24
14
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T11224 |
Rineterkib
ERK-IN-1 |
ERK; Raf | MAPK |
Rineterkib (ERK-IN-1) 是口服有效的RAF 和ERK1/2的抑制剂,与 KRAS-突变型非小细胞肺癌、BRAF-突变型非小细胞肺癌、KRAS-突变型胰腺癌、KRAS -突变型结肠癌和 KRAS-突变型卵巢癌尤为相关。 | |||
T7953 |
BpV(HOpic)
bpV (HOpic) |
PTEN | PI3K/Akt/mTOR signaling |
BpV(HOpic) (bpV (HOpic)) 是 PTEN 选择性抑制剂,IC50=14 nM。BpV(HOpic) 具有神经保护作用。 | |||
T21980 |
PD 198306
|
MEK | MAPK |
PD 198306 是一种具有抗痛觉过敏作用的 MAPK/ERK 激酶 (MEK) 选择性抑制剂。 PD 198306 可降低链脲佐菌素诱导的活性 ERK1 水平升高。 | |||
T23046 |
N-tert-butyl-α-Phenylnitrone
(Z)-N-benzylidene-2-Methylpropan-2-aMine oxide,N-叔丁基-α-苯基硝酮 |
ROS; COX | Immunology/Inflammation; Neuroscience |
N-tert-butyl-α-Phenylnitrone ((Z)-N-benzylidene-2-Methylpropan-2-aMine oxide) 是基于硝酮的自由基清除剂,可形成一氧化氮自旋加合物。它可以穿透血脑屏障,抑制 COX2的催化活性,有 ROS 清除、抗炎、神经保护、抗衰老和抗糖尿病的作用。 | |||
T64587 | p44/42 MAPK (Erk1/2) (137F5) Rabbit mAb #4695R | ||
p44/42 MAPK (Erk1/2) (137F5) Rabbit mAb #4695R 是一种有用的有机化合物,可用于生命科学领域的相关研究,其产品编号为 T64587。 | |||
T64608 | Phospho-p44/42 MAPK (Erk1/2) (Thr202/Tyr204) (20G11) Rabbit mAb #4376R | ||
Phospho-p44/42 MAPK (Erk1/2) (Thr202/Tyr204) (20G11) Rabbit mAb #4376R 是一种有用的有机化合物,可用于生命科学领域的相关研究,其产品编号为 T64608。 | |||
T27242 |
EF24
EF 24,EF-24,3,5-Bis[(2-fluorophenyl)Methylene]-4-piperidinone |
ERK; MEK; Caspase | Apoptosis; MAPK; Proteases/Proteasome |
EF24 (3,5-Bis[(2-fluorophenyl)Methylene]-4-piperidinone) 是姜黄素类似物,口服生物利用度高,抗肿瘤作用强。它可增强活化的 Caspase3 及 Caspase9 的水平,并抑制 MEK1 及 ERK 的磷酸化形式的表达。它可以抑制口腔鳞状细胞癌细胞的 MAPK/ERK 信号通路,从而发挥抗肿瘤作用。 | |||
T6277 |
Doramapimod
BIRB 796,达马莫德,度马莫德 |
Raf; p38 MAPK; Autophagy | Autophagy; MAPK |
Doramapimod (BIRB 796) 是一种具有口服活性的p38 MAPK 抑制剂,Kd 值为0.1nM。它也抑制B-Raf 和 Abl,IC50分别为 83 nM 和 14.6 μM。 | |||
T3636 |
(E)-SIS3
SIS3,SIS3 盐酸盐,SIS3 HCl |
TGF-beta/Smad | Stem Cells |
(E)-SIS3 (SIS3) 是 Smad3 的选择性抑制剂,能够抑制 Smad3 磷酸化(IC50:3 μM)。它利用 TGF-β1 抑制成纤维细胞向肌成纤维细胞分化。 | |||
T6066 |
SCH772984
|
ERK; MEK | MAPK |
SCH772984 是高选择性和 ATP 竞争性ERK 抑制剂,对 ERK1 和 ERK2 的IC50分别为 4 和 1 nM。它在含有 BRAF 或 RAS 突变的 MAPK 抑制剂初治和 MAPK 抑制剂耐药细胞中具有抗肿瘤活性。 | |||
T60821 | ACA-28 | ||
ACA-28 (compound 2a) 是ERK MAPK 信号的有效调节剂,可通过过度激活 ERK 诱导细胞凋亡,从而选择性抑制癌细胞生长。ACA-28 对黑色素瘤细胞 (SK-MEL-28) 和正常黑色素细胞 (NHEM) 细胞生长的IC50值分别为 5.3 和 10.1 μM。 | |||
T74374 |
ERK1/2 inhibitor 4
|
||
ERK1/2 inhibitor 5 是一种有效的ERK1/2抑制剂。丝裂原活化蛋白激酶 (MAPK) 在信号转导通路中起着极其重要的作用,而细胞外信号调节激酶 (ERK) 是MAPK 家族的成员。ERK1/2 inhibitor 5 具有研究或预防癌症、炎症或其他增殖性疾病的潜力。 | |||
T15113 |
Diazepinomicin
TLN-4601,BU 4664L,ECO-4601 |
Others | Others |
Diazepinomicin is a secondary metabolite produced by Micromonospora sp. It inhibits the EGF-induced Ras-ERK MAPK signaling pathway and induces apoptosis. Diazepinomicin also is an anti-tumor agent for K-Ras mutant models. | |||
T39294 |
Cobomarsen
MRG-106,Cobomarsen |
||
Cobomarsen (MRG-106) is an oligonucleotide inhibitor targeting miR-155. This compound effectively suppresses various gene pathways involved in cell survival, such as JAK/STAT, MAPK/ERK, and PI3K/AKT. Cobomarsen is particularly valuable in the study of B-cell lymphoma. | |||
T74373 |
ERK1/2 inhibitor 3
|
||
ERK1/2 inhibitor 3 是一种有效的 ERK1/2抑制剂。丝裂原活化蛋白激酶 (MAPK) 在信号转导通路中起着极其重要的作用,而细胞外信号调节激酶 (ERK) 是 MAPK 家族的成员。ERK1/2 inhibitor 3 具有研究或预防癌症、炎症或其他增殖性疾病的潜力。 | |||
T69826 |
U-0126
|
||
U0126 is a highly selective inhibitor of both MEK1 and MEK2, a type of MAPK/ERK kinase. It was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition of the dual specificity kinase MEK with IC50 of 72 nM for MEK1 and 58 nM for MEK2. U0126 inhibited anchorage-independent growth of Ki-ras-transformed rat fibroblasts by simultaneously blocking both extracellular signal-regulated kinase and mammalian target of rapamycin pathways. | |||
T41240 |
Verrucarin A
|
||
Verrucarin A (Muconomycin A) 是一种 D 型大环真菌毒素。Verrucarin A 是一种蛋白质合成 (protein synthesis) 的抑制剂,来源于Myrothecium verrucaria,可抑制白血病细胞系生长,并激活巨噬细胞 caspases、凋亡和炎症信号。Verrucarin A 能有效提高 p38 MAPK 的磷酸化,降低 ERK/Akt 的磷酸化。Verrucarin A 通过 p21 和 p53 的诱导引起细胞周期调控的解除。 | |||
T76059 |
SAH-SOS1A TFA
|
||
SAH-SOS1A TFA 是一种基于肽的SOS1/KRAS 蛋白相互作用抑制剂。SAH-SOS1A TFA 以纳摩尔亲和力 (EC50=106-175 nM) 与野生型和突变型 KRAS (G12D, G12V, G12C, G12S, Q61H) 结合,直接和独立地阻断核苷酸结合。SAH-SOS1A TFA 损害 KRAS 驱动的癌细胞活力,并通过阻断 KRAS 下游 ERK-MAPK 磷酸化信号级联的机制发挥作用。 | |||
T21547 |
PAF (C16)
C16-PAF |
ERK; MEK; MAPK; Endogenous Metabolite | MAPK; Metabolism |
PAF (C16) 是有效的 MAPK 和 MEK/ERK 激活剂,可诱导血管通透性增加。PAF (C16) (PAF (C16)) 是血小板活化因子,是一种磷脂衍生介质,也是 PAF G 蛋白偶联受体 (PAFR) 的配体。PAF (C16) 在体外实验中显示出抗凋亡和抗炎活性,通过与其受体 (PAF-R) 相互作用以执行细胞信号传导来抑制 caspase 依赖性凋亡。 | |||
T36676 |
Rineterkib hydrochloride
|
||
Rineterkib hydrochloride (compound B) is an orally active RAF and ERK1/2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer[1]. ERK-IN-1 (compound B) (50, 75 mg/kg, p.o., qd/q2d, 27 days) treatment significantly reduces the tumor volume in the C... | |||
TP2116 |
SAH-SOS1A
|
||
