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抑制剂 & 化合物

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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。
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).

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
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
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
BI-847325
Cat.No: T6785
Synonym:
Target: Apoptosis, MEK, Aurora Kinase
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
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
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