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化学和生化试剂
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蒽[1,9-cd]吡唑-6(2H)-酮, 丝裂原活化蛋白激酶 10 抑制剂；丝裂原活化蛋白激酶 8 抑制剂；丝裂原活化蛋白激酶 9 抑制剂

蒽[1,9-cd]吡唑-6(2H)-酮, 丝裂原活化蛋白激酶 10 抑制剂；丝裂原活化蛋白激酶 8 抑制剂；丝裂原活化蛋白激酶 9 抑制剂

JNK抑制剂

7篇引用文献

Moligand™

≥98%

CAS编号: 129-56-6
分子式: C₁₄H₈N₂O
分子量: 220.233
MDL号: MFCD00022289
PubChem编号: 8515
PubChem SID: 504751698

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货号 (SKU)	包装规格	是否现货
S125267-25mg	25mg	现货
S125267-50mg	50mg	现货
S125267-100mg	100mg	现货
S125267-500mg	500mg	现货
S125267-1g	1g	现货
S125267-5g	5g	现货

查看相关系列

Apoptosis (1467) Autophagy (555) Ferroptosis (208) JNK (62) MAPK/ERK Pathway (546) mitogen-activated protein kinase 10 Inhibitor (14) mitogen-activated protein kinase 8 Inhibitor (13) mitogen-activated protein kinase 9 Inhibitor (10)

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基本描述

别名	吡唑蒽酮
英文别名	HMS1362F07 \| KBioGR_000406 \| Anthra[1-9-cd]pyrazol-6(2H)-one \| SDCCGSBI-0050458.P003 \| WLN: T C66651A P IV OMNJ \| Pyrazolanthrone \| Pyrazoleanthrone \| HMS3295M01 \| 2,6-dihydrodibenzo[cd,g]indazol-6-one \| JMC517015 Compound 2 \| Bio1_001313 \| NCGC00015958-0
规格或纯度	Moligand™, ≥98%
英文名称	SP600125
生化机理	SP600125 是一种 c-Jun N 端激酶（JNK）选择性抑制剂。SP600125 对 JNK1、2 和 3 具有竞争性和可逆性抑制作用（IC50 = 40 - 90 nM），对 ERK2、p38β 和一系列酶的活性可忽略不计（IC50 > 10 μM）。体内活性。在某些条件下对其他蛋白激酶的选择性降低。保护肾小管上皮细胞免受缺血/再灌注诱导的细胞凋亡。强效、选择性的 JNK1、-2 和 -3 抑制剂（IC50 = 0.11 μM）。SP600125 是一种可逆的 ATP 竞争性抑制剂，对一系列激酶的选择性大于 20 倍。它能剂量依赖性地抑制 c-Jun 的磷酸化和炎症-3 的表达。
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
作用类型	抑制剂
作用机制	丝裂原活化蛋白激酶 10 抑制剂；丝裂原活化蛋白激酶 8 抑制剂；丝裂原活化蛋白激酶 9 抑制剂
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

关联靶点（人）

MAPK10 Tchem 丝裂原活化蛋白激酶10(Mitogen-activated protein kinase 10) (2 活性数据)

点击查看靶蛋白信息： MAPK10

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

MAPK8 Tchem 丝裂原活化蛋白激酶 8(Mitogen-activated protein kinase 8) (1 活性数据)

点击查看靶蛋白信息： MAPK8

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

MAPK9 Tchem 丝裂原活化蛋白激酶9(Mitogen-activated protein kinase 9) (1 活性数据)

点击查看靶蛋白信息： MAPK9

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

名称和识别符

PubChem SID	504751698
分子类型	小分子
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
Isomeric 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
分子量	220.230 g/mol
XLogP3	2.700
氢键供体数Hydrogen Bond Donor Count	1
氢键受体数Hydrogen Bond Acceptor Count	2
可旋转键计数Rotatable Bond Count	0
精确质量Exact Mass	220.064 Da
单同位素质量Monoisotopic Mass	220.064 Da
拓扑极表面积Topological Polar Surface Area	45.800 Å²
重原子数Heavy Atom Count	17
形式电荷Formal Charge	0
复杂度Complexity	343.000
同位素原子数Isotope Atom Count	0
定义的原子立体中心计数Defined Atom Stereocenter Count	0
未定义的原子立体中心计数Undefined Atom Stereocenter Count	0
定义的键立体中心计数Defined Bond Stereocenter Count	0
未定义的键立体中心计数Undefined Bond Stereocenter Count	0
所有立体化学键的总数The total count of all stereochemical bonds	0
共价键合单元计数Covalently-Bonded Unit Count	1

安全和危险性（GHS）

象形图	GHS07
信号词	Warning
危险声明	H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激
预防措施声明	P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染：用水充分清洗。 P321: 特殊处理（请参阅此标签上的...）。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P271: 仅在室外或通风良好的地方使用。 P304+P340: 如误吸入：将人转移到空气新鲜处，保持呼吸舒适体位。 P403+P233: 存放在通风良好的地方。保持容器密闭。 P362+P364: 脱掉沾污的衣服，清洗后方可重新使用。 P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。 P337+P317: 如果眼睛刺激持续：寻求医疗帮助。 P332+P317: 如果出现皮肤刺激：请寻求医疗帮助。 P319: 如果你感到不适，请寻求医疗帮助。

SDS英文版

质量标准

Purity(HPLC)	98-100（%）
Appearance（S125267)	yellow solid
Infrared spectrum	Conforms to Structure
Proton NMR spectrum	Conforms to Structure

质量标准

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找到8个结果

批号(Lot Number)	证书类型	日期	货号
L1805123	分析证书	24-05-14	S125267
L1805121	分析证书	24-05-14	S125267
A2509321	分析证书	24-04-13	S125267
F2209263	分析证书	24-03-20	S125267
F2209277	分析证书	24-03-20	S125267
F2209285	分析证书	24-03-20	S125267
A2506223	分析证书	24-03-20	S125267
A2125110	分析证书	22-11-16	S125267

此产品的引用文献

如何在您的发表作品中引用阿拉丁的产品和网站?

1. Lin Zhao, Liyuan Wang, Han Wang, Tao Xi, Sijia Liu, Yang Li, Jianping Ruan, Yongqing Huang. (2023) Endoplasmic reticulum chaperone GRP78 participates in fluoride-induced autophagy in LS8 cells by regulating the IRE1-TRAF2-JNK pathway. ENVIRONMENTAL TOXICOLOGY, 38 (7): (1756-1767). [PMID:37070943] [10.1002/tox.23805]
2. Niu Ting, Wei Zhiying, Fu Jiao, Chen Shu, Wang Ru, Wang Yuya, Zheng Ruihe. (2023) Venlafaxine, an anti-depressant drug, induces apoptosis in MV3 human melanoma cells through JNK1/2-Nur77 signaling pathway. Frontiers in Pharmacology, 13 [PMID:36686679] [10.3389/fphar.2022.1080412]
3. Xing Ying, Liu Yang, Qi Zhong, Liu Zhengrong, Wang Xin, Zhang Hongyi. (2021) LAGE3 promoted cell proliferation, migration, and invasion and inhibited cell apoptosis of hepatocellular carcinoma by facilitating the JNK and ERK signaling pathway. CELLULAR & MOLECULAR BIOLOGY LETTERS, 26 (1): (1-16). [PMID:34837962] [10.1186/s11658-021-00295-4]
4. Bai Yu, Du Qiang, Zhang Le, Li Ling, Wang Nana, Wu Bo, Li Ping, Li Ling. (2021) Silencing of ANGPTL8 Alleviates Insulin Resistance in Trophoblast Cells. Frontiers in Endocrinology, 12 (597). [PMID:34163433] [10.3389/fendo.2021.635321]
5. Zhaohui Shi, Min Xu, Xiaodong Chen, Jian Wang, Tianfeng Zhao, Dingjun Zha. (2021) The regulatory role of SFRP5/WNT5A axis in allergic rhinitis through inhibiting JNK pathway activation and lowering mucin generation in human nasal epithelial cells. EXPERIMENTAL AND MOLECULAR PATHOLOGY, 118 (104591). [PMID:33285209] [10.1016/j.yexmp.2020.104591]
6. Tian Xusheng, Zhang Yukun, Li Han, Li Yunfeng, Wang Ning, Zhang Wei, Ma Boyan. (2020) Palmatine ameliorates high fat diet induced impaired glucose tolerance. BIOLOGICAL RESEARCH, 53 (1): (1-12). [PMID:32928312] [10.1186/s40659-020-00308-0]
7. Kang An, Yuehan Zhang, Yingjiao Liu, Shengxi Yan, Zhaowei Hou, Meng Cao, Guangkuo Liu, Congcong Dong, Juncha Gao, Gaifang Liu. (2020) Neferine induces apoptosis by modulating the ROS‑mediated JNK pathway in esophageal squamous cell carcinoma. ONCOLOGY REPORTS, 44 (3): (1116-1126). [PMID:32705225] [10.3892/or.2020.7675]

