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蒽[1,9-cd]吡唑-6(2H)-酮

JNK抑制剂
规格或纯度: ≥98%
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货号 (SKU) 包装规格 是否现货 价格 数量
S125267-25mg
 25mg 现货 Stock Image
S125267-100mg
 100mg 现货 Stock Image
S125267-500mg
 500mg 现货 Stock Image
S125267-1g
 1g 现货 Stock Image
S125267-5g
 5g 现货 Stock Image
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mitogen-activated protein kinase 10 Inhibitor mitogen-activated protein kinase 8 Inhibitor mitogen-activated protein kinase 9 Inhibitor
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基本描述

规格或纯度 ≥98%
英文名称 SP600125
别名 吡唑蒽酮
英文别名 129-56-6|1,9-Pyrazoloanthrone|SP600125|Pyrazolanthrone|Dibenzo[cd,g]indazol-6(2H)-one|Pyrazoleanthrone|SP 600125|Anthra[1,9-cd]pyrazol-6(2H)-one|SP-600125|JNK Inhibitor II|Anthra-1,9-pyrazol-6-none|ANTHRA(1,9-cd)PYRAZOL-6(2H)-ONE|C.I. 70300|2H-Dibenzo[cd,
生化机理 SP600125 is selective inhibitor of c-Jun N-terminal kinase (JNK). SP600125 competitively and reversibly inhibits JNK1, 2 and 3 (IC50 = 40 - 90 nM) with negligible activity at ERK2, p38β and a range of enzymes (IC50 > 10 μM). Active in vivo. Shown to have reduced selectivity over other protein kinases under certain conditions. Protects renal tubular epithelial cells against ischemia/reperfusion-induced apoptosis.Potent and selective JNK1, -2, and -3 inhibitor (IC 50 = 0.11 μM). SP600125 is a reversible ATP-competitive inhibitor with >20-fold selectivity over a range of kinases. It dose-dependently inhibits the phosphorylation of c-Jun and the expression of inflam
应用 A potent, selective and reversible inhibitor of JNK1, JNK-2, and JNK-3
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍

SP600125是泛JNK抑制剂，对JNK1，JNK2和JNK3的IC50分别为40 nM，40 nM和90 nM，比对MKK4和MKK3，MKK6，PKB，PKCα的抑制性高10倍和超过25倍。A potent, selective and reversible inhibitor of JNK1, JNK-2, and JNK-3

SP600125 is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc.
A potent, selective and reversible inhibitor of JNK1, JNK-2, and JNK-3

名称和标识符

IUPAC Name 14,15-diazatetracyclo[7.6.1.02,7.013,16]hexadeca-1(15),2,4,6,9(16),10,12-heptaen-8-one
INCHI InChI=1S/C14H8N2O/c17-14-9-5-2-1-4-8(9)13-12-10(14)6-3-7-11(12)15-16-13/h1-7H,(H,15,16)
InChi Key ACPOUJIDANTYHO-UHFFFAOYSA-N
Canonical SMILES C1=CC=C2C(=C1)C3=NNC4=CC=CC(=C43)C2=O
PubChem CID 8515
分子量 220.233

化学和物理性质

溶解性 DMSO ≥42mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL
敏感性 对热敏感
熔点 283°C

安全和危险性（GHS）

象形图
ghs07

Harmful
信号词 Warning
危险声明 H315: Causes skin irritation
H319: Causes serious eye irritation
H335: May cause respiratory irritation
预防措施声明 P261,P305+P351+P338,P280,P302+P352,P321,P405,P501,P264,P271,P304+P340,P403+P233,P362+P364,P264+P265,P337+P317,P332+P317,P319

关联配体

Ligand ID 5273
名称 SP600125
别名 1,9-pyrazoloanthrone
类别 Synthetic organic
学名 4-amino-N-(4,6-dimethylpyrimidin-2-yl)benzenesulfonamide
生物活性评价 The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价 SP600125 is an ATP-competitive, pan JNK inhibitor with potent activity against JNK1, JNK2 and JNK3 . Off targets including the aryl hydrocarbon receptor (AhR; agonist) , Mps1 (TTK, a tyrosine, serine and threonine kinase) , and some serine/threonine kinases (Aurora kinase A, FLT3, MELK, and TRKA) have been identified.

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参考文献

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