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Home >> Signaling Pathways >> Apoptosis >> RIP kinase

RIP kinase

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.

Targets for  RIP kinase

Products for  RIP kinase

  1. Cat.No. Product Name Information
  2. GC65004 Apostatin-1

    Apt-1

     Apostatin-1 (Apt-1) is a potent TRADD inhibitor. Apostatin-1 Chemical Structure
  3. GC49556 Cl-Necrostatin-1

    7-Cl-Nec-1, 7-Cl-Necrostatin-1, Nec-1f

     A RIPK1 inhibitor Cl-Necrostatin-1 Chemical Structure
  4. GC34543 cRIPGBM cRIPGBM, a proapoptotic derivative of RIPGBM, a cell type-selective inducer of apoptosis in GBM cancer stem cells (CSCs) by binding to receptor-interacting protein kinase 2 (RIPK2), with an EC50 of 68 nM in GBM-1 cells. cRIPGBM Chemical Structure
  5. GC68903 cRIPGBM chloride

    cRIPGBM chloride is an orally effective pro-apoptotic derivative that can be produced from cancer stem cells (CSC) of glioblastoma multiforme (GBM). cRIPGBM chloride induces caspase 1-dependent cell apoptosis by targeting receptor-interacting protein kinase 2 (RIPK2) through the formation of RIPK2/caspase 1 complex and inhibition of RIPK2/TAK1 (pro-survival complex) formation. In animal models, cRIPGBM chloride exhibits strong in vivo anti-tumor activity.

     cRIPGBM chloride Chemical Structure
  6. GC63470 Eclitasertib

    DNL-758; SAR-443122

     Eclitasertib (DNL-758) is a potent receptor-interacting protein kinase 1 (RIPK1) inhibitor with an IC50 of <1 ?Μ (From patent WO2017136727A2, example 42). Eclitasertib Chemical Structure
  7. GC36170 GNE684 GNE684 is a potent inhibitor of potent receptor interacting protein 1 (RIP1), with mean Kiapp values of 21 nM, 189 nM and 691 nM for human mouse and rat RIP1, respectively. GNE684 Chemical Structure
  8. GC34606 GSK-843

    GSK'843

     GSK-843 (GSK'843) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 8.6 nM, and inhibits kinase activity with an IC50 of 6.5 nM. GSK-843 Chemical Structure
  9. GC19175 GSK-872 GSK-872 is a RIPK3 inhibitor. GSK-872 Chemical Structure
  10. GC62997 GSK-872 hydrochloride GSK-872 hydrochloride is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 hydrochloride Chemical Structure
  11. GC66479 GSK2593074A

    GSK'074

     GSK2593074A (GSK'074) is a necroptosis inhibitor with dual targeting ability to both RIP1 and RIP3. GSK2593074A Chemical Structure
  12. GC19182 GSK2982772 GSK2982772 is a potent and ATP competitive RIP1 inhibitor with an IC50 of 16 nM. GSK2982772 Chemical Structure
  13. GC36189 GSK2983559 A RIPK2 inhibitor GSK2983559 Chemical Structure
  14. GC38037 GSK2983559 free acid A RIPK2 inhibitor GSK2983559 free acid Chemical Structure
  15. GC15291 GSK3145095

    GSK3145095 is a RIP1 kinase inhibitor

     GSK3145095 Chemical Structure
  16. GC15573 GSK481 RIP1(Receptor Interacting Protein Kinase 1) inhibitor GSK481 Chemical Structure
  17. GC19503 GSK547

    GSK'547

    GSK547, a highly selective and potent RIP1 inhibitor

     GSK547 Chemical Structure
  18. GC19185 GSK583 GSK583 is a highly potent and selective inhibitor of RIP2 Kinase, with IC50 of 5 nM. GSK583 Chemical Structure
  19. GC34605 GSK840

    GSK'840

     GSK840 (GSK'840) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 0.9 nM, and inhibits kinase activity with an IC50 of 0.3 nM. GSK840 Chemical Structure
  20. GC64951 GSK963 GSK963 is a chiral, highly potent and selective inhibitor of RIP1 kinase, with an IC50 of 29 nM. GSK963 Chemical Structure
  21. GC32280 HS-1371 A RIPK3 inhibitor HS-1371 Chemical Structure
  22. GC72931 HTH-01-091 TFA HTH-01-091 TFA is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. HTH-01-091 TFA Chemical Structure
  23. GC62626 ICCB-19 hydrochloride ICCB-19 hydrochloride is a TRADD (TNFRSF1A associated via death domain) inhibitor. ICCB-19 hydrochloride Chemical Structure
  24. GC64370 Kongensin A Kongensin A is a natural product isolated from Croton kongensis. Kongensin A Chemical Structure
  25. GC33620 Nec-4 Nec-4, a tricyclic derivative, is a potent receptor interacting protein 1 (RIP1) inhibitor, with an IC50 of 2.6 μM, Ki of 0.46 μM. Nec-4 Chemical Structure
  26. GC11167 Necrostatin 2

    Cl-Necrostatin analog

     A potent inhibitor of necroptosis Necrostatin 2 Chemical Structure
  27. GC36711 Necrostatin 2 racemate

    7-Cl-O-Nec-1, Nec-1s

     A RIPK1 inhibitor Necrostatin 2 racemate Chemical Structure
  28. GC36712 Necrostatin 2 S enantiomer Necrostatin 2 S enantiomer is the S enantiomer of Necrostatin 2. Necrostatin 2 S enantiomer Chemical Structure
  29. GC11008 Necrostatin-1