KRas/son of sevenless 1 (SOS1) interaction inhibitor. Binds within nucleotide binding pocket of KRas (Kd values are 106 - 176 nM for wild type KRas and various KRas mutants). Inhibits nucleotide binding to KRas in a concentration dependent manner. Display | |||
T38048 |
Globotetraosylceramides (porcine RBC)
|
||
Globotetraosylceramides are bioactive neutral glycosphingolipids. They are the major glycolipids in human erythrocytes. They act as receptors for the Shiga toxins Stx1, Stx2, and Stx2e, the cytotoxic protein pierisin-1, and parvovirus B19. Globotetraosylceramides increase the expression of proteins responsible for enamel deposition, including ameloblastin, amelogenin, and enamelin, in dental epithelial cells and activate the ERK and p38 MAPK signaling pathways. Levels of globotetraosylceramides ... | |||
T64155 | ERK1/2 inhibitor 5 | ||
ERK1/2 inhibitor 5 是一种 ERK1/2 的有效抑制剂。其中丝裂原活化蛋白激酶 (MAPK) 在信号转导通路中发挥着极大的作用,而细胞外信号调节激酶 (ERK) 是 MAPK 家族的成员。ERK1/2 inhibitor 5 具有研究或预防癌症、炎症或其他增殖性疾病的潜力。 | |||
T64147 |
ERK1/2 inhibitor 6
|
||
ERK1/2 inhibitor 6 是 ERK1/2 的有效抑制剂。其中丝裂原活化蛋白激酶 (MAPK) 在信号转导通路中发挥着极大的作用,而细胞外信号调节激酶 (ERK) 是 MAPK 家族的成员。ERK1/2 inhibitor 6 对癌症、炎症或其他增殖性疾病表现出研究或预防的潜力。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN1721 |
Gypenoside L
|
ERK; p38 MAPK; Calcium Channel; NF-κB; ROS | Immunology/Inflammation; MAPK; Membrane transporter/Ion channel; Metabolism; NF-κB |
Gypenoside L 是存在于绞股蓝中的一种皂苷,可增加 SA-β-半乳糖苷酶活性,促进衰老相关分泌细胞因子的产生。它还可以激活p38和ERK MAPK 通路和NF-κB 通路以诱导衰老,具有抗肿瘤和抗炎活性。 | |||
T5S0761 |
Nitidine chloride
|
Apoptosis; ERK; FAK; p38 MAPK; NF-κB; Topoisomerase; STAT; Parasite | Angiogenesis; Apoptosis; Cytoskeletal Signaling; DNA Damage/DNA Repair; JAK/STAT signaling; MAPK; Microbiology/Virology; NF-κB; Stem Cells; Tyrosine Kinase/Adaptors |
Nitidine chloride 是从Zanthoxylum nitidum (Roxb) DC 中分离得到的,具有抗疟疾活性。它通过多个靶点通路,起抗癌作用,抑制STAT3、DNA 拓扑异构酶1和2A、ERK 和c-Src/FAK 相关信号通路。它通过MAPK 和NF-kB 途径抑制Lps 诱导的炎性细胞因子的产生。 | |||
T6427 |
Butein
2’,3,4,4’-tetrahydroxy Chalcone,紫铆因 |
Apoptosis; EGFR; Others; PDE; Autophagy | Angiogenesis; Apoptosis; Autophagy; JAK/STAT signaling; Metabolism; Others; Tyrosine Kinase/Adaptors |
Butein (2’,3,4,4’-tetrahydroxy Chalcone) 是一种 cAMP 特异性PDE 抑制剂,也是蛋白酪氨酸激酶抑制剂,还是一种SIRT1激活剂。它通过 AKT 和 ERK/p38 MAPK 通路,靶向 FoxO3a 使 HeLa 细胞对 Cisplatin 敏感。 | |||
TN4114 |
Gardenin A
|
ERK; LDL; MAPK; PKA; PKC | Chromatin/Epigenetic; Cytoskeletal Signaling; MAPK; Metabolism; Tyrosine Kinase/Adaptors |
Gardenin A 通过激活 MAPK/ERK、PKC 和 PKA 表现出神经营养作用。 Gardenin A 具有抗抑郁、抗惊厥和抗焦虑作用。 | |||
T10383 |
Asatone