参考文献

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43. Niu Ting, Wei Zhiying, Fu Jiao, Chen Shu, Wang Ru, Wang Yuya, Zheng Ruihe. (2023) Venlafaxine, an anti-depressant drug, induces apoptosis in MV3 human melanoma cells through JNK1/2-Nur77 signaling pathway. Frontiers in Pharmacology, 13 [PMID:36686679] [10.3389/fphar.2022.1080412]
44. Xing Ying, Liu Yang, Qi Zhong, Liu Zhengrong, Wang Xin, Zhang Hongyi. (2021) LAGE3 promoted cell proliferation, migration, and invasion and inhibited cell apoptosis of hepatocellular carcinoma by facilitating the JNK and ERK signaling pathway. CELLULAR & MOLECULAR BIOLOGY LETTERS, 26 (1): (1-16). [PMID:34837962] [10.1186/s11658-021-00295-4]
45. Bai Yu, Du Qiang, Zhang Le, Li Ling, Wang Nana, Wu Bo, Li Ping, Li Ling. (2021) Silencing of ANGPTL8 Alleviates Insulin Resistance in Trophoblast Cells. Frontiers in Endocrinology, 12 (597). [PMID:34163433] [10.3389/fendo.2021.635321]
46. Zhaohui Shi, Min Xu, Xiaodong Chen, Jian Wang, Tianfeng Zhao, Dingjun Zha. (2021) The regulatory role of SFRP5/WNT5A axis in allergic rhinitis through inhibiting JNK pathway activation and lowering mucin generation in human nasal epithelial cells. EXPERIMENTAL AND MOLECULAR PATHOLOGY, 118 (104591). [PMID:33285209] [10.1016/j.yexmp.2020.104591]
47. Tian Xusheng, Zhang Yukun, Li Han, Li Yunfeng, Wang Ning, Zhang Wei, Ma Boyan. (2020) Palmatine ameliorates high fat diet induced impaired glucose tolerance. BIOLOGICAL RESEARCH, 53 (1): (1-12). [PMID:32928312] [10.1186/s40659-020-00308-0]
48. Kang An, Yuehan Zhang, Yingjiao Liu, Shengxi Yan, Zhaowei Hou, Meng Cao, Guangkuo Liu, Congcong Dong, Juncha Gao, Gaifang Liu. (2020) Neferine induces apoptosis by modulating the ROS‑mediated JNK pathway in esophageal squamous cell carcinoma. ONCOLOGY REPORTS, 44 (3): (1116-1126). [PMID:32705225] [10.3892/or.2020.7675]

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