    MTH-DL-Tryptophan,Nec-1

     Necrostatin-1 mainly acts on RIP1 in cells [5], Necrostatin-1 is a RIP1 kinase inhibitor with an IC50 value of 0.32 mM. Necrostatin-1 Chemical Structure
  30. GC62316 Necrostatin-34 Necrostatin-34 (Nec-34), a RIPK1 kinase inhibitor, stabilizes RIPK1 kinase in an inactive conformation by occupying a distinct binding pocket in the kinase domain. Necrostatin-34 Chemical Structure
  31. GC50517 OD 36 hydrochloride OD 36 hydrochloride is a RIPK2 inhibitor with an IC50 of 5.3 nM. OD 36 hydrochloride Chemical Structure
  32. GC71050 Oditrasertib Oditrasertib is a receptor-interacting protein kinase 1 (RIPK1) inhibitor with an IC50 value lower than 100 nM. Oditrasertib Chemical Structure
  33. GC36933 PK68 PK68 is a potent orally active and specifical type II inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC50 of ~90?nM, displays inhibition of RIPK1-dependent necroptosis. PK68 Chemical Structure
  34. GC60307 PROTAC RIPK degrader-2 PROTAC RIPK degrader-2 is a nonpeptidic PROTAC based on von Hippel-Lindau ligand which potently targets serine-threonine kinase RIPK2 and has highly selective for RIPK2 degradation. PROTAC RIPK degrader-2 Chemical Structure
  35. GC61215 PROTAC RIPK degrader-6 PROTAC RIPK degrader-6 (example 1) is a Cereblon-based PROTAC targeting RIP Kinase degradation wherein the RIP2 kinase inhibitor is linked via a linker to a cereblon binder. PROTAC RIPK degrader-6 Chemical Structure
  36. GC37533 RIP1 kinase inhibitor 1 RIP1 kinase inhibitor 1 (compound 22) is a highly potent, orally available, and brain-penetrating RIP1 kinase inhibitor (pKi=9.04). RIP1 kinase inhibitor 1 Chemical Structure
  37. GC67969 RIP1/RIP3/MLKL activator 1 RIP1/RIP3/MLKL activator 1 Chemical Structure
  38. GC32775 RIP2 kinase inhibitor 1 RIP2 kinase inhibitor 1 is an active metabolite of GSK2983559. RIP2 kinase inhibitor 1 is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043446 A1, compound example 1. RIP2 kinase inhibitor 1 Chemical Structure
  39. GC32860 RIP2 kinase inhibitor 2 RIP2 kinase inhibitor 2 is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043437 A1, compound example 9. RIP2 kinase inhibitor 2 Chemical Structure
  40. GC65967 RIP2 Kinase Inhibitor 3 RIP2 Kinase Inhibitor 3 is a highly potent and selective inhibitor of receptor interacting protein-2 (RIP2) Kinase with an IC50 of 1 nM . RIP2 Kinase Inhibitor 3 Chemical Structure
  41. GC31652 RIPA-56 A RIPK1 inhibitor RIPA-56 Chemical Structure
  42. GC37537 RIPK-IN-4 RIPK-IN-4 is a potent and selective RIPK2 inhibitor with excellent oral bioavailability, and has an IC50 of 3 nM. RIPK-IN-4 Chemical Structure
  43. GC65467 RIPK1-IN-10 RIPK1-IN-10 is a potent RIPK1 inhibitor, example 37, extracted from patent WO2021160109. RIPK1-IN-10 Chemical Structure
  44. GC73725 RIPK1-IN-17 RIPK1/3-IN-17 (Compound 10) is a RIPK1 and RIPK3 inhibitor. RIPK1-IN-17 Chemical Structure
  45. GC37535 RIPK1-IN-3 RIPK1-IN-3 (Example 38), a RIPK1 inhibitor, extracted from patent WO2018148626A1, possesses anti-inflammatory proprieties. RIPK1-IN-3 Chemical Structure
  46. GC38841 RIPK1-IN-4 RIPK1-IN-4 (compound 8) is a potent and selective type II kinase inhibitor of receptor interacting protein 1 (RIP1) kinase and binds to a DLG-out inactive form of RIP1 with an IC50s of 16 nM and 10 nM for RIP1 and ADP-Glo kinase. RIPK1-IN-4 Chemical Structure
  47. GC37536 RIPK1-IN-7 RIPK1-IN-7 is a potent and selective RIPK1 inhibitor with a Kd of 4 nM and an enzymatic IC50 of 11 nM. RIPK1-IN-7 exhibits excellent antimetastasis activity in the experimental B16 melanoma lung metastasis model. RIPK1-IN-7 Chemical Structure
  48. GC70875 RIPK1-IN-9 RIPK1-IN-9 (example 45), a dihydronaphthyridone compound, is a potent and selective RIPK1 inhibitor. RIPK1-IN-9 Chemical Structure
  49. GC62455 RIPK3-IN-1 RIPK3-IN-1 is a RIPK3 type II DFG-out inhibitor with an IC50 of 9.1 nM. RIPK3-IN-1 Chemical Structure
  50. GC90886 SZM-1209

    A RIPK1 inhibitor

     SZM-1209 Chemical Structure
  51. GC71180 SZM679 SZM679 is a potent, orally active and selective RIPK1 inhibitor with Kd values of 8.6 nM and >5000 nM for RIPK1 and RIPK3, respectively. SZM679 Chemical Structure
  52. GC18177 WEHI-345 WEHI-345 is an inhibitor of receptor-interacting protein kinase 2 (RIPK2; IC50 = 130 nM in a kinase assay using human recombinant RIPK2). WEHI-345 Chemical Structure
  53. GC71355 Zharp2-1 Zharp2-1 is an oral effective RIPK2 inhibitor, highly associated with inflammatory bowel disease (IBD). Zharp2-1 Chemical Structure

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