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Cat. No. | Product Name | Target | Signaling Pathways |
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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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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 |
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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). |
Cat. No. | Product Name | Species | Expression System |
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TMPY-04544 |
MEK2 Protein, Human, Recombinant (GST)
mitogen-activated protein kinase kinase 2,FLJ2<... |
Human | Baculovirus Insect Cells |
Dual specificity mitogen-activated protein kinase kinase 2, also known as MAP kinase kinase 2, MAPKK2, ERK activator kinase 2, MAPK / ERK kinase 2, MEK2 and MAP2K2, is a member of the protein kinase superfamily, STE Ser/Thr protein kinase family and MAP kinase kinase subfamily. MAP2K2 / MEK2 contains one protein kinase domain. MEK1 and MEK2 (also known as MAP2K1 and MAP2K2, respectively) are evolutionarily conserved, dual-specificity kinases that mediate Erk1 and Erk2 activation during adhesion ... | |||
TMPY-05095 |
RAF1 Protein, Human, Recombinant (His & GST)
Raf-1 proto-oncogene, serine/threonine kinase,CRAF,NS5,CMD1N... |
Human | Baculovirus Insect Cells |
RAF1 gene is the cellular homolog of viral raf gene (v-raf). The encoded protein is a MAP kinase kinase kinase (MAP3K), which functions downstream of the Ras family of membrane associated GTPases to which it binds directly. Once activated, the cellular RAF1 protein can phosphorylate to activate the dual specificity protein kinases MEK1 and MEK2, which in turn phosphorylate to activate the serine/threonine specific protein kinases, ERK1 and ERK2. Activated ERKs are pleiotropic effectors of cell p... |