MEK1/2
MEK1/2, also known as MAPKK (mitogen-activated protein kinase kinase), is a kinase enzyme which phosphorylates MAPK (mitogen-activated protein kinase).
- Cat.No. 产品名称 Information
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GC70053
Trametiglue
Trametiglue 是 Trametinib 的衍生物,通过独特的界面结合相互作用,以前所未有的效力和选择性靶向 KSR-MEK 和 RAF-MEK。
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GC69191
GSK1790627
GSK1790627 是 Trametinib 的 N-脱乙酰代谢物。Trametinib 是一种具有口服活性的 MEK 抑制剂,可激活自噬并诱导细胞凋亡。
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GC64904
MAP855
MAP855 是一种高效、具有选择性且口服有效的 ATP 竞争性 MEK1/2 激酶抑制剂 (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM)。MAP855 对野生型和突变型 MEK1/2 具有同等的抑制作用。
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GC64292
MS432
MS432 是创新的、高度选择性的、基于 PD0325901 和 von Hippel-Lindau 配体的 MEK1 和 MEK2 的 PROTAC 降解剂。MS432 在小鼠体内显示了较高且长时间的血浆暴露量,对 HT29 细胞中 MEK1 和 MEK2 蛋白的DC50 值分别为 31 nM 和 17 nM。
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GC63554
PD0325901-O-C2-dioxolane
PD0325901-O-C2-dioxolane 含有 MEK 抑制剂 PD0325901 主要部分。PD0325901-O-C2-dioxolane 和 VHL 或 CRBN E3 连接酶的配体可用于 MEK1/2 降解剂的合成。
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GC63264
Zapnometinib
Zapnometinib (PD0184264, ATR-002), an major active metabolite of CI-1040, is a novel MEK inhibitor with an IC50 of 5.7 nM.
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GC38653
Selumetinib sulfate
Selumetinib (AZD6244) 是一种高效选择性的,非 ATP 竞争性的 MEK1/2 抑制剂, 抑制 MEK1 的 IC50 为 14 nM。Selumetinib (AZD6244) 抑制 MEK1/2 磷酸化水平。
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GC37523
RGB-286638 free base
A multi-kinase inhibitor
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GC37522
RGB-286638
A multi-kinase inhibitor
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GC37516
Refametinib R enantiomer
Refametinib R enantiomer 是一种 MEK 抑制剂,EC50为 2.0-15 nM,详细信息请参考专利文献WO2007014011A2 中的化合物 1022。
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GC36199
GW284543
GW284543 (UNC10225170), a MEK5-selective inhibitor, inhibits MEK5 in a dose-dependently way as determined by reductions in pERK5, and decreases endogenous MYC protein.
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GC35719
Cobimetinib hemifumarate
A potent, orally available MEK1 inhibitor
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GC35684
CHMFL-EGFR-202
CHMFL-EGFR-202 是一种有效、不可逆的表皮生长因子受体 (EGFR) 突变型激酶抑制剂, 对 耐药突变型 EGFR T790M 和 WT EGFR 激酶作用的 IC50 值分别为 5.3 nM 和 8.3 nM。在细胞中,CHMFL-EGFR-202 对 EGFR L858R/T790M 的选择性是 EGFR 野生型的 10 倍。CHMFL-EGFR-202 以 “DFG-in-C-helix-out” 的不活跃结合构象形式共价结合 EGFR,对 EGFR 突变体驱动的非小细胞肺癌 (NSCLC) 细胞株具有较强的抗增殖作用。
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GC45099
U-0126
A MEK inhibitor and AMPK activator
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GC43885
Hypothemycin
A resorcylic acid lactone polyketide with diverse biological activities
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GC41573
Theaflavin 3,3'-digallate
A polyphenol with diverse biological activities
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GC33831
Lidocaine hydrochloride (Lignocaine hydrochloride)
An Analytical Reference Standard
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GC33388
MEK-IN-1
MEK-IN-1是来自专利WO2008076415A1的MEK抑制剂。
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GC33305
Balamapimod (MKI 833)
Balamapimod (MKI 833) (MKI 833) 是一种可逆的 Ras/Raf/MEK 抑制剂,具有潜在的抗肿瘤活性。
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GC30162
trans-Zeatin
A cytokinin plant growth regulator
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GC15646
PD 184161
A potent MEK1/2 inhibitor
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GC15240
APS-2-79
An inhibitor of KSR-dependent MAPK signaling
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GC17828
BI-847325
A selective dual MEK/Aurora kinase inhibitor
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GC14647
SCH772984 HCl
A selective inhibitor of ERK1/2
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GC15044
SCH772984 TFA
A selective inhibitor of ERK1/2
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GC12406
RO5126766(CH5126766)
A dual inhibitor of MEK1 and Raf kinases
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GC12006
GDC-0994
A selective ERK1/2 inhibitor
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GC17485
PD 334581
A MEK inhibitor
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GC12851
10Z-Hymenialdisine
A natural alkaloid that inhibits MEK-1 and other kinases
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GC17964
PD 198306
A potent inhibitor of MEK1/2
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GC15061
U0124
An inactive analog of U-0126
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GC14247
GDC-0623
A potent, ATP-uncompetitive inhibitor of MEK1
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GC16872
Refametinib
An allosteric inhibitor of MEK1/2
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GC10209
TAK-733
A MEK1 inhibitor
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GC12141
RO4987655
A MEK inhibitor
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GC14643
AZD8330
A MEK1/2 inhibitor
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GC12843
MEK162 (ARRY-162, ARRY-438162)
A MEK1/2 inhibitor
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GC15693
BIX 02188
A potent MEK5 inhibitor
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GC12220
BIX 02189
An inhibitor of MEK5 and ERK5
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GC10110
PD318088
An allosteric inhibitor of MEK1
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GC18050
Pimasertib (AS-703026)
A MEK1/2 inhibitor
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GC12989
PD184352 (CI-1040)
A potent MEK inhibitor
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GC15359
SL-327
A selective MEK1/2 inhibitor
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GC12819
PD98059
PD98059 is a potent and selective MEK inhibitor with an IC50 of 2 μM.
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GC17608
Lidocaine
An Analytical Reference Standard
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GC17030
AZD6244(Selumetinib)
A highly selective inhibitor of MEK1/2
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GC15260
Trametinib DMSO solvate
Trametinib DMSO solvate (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) 是一种具有口服活性的 MEK 抑制剂,抑制 MEK1 和 MEK2,IC50 约为 2 nM。 Trametinib DMSO solvate 激活自噬并诱导细胞凋亡。
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GC16001
SCH772984
A selective inhibitor of ERK1/2
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GC11277
MEK inhibitor
MEK 抑制剂是一种有效的 MEK 抑制剂,具有抗肿瘤效力。
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GC14337
Cobimetinib (R-enantiomer)
Cobimetinib R-对映异构体是 Cobimetinib 活性较低的 R-对映异构体。 Cobimetinib 是一种有效的选择性 MEK 抑制剂。