货号:A248150 同义名: RWJ 64809;Adezmapimod
SB-203580 (Adezmapimod) is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM.
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产品名称 | p38 MAPK ↓ ↑ | p38α ↓ ↑ | p38β ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
BMS-582949 |
+++
p38 MAPK, IC50: 13 nM |
98% | |||||||||||||||||
SB 203580 | 99%+ | ||||||||||||||||||
Pexmetinib | ✔ | Tie-2 | 99%+ | ||||||||||||||||
Skepinone-L |
++++
p38α, IC50: 5 nM |
98% | |||||||||||||||||
Doramapimod |
++++
p38α, Kd: 0.1 nM p38α, IC50: 38 nM |
99%+ | |||||||||||||||||
VX-702 | 99%+ | ||||||||||||||||||
Ralimetinib dimesylate |
++++
p38α, IC50: 7 nM |
98% | |||||||||||||||||
SB 202190 |
++
p38α, IC50: 50 nM |
++
p38β, IC50: 100 nM |
99%+ | ||||||||||||||||
Losmapimod |
++++
p38α, pKi: 8.1 |
+++
p38β, pKi: 7.6 |
99%+ | ||||||||||||||||
Neflamapimod |
+++
p38α, IC50: 10 nM |
+
p38β, IC50: 220 nM |
99%+ | ||||||||||||||||
PH-797804 |
++
p38α, IC50: 26 nM |
+
p38β, IC50: 102 nM |
98% | ||||||||||||||||
TAK-715 |
++++
p38α, IC50: 7.1 nM |
+
p38β, IC50: 0.20 μM |
99%+ | ||||||||||||||||
SB 239063 |
++
p38α, IC50: 44 nM |
++
p38β, IC50: 44 nM |
99%+ | ||||||||||||||||
Pamapimod |
+++
p38α, IC50: 0.014 μM |
+
p38β, IC50: 0.48 μM |
98%+ | ||||||||||||||||
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。 |
产品名称 | Akt ↓ ↑ | Akt1 ↓ ↑ | Akt2 ↓ ↑ | Akt3 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Honokiol | ✔ | MEK | 98% | ||||||||||||||||
PF-04691502 |
++++
P-Akt (S473), IC50: 3.8 nM P-Akt (T308), IC50: 7.5 nM |
98+% | |||||||||||||||||
PHT-427 |
+
Akt, Ki: 2.7 μM |
99%+ | |||||||||||||||||
Deguelin | ✔ | PI3K | 99%+ | ||||||||||||||||
TIC10 isomer | ✔ | ERK | 98+% | ||||||||||||||||
Perifosine |
+
Akt, IC50: 4.7 μM |
98% | |||||||||||||||||
Miltefosine | ✔ | PI3K,PKC | 98% | ||||||||||||||||
Triciribine |
+
Akt, IC50: 130 nM |
99%+ | |||||||||||||||||
Uprosertib |
+
Akt1, IC50: 180 nM |
+
Akt2, IC50: 328 nM |
++
Akt3, IC50: 38 nM |
99%+ | |||||||||||||||
Afuresertib |
++++
Akt1, Ki: 0.08 nM |
++++
Akt2, Ki: 2 nM |
++++
Akt3, Ki: 2.6 nM |
99%+ | |||||||||||||||
Miransertib |
++++
Akt1, IC50: 5 nM |
++++
Akt2, IC50: 4.5 nM |
++
Akt3, IC50: 16 nM |
98+% | |||||||||||||||
GSK-690693 |
++++
Akt1, IC50: 2 nM |
+++
Akt2, IC50: 13 nM |
+++
Akt3, IC50: 9 nM |
99%+ | |||||||||||||||
AT7867 |
++
Akt1, IC50: 32 nM |
++
Akt2, IC50: 17 nM |
++
Akt3, IC50: 47 nM |
PKA | 99%+ | ||||||||||||||
AKT inhibitor VIII |
++
Akt1, IC50: 58 nM |
+
Akt2, IC50: 210 nM |
+
Akt3, IC50: 2119 nM |
98+% | |||||||||||||||
MK-2206 2HCl |
+++
Akt1, IC50: 8 nM |
+++
Akt2, IC50: 12 nM |
+
Akt3, IC50: 65 nM |
99%+ | |||||||||||||||
Ipatasertib |
++++
Akt1, IC50: 5 nM |
++
Akt2, IC50: 18 nM |
+++
Akt3, IC50: 8 nM |
99%+ | |||||||||||||||
AT13148 |
++
Akt1, IC50: 38 nM |
+
Akt2, IC50: 402 nM |
++
Akt3, IC50: 50 nM |
PKA | 98+% | ||||||||||||||
Capivasertib |
++++
Akt1, IC50: 3 nM |
+++
Akt2, IC50: 8 nM |
+++
Akt3, IC50: 8 nM |
99%+ | |||||||||||||||
A-674563 HCl |
+++
Akt1, Ki: 11 nM |
PKA | 98% | ||||||||||||||||
CCT128930 |
+++
Akt2, IC50: 6 nM |
PKA | 98+% | ||||||||||||||||
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 | The stress-activated protein kinase (SAPK) p38 isoforms are mitogen-activated protein kinase (MAPK) family members. MAPKs act as an integration point for multiple biochemical signals, and are involved in a wide variety of cellular processes such as proliferation, differentiation, transcription regulation and development. SB 203580 is a p38 MAPK inhibitor. SB 203580 inhibited the ATPase activity of non-phosphorylated p38 MAPK with a Km of 9.6 mM. SB 203580 was competitive with ATP with a Ki of 21 nM, detected in a kinetic study of yeast expressed active p38 MAPK[3]. 24h treatment of SB 203580 dose-dependently inhibited IL-1β-induced PGE2 release with an EC50 of 0.18 μM[4]. SB 203580 was dissolved in drinking water at the concentration of 250 μM and orally administrated 0.4 ml/day to MRL/lpr mice aged from 14 to 22 weeks. SB203580 improved renal function by decreasing the levels of proteinuria and serum BUN, ameliorating the pathologic changes of kidney and reducing Ig and C3 depositions in the kidney. Moreover, hepatocytes necrosis, recruitment and proliferation of leucocytes in liver and spleen were found to be inhibited by administration of SB203580[5]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
HCA2 | 2.5 μM | Function Assay | Inhibits p38 mediated MK2 activation | 17964780 | |
Hela | Function Assay | Inhibits Tat-induced HIV1 LTR transactivation in human HeLa cells with IC50 of 0.1 μM | 18926711 | ||
hESCs | 5 μM | Growth Inhibition Assay | Induces cardiomyogenic activity assessed as cell growth | 23602399 | |
IEC-18 | 10 μM | Function Assay | Inhibits LPS-induced p38 MAPK phosphorylation | 23758110 | |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.65mL 0.53mL 0.26mL |
13.25mL 2.65mL 1.32mL |
26.49mL 5.30mL 2.65mL |
CAS号 | 152121-47-6 |
分子式 | C21H16FN3OS |
分子量 | 377.435 |
别名 | RWJ 64809;Adezmapimod;SB203850;PB 203580 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
溶解度 |
DMSO: 18 mg/mL(47.69 mM),配合低频超声,并水浴加热至45℃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 |
IP 2% DMSO+2% Tween80+40% PEG300+water 4 mg/mL clear PO 0.5% CMC-Na 60 mg/mL suspension |