计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
概述
SB203580是一种p38 MAPK抑制剂，在THP-1细胞中IC50为0.3-0.5 μM，对SAPK3(106T)和SAPK4(106T)选择性低10倍，且阻断PKB磷酸化，IC50为3-5 μMMDCK cells were treated with SB 203580 to study the role of MAPK signaling in inducing hypertonicity of cell membrane and potassium depletion.16 It was used to inhibit MAPK signaling in mouse cortical neurons17 and human hepatocellular carcinoma cell lines.18
Information
In vitro
SB203580 inhibits the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC50 of 3–5 μm. SB203580 also inhibits IL-2-induced p70S6 kinase activation, although the concentration required is slightly higher with an IC50 above 10 μm. SB203580 also inhibits the activity of PDK1 in a dose-dependent manner with an IC50 in the 3–10 μm range. SB203580 inhibits p38-MAPK stimulation of MAPKAPK2 with an IC50 of approximately 0.07 μM, whereas inhibits total SAPK/JNK activity with an IC50 of 3–10 μM. SB203580 at higher concentrations activates the ERK pathway, which subsequently enhances NF-κB transcriptional activity. SB203580 induces autophagy in human hepatocellular carcinoma (HCC) cells.
In vivo
SB203580 protects pig myocardium against ischemic injury in an in vivo model. SB203580 is effective to prevent and treat the disease in MRL/lpr mice model of Systemic lupus erythematosus (SLE).
Cell Data
cell lines：
Concentrations：0–30 μM
Incubation Time：1 hour
Powder Purity:≥99%
规格
英文别名
RWJ 64809, PB 203580
规格或纯度
Moligand™, 10mM in DMSO
英文名称
SB203580
生化机理
SB203580 （RWJ 64809，PB 203580）是一种 p38 MAPK 抑制剂，在 THP-1 细胞中的 IC50 为 0.3-0.5 μM，对 SAPK3(106T) 和 SAPK4(106T) 的敏感性低 10 倍，阻断 PKB 磷酸化的 IC50 为 3-5 μM。SB203580 可诱导有丝分裂和自噬。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
细胞周期蛋白 G 相关激酶抑制剂；丝裂原活化蛋白激酶 11 抑制剂；丝裂原活化蛋白激酶 14 抑制剂
名称和识别符
EC号
688-252-3
分子类型
小分子
Isomeric SMILES
CS(=O)C1=CC=C(C=C1)C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F
PubChem CID
分子量
377.43
高级数据
关联靶点（人）
CYP1A2
Tchem
细胞色素 P450 1A2(Cytochrome P450 1A2)
(1 活性数据)
CYP2C19
Tchem
细胞色素 P450 2C19(Cytochrome P450 2C19)
(2 活性数据)
CYP3A4
Tclin
细胞色素P450 3A4(Cytochrome P450 3A4)
(1 活性数据)
CYP2C9
Tchem
细胞色素 P450 2C9(Cytochrome P450 2C9)
(1 活性数据)
GAK
Tchem
细胞周期蛋白G相关激酶(Cyclin-G-associated kinase)
(3 活性数据)
TBXAS1
Tchem
血栓素A合酶(Thromboxane-A synthase)
(1 活性数据)
RIPK2
Tchem
受体相互作用丝氨酸/苏氨酸蛋白激酶 2(Receptor-interacting serine/threonine-protein kinase 2)
(4 活性数据)
MAPK10
Tchem
丝裂原活化蛋白激酶10(Mitogen-activated protein kinase 10)
(1 活性数据)
ALOX5
Tclin
花生四烯酸5-脂氧合酶(Arachidonate 5-lipoxygenase)
(1 活性数据)
GCGR
Tclin
胰高血糖素受体(Glucagon receptor)
(1 活性数据)
P2RX7
Tchem
P2X嘌呤受体 7(P2X purinoceptor 7)
(1 活性数据)
NLK
Tchem
丝氨酸/苏氨酸蛋白激酶 NLK(Serine/threonine-protein kinase NLK)
(2 活性数据)
MAPK11
Tchem
丝裂原活化蛋白激酶 11(Mitogen-activated protein kinase 11)
(2 活性数据)
MAPK14
Tchem
丝裂原活化蛋白激酶 14(Mitogen-activated protein kinase 14)
(18 活性数据)
化学和物理性质
折光率
1.71
沸点
615.6° C
熔点
280.73°C
安全和危险性（GHS）
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
Small-Molecule Inhibitors: A Practical Guide for Research Selection — A Minimal Evidence Chain and Scenario-Based Validation Framework (Including a Selection Matrix, Case Cards, and Product Tables 1–4)
目录： 技术文章
Inflammatory Signaling Pathway Research Guide: Danger Signal Recognition, Core Signaling Modules, Detection Readouts, and Representative Research Reagents
目录： 技术文章
MAPK/ERK Signaling Pathway: RAS–RAF–MEK–ERK Cascade Regulation, Cellular Functional Outputs, and Research Tool Applications
目录： 技术文章
Gentiana Root Extract and Gentiopicroside: Chemical Composition, Antioxidant and Inflammation-Modulating Mechanisms, and Their Potential Effects on Skin Barrier Homeostasis
目录： 技术文章
How Palmitoyl Pentapeptide-4 Acts on the Skin: From the KTTKS Sequence and Skin Delivery to Collagen Matrix Responses
目录： 技术文章
Potential Mechanisms of p-Cymene in Problem-Prone Skin: Membrane Perturbation, Inflammatory Signaling Modulation, and Localized Delivery
目录： 技术文章
Structure–Function Relationships of Ganoderma lucidum Extract: Skin-Protective Effects of Polysaccharides and Triterpenoids and Formulation Delivery Strategies
目录： 技术文章
Structural Characteristics of Ergothioneine, OCTN1-Mediated Uptake by Skin Cells, and Antioxidant Mechanisms
目录： 技术文章
Molecular Composition, Signal Transduction Mechanisms, and Targeted Regulatory Strategies of the Hippo Signaling Pathway
目录： 技术文章
天然产物调控脂肪褐变的分子机制
目录： 技术文章
此产品的引用文献
溶液计算器
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