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Home >> Signaling Pathways >> MAPK Signaling >> MEK1/2

MEK1/2

MEK1/2, also known as MAPKK (mitogen-activated protein kinase kinase), is a kinase enzyme which phosphorylates MAPK (mitogen-activated protein kinase).

  1. Cat.No. 产品名称 Information
  2. 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。
  3. 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。
  4. 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。
  5. 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。
  6. 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。
  7. 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.
  8. 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。
  9. GC37523 RGB-286638 free base A multi-kinase inhibitor
  10. GC37522 RGB-286638 A multi-kinase inhibitor
  11. 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。
  12. 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.
  13. GC35719 Cobimetinib hemifumarate A potent, orally available MEK1 inhibitor
  14. 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。
  15. GC45099 U-0126

    A MEK inhibitor and AMPK activator
  16. GC43885 Hypothemycin A resorcylic acid lactone polyketide with diverse biological activities
  17. GC41573 Theaflavin 3,3'-digallate A polyphenol with diverse biological activities
  18. GC33831 Lidocaine hydrochloride (Lignocaine hydrochloride) An Analytical Reference Standard
  19. GC33388 MEK-IN-1 MEK-IN-1是来自专利WO2008076415A1的MEK抑制剂。
  20. 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。
  21. GC30162 trans-Zeatin

    A cytokinin plant growth regulator
  22. GC15646 PD 184161 A potent MEK1/2 inhibitor
  23. GC15240 APS-2-79 An inhibitor of KSR-dependent MAPK signaling
  24. GC17828 BI-847325 A selective dual MEK/Aurora kinase inhibitor
  25. GC14647 SCH772984 HCl

    A selective inhibitor of ERK1/2
  26. GC15044 SCH772984 TFA

    A selective inhibitor of ERK1/2
  27. GC12406 RO5126766(CH5126766) A dual inhibitor of MEK1 and Raf kinases
  28. GC12006 GDC-0994 A selective ERK1/2 inhibitor
  29. GC17485 PD 334581 A MEK inhibitor
  30. GC12851 10Z-Hymenialdisine A natural alkaloid that inhibits MEK-1 and other kinases
  31. GC17964 PD 198306 A potent inhibitor of MEK1/2
  32. GC15061 U0124 An inactive analog of U-0126
  33. GC14247 GDC-0623 A potent, ATP-uncompetitive inhibitor of MEK1
  34. GC16872 Refametinib An allosteric inhibitor of MEK1/2
  35. GC10209 TAK-733 A MEK1 inhibitor
  36. GC12141 RO4987655 A MEK inhibitor
  37. GC14643 AZD8330 A MEK1/2 inhibitor
  38. GC12843 MEK162 (ARRY-162, ARRY-438162) A MEK1/2 inhibitor
  39. GC15693 BIX 02188 A potent MEK5 inhibitor
  40. GC12220 BIX 02189 An inhibitor of MEK5 and ERK5
  41. GC10110 PD318088 An allosteric inhibitor of MEK1
  42. GC18050 Pimasertib (AS-703026) A MEK1/2 inhibitor
  43. GC12989 PD184352 (CI-1040) A potent MEK inhibitor
  44. GC15359 SL-327 A selective MEK1/2 inhibitor
  45. GC12819 PD98059

    PD98059 is a potent and selective MEK inhibitor with an IC50 of 2 μM. 
  46. GC17608 Lidocaine An Analytical Reference Standard
  47. GC17030 AZD6244(Selumetinib) A highly selective inhibitor of MEK1/2
  48. 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。
  49. GC16001 SCH772984

    A selective inhibitor of ERK1/2
  50. GC11277 MEK inhibitor MEK 抑制剂是一种有效的 MEK 抑制剂，具有抗肿瘤效力。
  51. 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。

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