|
NF-κB | NF-κB |
Asatone 是一种从细辛中分离到的活性成分,通过活化 NF-κB 及下调 p-MAPK (ERK,JNK 和 p38) 通路起作用,具有抗炎作用。 | |||
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)。 | |||
TN1880 |
Lucidenic acid B
Lucidenicacid B |
Apoptosis; Caspase | Apoptosis; Proteases/Proteasome |
Lucidenic acid B (Lucidenicacid B) 是从灵芝中提取得到的天然化合物,可诱导caspase-9 和 caspase-3 的活化和 PARP 的裂解,可通过线粒体介导诱导人白血病细胞凋亡 。 Lucidenic acid B通过灭活MAPK / ERK信号转导途径和降低NF-kappaB和AP-1的结合活性来抑制PMA诱导的人肝癌细胞侵袭。。Lucidenic acid B 对细胞周期和坏死细胞没有影响。 | |||
TN5888 |
Toddaculin
|
Others | Others |
Toddaculin 是一种天然香豆素,抑制过度的破骨细胞活性并增强成骨细胞分化和矿化。它可诱导白血病细胞分化和凋亡,具有抗炎活性。 | |||
T3398 |
Icaritin
Anhydroicaritin,去水淫羊藿黄素,Cycloicaritin |
Apoptosis; JAK; STAT; Autophagy | Angiogenesis; Apoptosis; Autophagy; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
Icaritin (Anhydroicaritin) 是Epimedium Genusis 的异戊二烯类黄酮衍生物,有效抑制 K562 细胞和原代 CML 细胞的增殖。它可以调节MAPK/ERK/JNK 和JAK2/STAT3/AKT 信号传导,并具有增强成骨的作用。 | |||
TN1485 |
Chicanine
|
Others; NF-κB; Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation; NF-κB; Others |
Chicanine has anti-inflammatory activity in macrophages by down-regulating LPS-induced inflammatory cytokines in IκBα±/MAPK/ERK signaling pathways. | |||
TN5387 |
Grasshopper ketone
|
ERK; p38 MAPK; NO Synthase; JNK | Immunology/Inflammation; MAPK |
Grasshopper ketone 是从褐藻马尾藻中分离的化合物,是 RAW 264.7 细胞中 LPS 诱导的 NO 产生的有效抑制剂,通过抑制 MAPK(ERK,JNK 和 p38)和 NF-κB p65磷酸化来诱导抗炎作用。 | |||
TN2328 |
Zeylenone
|
Apoptosis; ERK; MAPK; Akt; PI3K; mTOR | Apoptosis; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling |
Zeylenone 是一种来自 Uvaria grandiflora的环己烯氧化物,具有抗肿瘤和抗癌细胞增殖活性,通过 PI3K/AKT/mTOR 和 MAPK/ERK 信号通路抑制宫颈癌细胞增殖,诱导细胞凋亡 (apoptosis)。 | |||
TN3541 |
Broussonin E
|
ERK; p38 MAPK; TNF; JAK; STAT | Angiogenesis; Apoptosis; Chromatin/Epigenetic; JAK/STAT signaling; MAPK; Stem Cells |
Broussonin E could suppress inflammation by modulating macrophages activation state via inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathway, and can be further developed as a promising drug for the treatment of inflammation-related | |||
TN3397 | Alpinumisoflavone | ERK; LDL; NF-κB; MEK; MAPK; Antifection | MAPK; Metabolism; Microbiology/Virology; NF-κB |
Alpinumisoflavone has atheroprotective effects, may result from their ability to upregulate mechanisms promoting HDL-cholesterol and bile acid formation, it is endowed with estrogenic properties accounting, at least in part, for E. lysistemon effects. Alp |