、IFN-γ 和 TNF-α，IC₅₀ 为 5 μM 至 12 μM^[1]。
在小鼠 β 细胞 MIN6 中，SP600125 (GMP) (20 μM) 诱导 p38 MAPK 的磷酸化及其下游 CREB 依赖性启动子激活^[2]。
在 HCT116 细胞中，SP600125 (GMP) (20 μM) 阻断 G2 期到有丝分裂的转变并诱导核内复制。SP600125 (GMP) 的这种能力独立于 JNK 抑制，但由于其抑制 Aurora A 和 Polo 样激酶 1 上游的 CDK1-细胞周期蛋白 B 激活^[3]。

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

SP600125 (GMP) (15 mg/kg 或 30 mg/kg；静脉注射) 显著抑制 TNF-α 血清水平，而 30 mg/kg 口服施用后，则剂量依赖性地阻断 TNF-α 表达^[1]。
SP600125 (GMP) 在大鼠体内减轻 LPS 诱导的 ALI。SP600125 (GMP) 组大鼠 BALF 中 TNF-α和 IL-6 的表达水平显著降低^[4]。

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

220.23

C₁₄H₈N₂O

129-56-6

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Bennett BL, et al. SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase. Proc Natl Acad Sci U S A, 2001, 98(24), 13681-13686.  [Content Brief]

  [2]. Vaishnav D, et al. SP600125, an inhibitor of c-jun N-terminal kinase, activates CREB by a p38 MAPK-mediated pathway. Biochem Biophys Res Commun, 2003, 307(4), 855-860.  [Content Brief]

  [3]. Kim JA, et al. SP600125 suppresses Cdk1 and induces endoreplication directly from G2 phase, independent of JNK inhibition. Oncogene, 2010, 29(11), 1702-1716.  [Content Brief]

  [4]. Zheng Y, et al. JNK inhibitor SP600125 protects against lipopolysaccharide-induced acute lung injury via upregulation ofclaudin-4. Exp Ther Med. 2014 Jul;8(1):153-158.  [Content Brief]