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RIP kinase(受体相互作用蛋白激酶)

Receptor interacting protein 2 (RIP2), a serine/threonine kinase, is an adaptor molecule of NOD1 and NOD2, and genetic variation in this receptor is known to be associated with the severity of allergic asthma in children.

Receptor interacting protein kinase 2 (RIPK2) is critical for NOD-mediated NF-κB activation and cytokine production. WEHI-345, a selective RIPK2 kinase inhibitor, which delays RIPK2 ubiquitylation and NF-κB activation downstream of NOD engagement.

Receptor interacting protein kinase 3 (RIPK3) is a cytosolic master regulator of necroptosis. RIPK3 has an active serine/threonine kinase domain at the N-terminus, and a unique protein-protein interaction domain called the RIP homotypic interaction motif (RHIM) at the C-terminus. Both kinase activity and RHIM are indispensable for necroptosis. RIPK3 interacts with other RHIM-containing proteins such as RIPK1, Toll/interleukin-1 (IL-1) receptor domain-containing adaptor protein inducing TRIF or DAI. RIPK3 induces necroptosis, a type of regulated necrosis, through its kinase domain and RHIM.

Products for  RIP kinase

  1. Cat.No. 产品名称 Information
  2. GC68903 cRIPGBM chloride cRIPGBM chloride 是一种口服有效的促凋亡衍生物,cRIPGBM 可从多形性胶质母细胞瘤 (GBM) 癌症干细胞 (CSC) 中产生。cRIPGBM chloride 靶向受体相互作用蛋白激酶 2 (RIPK2) 以诱导半胱天冬酶 caspase 1 依赖性细胞凋亡。cRIPGBM chloride 抑制 RIPK2/TAK1 (促存活复合物) 的形成,并增加 RIPK2/caspase 1 (促凋亡复合物) 的形成。cRIPGBM chloride 在动物模型中发挥了强力的体内抗肿瘤活性。
  3. GC67969 RIP1/RIP3/MLKL activator 1 RIP1/RIP3/MLKL activator 1 (Compound 6i) 是一种有效的抗胶质瘤 (anti-glioma) 药物。RIP1/RIP3/MLKL activator 1 通过激活 RIP1/RIP3/MLKL 通路诱导细胞坏死 (Necroptosis)。 RIP1/RIP3/MLKL activator 1 可透过血脑屏障。
  4. GC66479 GSK2593074A GSK2593074A (GSK'074) 是一种程序性坏死 (necroptosis) 抑制剂, 抑制 RIP1 和 RIP3。
  5. GC65967 RIP2 Kinase Inhibitor 3 RIP2 Kinase Inhibitor 3 是一种高效、选择性的受体相互作用蛋白 -2 (RIP2) 激酶抑制剂,IC50 值为 1 nM。
  6. GC65467 RIPK1-IN-10 RIPK1-IN-10 是一种有效的 RIPK1 抑制剂,例 37,提取自专利 WO2021160109。
  7. GC65004 Apostatin-1 Apostatin-1 (Apt-1) is a novel TRADD inhibitor. Apostatin-1 binds to a pocket on the N-terminal TRAF2-binding domain of TRADD (TRADD-N). Apostatin-1 inhibits bortezomib-induced apoptosis and RIPK1-dependent apoptosis (RDA) with an IC50 of about 1 μM.
  8. GC64951 GSK963 GSK'963 is a chiral small-molecule inhibitor of RIP1 kinase (RIPK1) with an IC50 of 29 nM in FP binding assays. It is >10?000-fold selective for RIP1 over 339 other kinases.
  9. GC64370 Kongensin A Kongensin A 是一种从 Croton kongensis 中分离的天然产物。 Kongensin A 是一种有效的,共价的 HSP90 抑制剂,可阻断 RIP3 依赖性坏死病。Kongensin A 是一种有效的坏死性抑制剂和凋亡诱导剂,并具有潜在的抗坏死性和消炎性应用。
  10. GC49556 Cl-Necrostatin-1 A RIPK1 inhibitor
  11. GC63470 Eclitasertib Eclitasertib (DNL-758) 是一种受体相互作用蛋白激酶1 (RIPK1) 抑制剂,IC50 值为 <1 µμ(来自专利WO2017136727A2,example 42)。
  12. GC62997 GSK-872 hydrochloride A selective inhibitor of RIPK3
  13. GC62626 ICCB-19 hydrochloride ICCB-19 hydrochloride is an inhibitor of TNFRSF1A Associated Via Death Domain (TRADD) with IC50 of 1.12 μM and 2.01 μM for protecting Velcade-induced apoptosis in Jurkat cells and protecting RDA in MEFs, respectively. ICCB-19 indirectly inhibits Receptor-interacting serine/threonine-protein kinase 1 (RIPK1). ICCB-19 effectively induces autophagy.
  14. GC62455 RIPK3-IN-1 RIPK3-IN-1 是 II 型 RIPK3 DFG-out 位点抑制剂,IC50 为 9.1 nM。RIPK3-IN-1 抑制 RIPK1 和 RIPK2,IC50 为 5.5 和 >10 μM。RIPK3-IN-1 还是 c-Met 激酶抑制剂,IC50 为 1.1 μM。
  15. GC62316 Necrostatin-34 Necrostatin-34 (Nec-34) is a small molecule inhibitor of RIPK1 kinase with an IC50 of 0.13 μM in L929 cells.
  16. GC61215 PROTAC RIPK degrader-6 PROTACRIPKdegrader-6(example1)是一种PROTAC类的有效RIPK降解剂。
  17. GC60307 PROTAC RIPK degrader-2 PROTAC RIPK degrader-2 是一种非肽性PROTAC,它以丝氨酸苏氨酸激酶 RIPK2 为靶点,对 RIPK2 的降解具有高度选择性。
  18. GC50517 OD 36 hydrochloride OD 36 hydrochloride 是一种 RIPK2 抑制剂,IC50 为 5.3 nM。
  19. GC38841 RIPK1-IN-4 RIPK1-IN-4 (compound 8) 是一种有效的 II 型激酶受体相互作用蛋白1 (RIP1) 激酶抑制剂,并且与 DL1-out 无活性形式的 RIP1 结合,对于 RIP1 和 ADP-Glo 激酶,IC50 为分别为 16 nM 和 10 nM。
  20. GC38037 GSK2983559 free acid A RIPK2 inhibitor
  21. GC37537 RIPK-IN-4 RIPK-IN-4 是一种有效选择性的、具有良好的口服生物利用度的 RIPK2 抑制剂,IC50 值为 3 nM。
  22. GC37536 RIPK1-IN-7 RIPK1-IN-7 is a potent and selective receptor-interacting serine/threonine-protein kinase 1 (RIPK1) inhibitor with a Kd of 4 nM and an enzymatic IC50 of 11 nM.
  23. GC37535 RIPK1-IN-3 RIPK1-IN-3 (Example 38) 是RIPK1 的抑制剂,信息来自专利WO2018148626A1,拥有抗炎活性。
  24. GC37533 RIP1 kinase inhibitor 1 RIP1 kinase inhibitor 1 (compound 22) 是一种高效的,口服有效的,可穿透大脑的 RIP1 激酶抑制剂 (pKi=9.04)。
  25. GC36933 PK68 PK68 is a potent orally active and specific inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC50 of ~90?nM.
  26. GC36712 Necrostatin 2 S enantiomer Necrostatin 2 S enantiomer 是 Necrostatin 2 的 S 型异构体。Necrostatin 2 是高活性的坏死性凋亡抑制剂,为有效的 RIPK1 抑制剂,缺乏 IDO 靶向作用。
  27. GC36711 Necrostatin 2 racemate A RIPK1 inhibitor
  28. GC36189 GSK2983559

