SU3327是一种选择性JNK抑制剂,IC50 为 0.7 μM。SU3327可抑制 JNK 和 JIP 之间的蛋白相互作用,IC50 值为 239 nM 。
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产品名称 | JNK ↓ ↑ | JNK1 ↓ ↑ | JNK2 ↓ ↑ | JNK3 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Mulberroside A | ✔ | 99%+ | |||||||||||||||||
Loureirin B | ✔ | Calcium Channel,Potassium Channel | 99%+ | ||||||||||||||||
Ginsenoside Re | ✔ | NF-κB | 98% | ||||||||||||||||
(+)-(3R,8S)-Falcarindiol | ✔ | STAT,ERK | 99%+ | ||||||||||||||||
trans-Zeatin | ✔ | p38 MAPK,ERK | 95+% | ||||||||||||||||
Urolithin B | ✔ | ERK,NF-κB | 95% | ||||||||||||||||
Cucurbitacin IIb | ✔ | NF-κB | 99% | ||||||||||||||||
Astragaloside IV | ✔ | Akt,mTOR,NF-κB | 98% | ||||||||||||||||
NDMC101 | ✔ | 99%+ | |||||||||||||||||
DB07268 |
++++
JNK1, IC50: 9 nM |
99%+ | |||||||||||||||||
SP600125 |
+
MKK4, IC50: 0.4 μM |
+++
JNK1, IC50: 40 nM |
+++
JNK2, IC50: 40 nM |
+++
JNK3, IC50: 90 nM |
98% | ||||||||||||||
JNK-IN-7 |
++++
JNK1, IC50: 1.5 nM |
++++
JNK2, IC50: 2 nM |
++++
JNK3, IC50: 0.7 nM |
99% | |||||||||||||||
JNK-IN-8 |
++++
JNK1, IC50: 4.7 nM |
+++
JNK2, IC50: 18.7 nM |
++++
JNK3, IC50: 1 nM |
99%+ | |||||||||||||||
3,3',5-Triiodo-L-thyronine |
++
JNK1, Kd: 240 nM |
++
JNK2, Kd: 290 nM |
+++
JNK3, Kd: 66 nM |
98% | |||||||||||||||
IQ-1S free acid |
+
JNK1, IC50: 390 nM |
++
JNK2, IC50: 360 nM |
+++
JNK3, IC50: 87 nM |
99% | |||||||||||||||
BI-78D3 |
++
JNK, IC50: 280 nM |
++
JNK, IC50: 280 nM |
++
JNK, IC50: 280 nM |
++
JNK, IC50: 280 nM |
99%+ | ||||||||||||||
Bentamapimod |
+++
JNK1, IC50: 80 nM |
+++
JNK2, IC50: 90 nM |
++
JNK3, IC50: 230 nM |
98% | |||||||||||||||
Resveratrol |
+
JNK1, IC50: 50 μM |
98% | |||||||||||||||||
Indirubin-3′-oxime | ✔ | 99%+ | |||||||||||||||||
SU3327 |
+
JNK, IC50: 0.7 μM |
+
JNK, IC50: 0.7 μM |
+
JNK, IC50: 0.7 μM |
+
JNK, IC50: 0.7 μM |
99%+ | ||||||||||||||
JNK Inhibitor VIII |
++++
JNK1, Ki: 2 nM JNK1, IC50: 45 nM |
++++
JNK2, IC50: 160 nM JNK2, Ki: 4 nM |
+++
JNK3, Ki: 52 nM |
98% | |||||||||||||||
Doramapimod | ✔ | 99%+ | |||||||||||||||||
RPI-1 | ✔ | 99% | |||||||||||||||||
TCS JNK 5a |
++
JNK2, pIC50: 6.5 |
++
JNK3, pIC50: 6.7 |
98% | ||||||||||||||||
SP 600125, negative control |
+
JNK2, IC50: 18 μM |
+
JNK3, IC50: 24 μM |
97% | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | JNKs (c-Jun N-terminal kinases) belong to mitogen-activated protein kinases' family and become activated by several growth factors, stress, radiation, and other extracellular signals. In turn, JNK activation results in phosphorylation of downstream molecules involved in many normal cellular processes[1]. JNK pathway regulates various physiological processes including inflammatory responses, cell differentiation, cell proliferation, cell death, cell survival and expression of proteins. Deregulation of JNK is linked with various diseases including neurodegenerative disease, autoimmune disease, diabetes, cancer, cardiac hypertrophy and asthma[2]. SU3327 is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. SU3327 also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. SU3327 shows less active against p38α and Akt kinase[3]. SU3327 is able to inhibit TNF-α stimulated phosphorylation of c-Jun in HeLa cells (EC50 = 6.23 μM). SU3327 (25 mg/kg; intraperitoneal injection; male BKS.Cg-+Leprdb/+Leprdb/OlaHsd db/db mice) treatment possesses the ability to restore insulin sensitivity in mice models of diabetes. SU3327 has favorable microsomal and plasma stability (T1/2 = 27 min)[4]. SU3327 (25 nM) pretreatment of human-derived cerebral microvascular endothelial cells (hCMEC/D3) effectively reduces LPS-induced polymorphonuclear leukocytes (PMN) rolling/adhesion to hCMEC/D3, prevents activation of AP-1, and significantly reduces expression of VCAM-1[5]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.83mL 0.77mL 0.38mL |
19.13mL 3.83mL 1.91mL |
38.27mL 7.65mL 3.83mL |
CAS号 | 40045-50-9 |
分子式 | C5H3N5O2S3 |
分子量 | 261.305 |
别名 | Halicin |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
溶解度 |
DMSO: 60 mg/mL(229.62 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |