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Cat. No. | Product Name | ||
---|---|---|---|
L1400 | MAPK 抑制剂库 | 365 compounds | |
365 种与MAPK 信号通路相关的生物活性小分子化合物的特有集合,可用于高通量筛选和高内涵筛选; |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T1031 |
Cloxacillin sodium monohydrate
Cloxacillin Sodium,Bactopen,氯唑西林钠一水合物 |
Antibacterial; Antibiotic | Microbiology/Virology |
Cloxacillin sodium monohydrate (Cloxacillin Sodium) 有抗菌作用,对Staphylococcus aureus25923 的最小抑菌浓度为256 mg/L。 | |||
T2036 |
6-OAU
GTPL5846 |
GPR | Endocrinology/Hormones; GPCR/G Protein |
6-OAU (GTPL5846) 是 GPR84 的替代激动剂,在 Gqi5 嵌合体存在的情况下,在 HEK293 细胞中激活人 GPR84,在 PI 测定中 EC50 为 105 nM。 | |||
T39823L |
Apelin-12 acetate
Apelin-12 acetate (229961-08-4 Free base) |
Apelin receptor; p38 MAPK; JNK | GPCR/G Protein; MAPK |
Apelin-12 acetate 对 APJ 受体具有高亲和力。 Apelin-12 acetate 抑制凋亡相关 MAPKs 家族的 JNK 和 p38 MAPK 信号通路,从而为神经元提供保护。 | |||
T4133 |
CCT196969
|
Raf; Src | Angiogenesis; MAPK; Tyrosine Kinase/Adaptors |
CCT196969 是泛-Raf 抑制剂,抑制B-Raf、BRafV600E 和CRAF,IC50分别为 0.1、0.04、和 0.01 μM。 | |||
T12871 |
Talmapimod
他匹莫德,SCIO-469 |
p38 MAPK | MAPK |
Talmapimod (SCIO-469) 是 选择性的,具有口服活性的,ATP 竞争性的 p38α抑制剂,对 p38α和 p38β的 IC50 值分别是 9 nM 和90 nM。Talmapimod 在 20 个其他激酶 (包括其他 MAPKs) 上显示出至少 2000 倍的选择性。 | |||
T12871L |
Talmapimod hydrochloride
SCIO-469 hydrochloride |
p38 MAPK | MAPK |
Talmapimod hydrochloride is a selective and ATP-competitive p38α inhibitor (IC50: 9 nM). It also shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs. | |||
T73058 |
Cloxacillin
氯唑西林 |
Others | Others |
Cloxacillin 是一种口服有效的抗菌剂和β-lactamase 抑制剂,其IC50值为 0.04 µM。Cloxacillin 可通过抑制MAPKs、NF-кB 和NLRP3相关蛋白的激活从而抑制金黄色葡萄球菌所引起的炎症反应。 | |||
T84435 |
Nε-(1-Carboxymethyl)-L-lysine
CML |
Others | Others |
Nε-(1-Carboxymethyl)-L-lysine (CML), an advanced glycation end product (AGE), is formed through the oxidative modification of glycated proteins under conditions of oxidative stress.1,2,3 Its levels escalate with age, diabetes, cancer, vascular diseases, and various pathologies associated with oxidative stress.1,4,5 CML interacts with the membrane-bound receptor for AGEs (RAGE), initiating signaling via MAPKs and NF-κB pathways. Conversely, a truncated version of RAGE generates a soluble protein ... | |||
TP2177 |
Amyloid Precursor C-Terminal Peptide
|
Others | Others |
Amyloid precursor c-terminal peptide has the amino acid sequence Gly-Tyr-Glu-Asn-Pro-Thr-Tyr-Lys-Phe-Phe-Glu-Gln-Met-Gln-Asn. APP is best known as the precursor molecule whose proteolysis generates beta-amyloid (Aβ), a 37 to 49 amino acid peptide whose am |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6S0107 |
Peimine
贝母素甲,Wanpeinine A,Dihydroisoimperialine,Verticine,贝母甲素 |
Others | Others |
Peimine (Wanpeinine A) 是一种天然化合物,具有很好抗炎症活性。 | |||
T3908 |
10-Gingerol
10-姜酚 |
Apoptosis | Apoptosis |
10-Gingerol 是一种姜根脂的主要刺激性成分,具有抗炎、抗氧化和抗增殖作用,能够抑制 MDA-MB-231 肿瘤细胞的增殖(IC50:12.1 μM)。 | |||
TN1879 |
Lucideric acid A
Lucidenic acid A,赤芝酸A |
MMP; p38 MAPK; JNK | MAPK; Proteases/Proteasome |
Lucideric acid A (Lucidenic acid A) 是分离自灵芝的天然产物,可抑制 PMA 诱导的MMP-9活性,具有抵抗肝癌细胞侵袭的作用。 | |||
TN1134 |
Euscaphic acid
|
Apoptosis; LDL; PI3K; DNA/RNA Synthesis; NO Synthase; Prostaglandin Receptor | Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; GPCR/G Protein; Immunology/Inflammation; Metabolism; PI3K/Akt/mTOR signaling |
Euscaphic acid 是来源于枣的一种三萜,是DNA 聚合酶抑制剂,可诱导细胞凋亡。它抑制小牛 DNA 聚合酶 α 和大鼠 DNA 聚合酶 β 的IC50值分别为 61 和 108 μM。 | |||
T3884 |
Neoandrographolide
Neoandrographiside,新穿心莲内酯 |
NOS; COX | Immunology/Inflammation; Neuroscience |
Neoandrographolide (Neoandrographiside) 是一种二萜类化合物,从穿心莲中分离得到。 | |||
T5S1895 |
Norisoboldine
Laurelliptine,去甲异波尔定,(+)-Laurelliptine |
MAPK; Adenosine Receptor | GPCR/G Protein; MAPK; Neuroscience |
Norisoboldine ((+)-Laurelliptine) 是一种可口服的芳基烃受体激动剂,是乌药中主要的异喹啉类生物碱,可用于类风湿性关节炎和溃疡性结肠炎的研究。 | |||
T5S1097 |
Neferine
(R)-1,2-Dimethoxyaporphine,(-)-Neferine,甲基莲心碱 |
Apoptosis; NF-κB; Autophagy | Apoptosis; Autophagy; NF-κB |
Neferine ((-)-Neferine) 是一种双苄基异喹啉类生物碱,可强效抑制NF-κB 激活,具有抗肿瘤活性。 | |||
TCS2170 |
2,5-Dihydroxyacetophenone
Quinacetophenone,2-Acetylhydroquinone,2-5-dihydroxyacetophenone,2 ',5'-二羟基苯乙酮,Acetylhydroquinone,2,5-二羟基苯乙酮,DHAP |
ERK; NF-κB; Tyrosinase | MAPK; NF-κB; Proteases/Proteasome |
2,5-Dihydroxyacetophenone (Quinacetophenone) 是从熟地黄中分离出的一种天然产物,通过阻断 ERK1/2和 NF-κB 信号通路,抑制活化巨噬细胞中炎症介质的产生。 | |||
T6S1917 |
Schisandrol B
Gomisin A,TJN-101,Besigomsin,五味子醇乙,Gamma-Schisandrin,戈米辛A,Schizandrol B,Wuweizi alcohol-B |
P450; Reactive Oxygen Species; Autophagy | Autophagy; Immunology/Inflammation; Metabolism; NF-κB |
Schisandrol B (Besigomsin) 是华中五味子的主要活性成分,具有保肝、抗炎、抗糖尿病和抗氧化的作用。它抑制活性氧的产生,也抑制 P-糖蛋白和CYP3A 的活性。 | |||
T5S2283 |
Sesamolin
|
p38 MAPK; Caspase; JNK | Apoptosis; MAPK; Proteases/Proteasome |
Sesaminol 是从Justicia orbiculata 中分离得到的一种天然产物,抑制脂质过氧化,具有神经保护作用和抗氧化活性。它通过抑制JNK、p38 MAPKs 和caspase-3磷酸化,抑制MAPK 的级联反应。 | |||
T2S2215 |
Crebanine
|
Apoptosis; Others; Akt | Apoptosis; Cytoskeletal Signaling; Others; PI3K/Akt/mTOR signaling |
Crebanine 是来自于韦诺萨千金藤的一种生物碱,通过抑制 MAPKs 和 Akt 信号通路表现出抗炎活性,还具有抗心律失常的作用。它可诱导人类癌细胞的 G1阻滞和凋亡。 | |||
TN4785 |
Picrasidine I
|
NF-κB; ROS; MAPK | Immunology/Inflammation; MAPK; NF-κB |
Picrasidine I has antiosteoclastogenic effect by inhibiting inflammation induced activation of MAPKs, NF-κB and ROS generation followed by suppressing the gene expression of c-Fos and NFATc1 in osteoclast precursors. | |||
TN2123 |
Quercetin 3-O-(6''-galloyl)-β-D-galactopyranoside
Hyperin 6''-gallate,槲皮素3-O-(6''-没食子酰基)-Β-D-半乳糖苷,Quercetin 3-O-(6''-galloyl)-beta-D-galactopyranoside |
MAPK; p53 | Apoptosis; MAPK |
Quercetin 3-O-(6''-galloyl)-beta-D-galactopyranoside can effectively induce apoptosis via p53, MAPKs and the mitochondrial apoptotic pathways. | |||
TN1504 |
Citreorosein
羟基大黄素 |
cAMP; NF-κB; PI3K | GPCR/G Protein; NF-κB; PI3K/Akt/mTOR signaling |
Citreorosein is a cAMP phosphodiesterase inhibitor, it has anti-inflammatory effect, inhibits proinflammatory cytokines production through the inhibition of both MAPKs and AKT-mediated IκB kinase (IKK) phosphorylation and subsequent inhibition of transcription factor NF-κB activation. | |||
TN2327 |
Zedoarondiol
蓬莪二醇 |
NOS; NF-κB; COX | Immunology/Inflammation; Neuroscience; NF-κB |
Zedoarondiol has anti-inflammatory activity, inhibits iNOS, COX-2, and pro-inflammatory cytokine expressions by suppressing the phosphorylations of IKK and MAPKs, and by subsequently inactivating the NF-kappaB pathway. | |||
TN1645 |
Flavokawain C
|
NADPH-oxidase; MAPK; AChR | Immunology/Inflammation; MAPK; Neuroscience |
Flavokawain C is a melanogenesis inhibitor, it inhibited melanogenesis with IC50 values of 6.9 μM. Flavokawain C has anti-tumor activity, it inhibited cell cycle and promoted apoptosis, associated with endoplasmic reticulum stress and regulation of MAPKs and Akt signaling pathways in HCT 116 human colon carcinoma cells. | |||
TN2243 |
Sugiol
10-Deoxoxanthoperol |
IL Receptor; TNF; ROS | Apoptosis; Immunology/Inflammation |
Sugiol (10-Deoxoxanthoperol) 是一种枞烷二萜,可从台湾板栗树 (Calocedrus formosana) 的树皮中分离出来。Sugiol 具有抗炎活性,可有效减少脂多糖 (LPS) 刺激巨噬细胞后的活性氧 (ROS) 产生。 | |||
T4700 |
1,3,5-Trihydroxy-4-prenylxanthone
|
||
1,3,5-Trihydroxy-4-prenylxanthone is a relatively potent inhibitor of phosphodiesterase type 5 (PDE5), with an IC50 value of 3.0 μM; it shows in vitro inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with IC50 valu | |||
TN4877 | Quercetin 3,4'-dimethyl ether | ERK; BCL; MAPK; Caspase; JNK | Apoptosis; MAPK; Proteases/Proteasome |
Quercetin 3,4'-dimethyl ether shows anti-lipid peroxidation activity (IC 50 values of 0.3 uM), it also shows anti-inflammatory activity. Quercetin 3,4'-dimethyl ether could be useful in the development of novel anticancer agents, it has high cytotoxic aga | |||
TN3587 |
Capillarisin
|
MMP; ERK; IL Receptor; BCL; VEGFR; TNF; NOS; NF-κB; TLR; MAPK; COX; DNA/RNA Synthesis; Prostaglandin Receptor; JNK; STAT | Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; GPCR/G Protein; Immunology/Inflammation; JAK/STAT signaling; MAPK; Neuroscience; NF-κB; Proteases/Proteasome; Stem Cells; Tyrosine Kinase/Adaptors |
Capillarisin is a novel blocker of STAT3 activation and thus may have a potential in negative regulation of growth, metastasis, and chemoresistance of tumor cells, it inhibits cancer cell growth of osteosarcoma cells by inducing apoptosis accompanied with | |||
TN3364 |
Agrimonolide
|
Apoptosis; Dehydrogenase; p38 MAPK; ROS; JAK | Angiogenesis; Apoptosis; Chromatin/Epigenetic; Immunology/Inflammation; JAK/STAT signaling; MAPK; Metabolism; Stem Cells |
Agrimonolide 是一种来自异香豆素的化合物,主要存在于草药Agrimonia pilosa Ledeb 中,具有显著的生物活性。Agrimonolide 通过抑制脂多糖(LPS)诱导的JAK-STATs 和p38 MAPKs 信号通路的激活而发挥抗炎作用。Agrimonolide 及其衍生物去甲阿戈莫内德已显示出能够有效提高肝细胞中胰岛素介导的糖原水平,可能在调节胰岛素抵抗的HepG2细胞中发挥关键作用。Agrimonolide 通过靶向卵巢癌细胞中的SCD1,对癌症的进展和诱导细胞死亡和凋亡表现出抑制作用。特别是,Agrimonolide 对A2780和SKOV-3细胞的增殖、迁移和侵袭表现出剂量依赖性的抑制,同时促进细胞凋亡。该化合物还被发现能诱导铁介导的细胞死亡,同时增加活性氧(ROS)和总铁的水平。Agrimonolide 很容易穿过血脑屏障,表明其在神经系统疾病的治疗应用方面具有潜力。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPH-02278 |
PTPN5 Protein, Human, Recombinant (His & SUMO)
PTPN5,Neural-specific protein-tyrosine phosphatase,Tyrosine-... |
Human | E. coli |
May regulate the activity of several effector molecules involved in synaptic plasticity and neuronal cell survival, including MAPKs, Src family kinases and NMDA receptors. PTPN5 Protein, Human, Recombinant (His & SUMO) is expressed in E. coli expression system with N-6xHis-SUMO tag. The predicted molecular weight is 45.5 kDa and the accession number is P54829. | |||
TMPJ-00907 |
GADD45A Protein, Human, Recombinant (His)
GADD45,DDIT1,Growth Arrest and DNA Damage-Inducible Protein ... |
Human | E. coli |
Growth Arrest and DNA Damage-Inducible Protein GADD45 α (GADD45A) is a member of the GADD45 family. GADD45A can be induced by UV irradiation, X-rays, growth arrest and alkylating agents, of which can be mediated by some kinases other than PKC. GADD45A can interact with MAPK14, GADD45GIP1, PCNA. In T-cells, GADD45A functions as a regulator of p38 MAPKs by inhibiting p88 phosphorylation and activity. GADD45A may affect PCNA interaction with some cell division protein kinase complexes, stimulating ... | |||
TMPJ-00700 |
GADD45B Protein, Human, Recombinant (His)
MYD118,Myeloid Differentiation Primary Response Protein MyD1... |
Human | E. coli |
Growth Arrest and DNA Damage-Inducible Protein GADD45 β (GADD45B) is a member of the GADD45 family. GADD45B has been shown to interact with MAP3K4, ASK1, MAP2K7, and GADD45GIP1. GADD45B is involved in the regulation of growth and apoptosis. GADD45B reacts to environmental stresses by mediating activation of stress-responsive MTK1/MEKK4 kinase, which is an upstream activator of both p38 and JNK MAPKs. In addition, GADD45B participates in the down-regulation of hepatocellular carcinoma (HCC). It m... | |||
TMPY-03655 |
GADD45G Protein, Human, Recombinant
GADD45γ,growth arrest and DNA-damage-inducible, γ,DDIT2,grow... |
Human | E. coli |
GADD45G, also known as CR6, is part of the nuclear proteins to interact with various proteins whose transcript levels are raised after stressful growth arrest conditions and treatment with DNA-damaging agents. GADD45G reacts to environmental stresses by mediating activation of the p38/JNK pathway which is mediated through their protein binding and activating MTK1/MEKK4 kinase, which is an upstream activator of both p38 and JNK MAPKs. GADD45G acts as a new-age tumor suppressor however is being fr... | |||
TMPY-02595 |
DUSP14 Protein, Human, Recombinant (His & MBP)
