19
1
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6636 |
Refametinib
BAY 86-97661,瑞法替尼//瑞美替尼,BAY 869766,RDEA119 |
MEK | MAPK |
Refametinib (RDEA119) 是可口服的、非 ATP 竞争和选择性的 MEK1/MEK2变构抑制剂,IC50分别为 19 和 47 nM。 | |||
T5412 |
RO4987655
CH4987655,RG7167 |
MEK | MAPK |
RO4987655 (RG7167) 是一种具有口服活性和高选择性的 MEK 抑制剂,抑制MEK1/MEK2,IC50为 5.2 nM。 | |||
T2253 |
TCS PIM-1 1
3-氰基-4-苯基-6-(3-溴-6-羟基苯基)-2(1H)-吡啶酮,SC 204330 |
Pim | Chromatin/Epigenetic; JAK/STAT signaling |
TCS PIM-1 1 (SC 204330) 是一种特异性有效的 ATP 竞争性 Pim-1 激酶抑制剂,IC50为 50 nM,对 MEK1/MEK2 和 Pim-2 表现出良好的特异性,IC50值大于 20000 nM。 | |||
T2125 |
Trametinib
GSK1120212,曲美替尼,JTP-74057 |
Apoptosis; MEK; Autophagy | Apoptosis; Autophagy; MAPK |
Trametinib (GSK1120212) 是一种 MEK 抑制剂,抑制 MEK1 和 MEK2 (IC50=0.7/0.9 nM),具有 ATP 非竞争性和口服活性。Trametinib 可以激活自噬,诱导凋亡。 | |||
T2623 |
PD98059
PD 98059 |
ERK; Aryl Hydrocarbon Receptor; MEK; Autophagy | Autophagy; Immunology/Inflammation; MAPK |
PD98059 是一种 MEK 抑制剂,抑制 MEK1 和 MEK2 (IC50=2/50 μM),具有非 ATP 竞争性。PD98059 也是一种 AHR 的配体而起拮抗作用。PD98059 可以抑制细胞自噬。 | |||
T6785 |
BI-847325
|
Apoptosis; MEK; Aurora Kinase | Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; MAPK |
BI847325是MEK 和极光激酶 (AK)的一种选择性双重抑制剂, 对人类MEK2和AK-C 的IC50值分别为4和15 nM。 | |||
T6131 |
Pimasertib
AS703026,MSC1936369B,N-[(2S)-2,3-二羟基丙基]-3-[(2-氟-4-碘苯基)氨基]-4-吡啶甲酰胺,SAR 245509 |
MEK | MAPK |
Pimasertib (AS703026) 是一种高效选择性和ATP 非竞争性的MEK1/2抑制剂,可用于癌症研究。 | |||
T6692 |
TAK-733
TAK733,TAK 733 |
MEK | MAPK |
TAK-733 是选择性 MEK 抑制剂,IC50为 3.2 nM。 | |||
T6223 |
U0126-EtOH
U0126 Ethanol,U0126 |
Mitophagy; Influenza Virus; MEK; Autophagy | Autophagy; MAPK; Microbiology/Virology |
U0126-EtOH (U0126 Ethanol) 是一种非 ATP 竞争性的选择性MEK1和MEK2抑制剂,IC50分别为 72 nM 和 58 nM。U0126-EtOH 可抑制自噬和线粒体自噬。 | |||
T6083 |
AZD8330
ARRY-424704,ARRY-704 |
ERK; MEK | MAPK |
AZD8330 (ARRY-704) 是非竞争性的 MEK1/MEK2抑制剂,IC50为 7 nM。 | |||
T5857 |
Trametinib (DMSO solvate)
Trametinib DMSO solvate,GSK-1120212 (DMSO solvate),Trametinib dimethyl sulfoxide,JTP-74057 (DMSO solvate) |
Apoptosis; MEK | Apoptosis; MAPK |
Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate)) 是一种口服有效的 MEK 抑制剂,抑制 MEK1 和 MEK2 的 IC50分别为 2 nM。它还能激活自噬,诱导凋亡。 | |||
T35610 |
2,5-dimethyl Celecoxib
|
Apoptosis; Wnt/beta-catenin; Prostaglandin Receptor | Apoptosis; Cytoskeletal Signaling; GPCR/G Protein; Immunology/Inflammation; Stem Cells |
2,5-dimethyl Celecoxib 是塞来昔布衍生物和微粒体前列腺素 E 合酶 1 (mPGES-1) 的靶向抑制剂,mPGES-1 是炎症介质 PGE2 合成途径中的关键酶。 | |||
T13782 |
MS432
|
MEK | MAPK |
MS432 is a highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2. | |||
T2708 |
SL327
SL 327,SL-327 |
MEK; DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; MAPK |
SL327 是能通过血脑屏障运输的选择性 MEK1/2 抑制剂,IC50 分别为 0.18 和 0.22 μM。 | |||
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. | |||
T2443 |
CI-1040
PD 184352 |
Apoptosis; MEK | Apoptosis; MAPK |
CI-1040 (PD 184352) 是一种有口服活性的高度特异性MEK 小分子抑制剂,对 MEK1 的IC50值为 17 nM 。 | |||
T71163 |
Pimasertib HCl
|
||
Pimasertib HCl is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity. Pimasertib selectively binds to and inhibits the activity of MEK1/2, preventing the activation of MEK1/2-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK1/2 (MAP2K1/K2) are dual-specificity threonine/tyrosine kinases that play key roles in the activati... | |||
T21332 |
U0126
U 0126,U-0126 |
Mitophagy; MEK; Autophagy | Autophagy; MAPK |
U0126 是一种有效的特异性非竞争性 MAP 激酶抑制剂,抑制 MEK-1 和 MEK-2,IC50 值分别为 0.07 和 0.06 μM。 U0126 抑制自噬和线粒体自噬。 | |||
T14928 |
Agerafenib hydrochloride
RXDX-105 hydrochloride,CEP-32496 (hydrochloride) |
c-RET; c-Kit | Apoptosis; Tyrosine Kinase/Adaptors |
Agerafenib hydrochloride is a highly potent inhibitor of BRAFV600E (Kd: 14 nM). |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T15542 |
Hypothemycin
|
Others | Others |
Hypothemycin is a fungal polyketide and is a multikinase inhibitor (Kis: 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively). |