    A RIPK2 inhibitor

  29. GC36170 GNE684 GNE684 是一种有效的受体相互作用蛋白 1 (RIP1) 抑制剂,作用于人类、小鼠与大鼠 RIP1 的 Kiapp 值分别为 21 nM、189 nM 和 691 nM。
  30. GC15291 GSK3145095 GSK3145095 是一种 RIP1 激酶抑制剂,IC50 为 6.3 nM。
  31. GC34606 GSK-843 GSK-843是一种受体相互作用蛋白激酶3(RIP3orRIPK3)抑制剂,高亲和力结合RIP3激酶结构域,IC50值为8.6nM,并抑制激酶活性,IC50值为6.5nM。
  32. GC34605 GSK840

    GSK840(GSK’840)是一种受体相互作用蛋白激酶3(RIP3orRIPK3)抑制剂,高亲和力结合RIP3激酶结构域,IC50值为0.9nM,并抑制激酶活性,IC50值为0.3nM。

  33. GC34543 cRIPGBM cRIPGBM是RIPGBM的促凋亡衍生物,是通过与受体相互作用蛋白激酶2(RIPK2)结合,诱导GBM肿瘤干细胞凋亡的选择性诱导剂,对GBM-1细胞的EC50值为68nM。
  34. GC19503 GSK547 GSK547 (GSK'547) 是受体相互作用的丝氨酸/苏氨酸蛋白激酶 1 (RIPK1) 的高选择性和强效抑制剂,可抑制巨噬细胞介导的胰腺癌适应性免疫耐受。
  35. GC33620 Nec-4 Nec-4,一个三环衍生物,是受体相互作用蛋白1(RIP1)的一个有效抑制剂,其IC50值为2.6μM,Ki值为0.46μM。
  36. GC32860 RIP2 kinase inhibitor 2 RIP2kinaseinhibitor2是一种受体相互作用蛋白-2(RIP2)激酶抑制剂,详细信息请参考专利WO/2014043437A1中的化合物example9。
  37. GC32775 RIP2 kinase inhibitor 1 GSK2983559 active metabolite is an active metabolite of GSK2983559, also is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043446 A1, compound example 1.
  38. GC32280 HS-1371 A RIPK3 inhibitor
  39. GC31652 RIPA-56 A RIPK1 inhibitor
  40. GC19185 GSK583 A selective inhibitor of RIP2 kinase
  41. GC19182 GSK2982772 A RIPK1 inhibitor
  42. GC19175 GSK-872 A selective inhibitor of RIPK3
  43. GC18177 WEHI-345 An inhibitor of RIPK2
  44. GC15573 GSK481 A selective inhibitor of RIP1
  45. GC11167 Necrostatin 2 A potent inhibitor of necroptosis
  46. GC11008 Necrostatin-1

    A RIP1 kinase inhibitor

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