MKP6,MKP-L,dual specificity phosphatase 14 |
Human | E. coli |
Dual specific phosphatase 14 / MAP-kinase phophatase-6 (DUSP14 / MKP6) is a member of Dual-specificity phosphatases that is a subclass of protein tyrosine phosphatases (PTP) families that can dephosphorylate bothe phosphotyrosine and phosphoserine / phosphothreonine residues in substrates. Unlike many other DUSPs, DUSP14 only contains a catalytic domain within the C-terminal region. In signal transduction, DUSP14 has been considered as negative regulator of the mitogen-activated protein kinase (... | |||
TMPY-04460 |
OXSR1 Protein, Human, Recombinant (GST)
OSR1,oxidative stress responsive 1 |
Human | Baculovirus Insect Cells |
Oxidative stress-responsive 1 protein (OXSR1), also known as Serine/threonine-protein kinase OSR1, is a member of the Ser/Thr protein kinase family of proteins. OXSR1 regulates downstream kinases in response to environmental stress, and may play a role in regulating the actin cytoskeleton. OXSR1 is a 58 kDa protein of 527 amino acids that is widely expressed in mammalian tissues and cell lines. The amino acid (aa) sequence of the predicted OXSR1 protein is 39% identical to that of human SOK1. Of... | |||
TMPY-02228 |
p53 Protein, Cynomolgus, Recombinant
tumor protein p53,p53,TP53 |
Cynomolgus | E. coli |
p53, also known as Tp53, is a DNA-binding protein which belongs to the p53 family. It contains transcription activation, DNA-binding, and oligomerization domains. p53 protein is expressed at low level in normal cells and at a high level in a variety of transformed cell lines, where it's believed to contribute to transformation and malignancy. p53 (TP53) is a transcription factor whose protein levels and post-translational modification state alter in response to cellular stress (such as DNA damag... | |||
TMPH-01692 |
MAPK3 Protein, Human, Recombinant (His)
MAP kinase isoform p44,p44-ERK1,MAPK3,Extracellular signal-r... |
Human | E. coli |
Serine/threonine kinase which acts as an essential component of the MAP kinase signal transduction pathway. MAPK1/ERK2 and MAPK3/ERK1 are the 2 MAPKs which play an important role in the MAPK/ERK cascade. They participate also in a signaling cascade initiated by activated KIT and KITLG/SCF. Depending on the cellular context, the MAPK/ERK cascade mediates diverse biological functions such as cell growth, adhesion, survival and differentiation through the regulation of transcription, translation, c... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T10901 |
Curcumin-d6
Turmeric yellow D6,Natural Yellow 3 D6,Curcumin D6,Diferuloylmethane D6 |
Others | Others |
Curcumin D6 (difluoroformylmethane D6) is deuterium-labeled curcumin (Turmeric yellow). Curcumin (Turmeric yellow) is a natural phenolic compound with various pharmacological effects, including anti-inflammatory, antioxidant, anti-proliferative and anti-a |