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Targets Recommended: MEK

19

抑制剂 & 化合物

1

天然产物

2

重组蛋白

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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。
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).

化合物

Refametinib
Cat.No: T6636
Synonym: BAY 86-97661,瑞法替尼//瑞美替尼,BAY 869766,RDEA119
Target: MEK
RO4987655
Cat.No: T5412
Synonym: CH4987655,RG7167
Target: MEK
Trametinib
Cat.No: T2125
Synonym: GSK1120212,曲美替尼,JTP-74057
Target: Apoptosis, MEK, Autophagy
PD98059
Cat.No: T2623
Synonym: PD 98059
Target: ERK, Aryl Hydrocarbon Receptor, MEK, Autophagy
TCS PIM-1 1
Cat.No: T2253
Synonym: 3-氰基-4-苯基-6-(3-溴-6-羟基苯基)-2(1H)-吡啶酮,SC 204330
Target: Pim
Pimasertib
Cat.No: T6131
Synonym: 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
Target: MEK
BI-847325
Cat.No: T6785
Synonym:
Target: Apoptosis, MEK, Aurora Kinase
TAK-733
Cat.No: T6692
Synonym: TAK733,TAK 733
Target: MEK
U0126-EtOH
Cat.No: T6223
Synonym: U0126 Ethanol,U0126
Target: Mitophagy, Influenza Virus, MEK, Autophagy
AZD8330
Cat.No: T6083
Synonym: ARRY-424704,ARRY-704
Target: ERK, MEK
Trametinib (DMSO solvate)
Cat.No: T5857
Synonym: Trametinib DMSO solvate,GSK-1120212 (DMSO solvate),Trametinib dimethyl sulfoxide,JTP-74057 (DMSO solvate)
Target: Apoptosis, MEK
2,5-dimethyl Celecoxib
Cat.No: T35610
Synonym:
Target: Apoptosis, Wnt/beta-catenin, Prostaglandin Receptor
MS432
Cat.No: T13782
Synonym:
Target: MEK
SL327
Cat.No: T2708
Synonym: SL 327,SL-327
Target: MEK, DNA/RNA Synthesis
U-0126
Cat.No: T69826
Synonym:
Target:
CI-1040
Cat.No: T2443
Synonym: PD 184352
Target: Apoptosis, MEK
Pimasertib HCl
Cat.No: T71163
Synonym:
Target:
U0126
Cat.No: T21332
Synonym: U 0126,U-0126
Target: Mitophagy, MEK, Autophagy
Agerafenib hydrochloride
Cat.No: T14928
Synonym: RXDX-105 hydrochloride,CEP-32496 (hydrochloride)
Target: c-RET, c-Kit
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).

天然产物

Hypothemycin
Cat.No: T15542
Synonym:
Target: Others
Cat. No. Product Name Species Expression System
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...

重组蛋白

MEK2 Protein, Human, Recombinant (GST)
Cat.No: TMPY-04544
Species: Human
Expression System: Baculovirus Insect Cells
RAF1 Protein, Human, Recombinant (His & GST)
Cat.No: TMPY-05095
Species: Human
Expression System: Baculovirus Insect Cells
TargetMol Loading
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