RIP kinase

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RIP kinase Products

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Catalog No. Product Name Information Product Use Citations Product Validations
E0301New Necrostatin-34 (Nec-34) Necrostatin-34 (Nec-34) is a small molecule inhibitor of RIPK1 kinase with an IC50 of 0.13 μM in L929 cells.
S2805 LY364947 LY364947 (HTS 466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM in a cell-free assay, shows 7-fold selectivity over TGFβR-II.
Cell Rep, 2022, 38(5):110329
Front Immunol, 2022, 13:853894
Aging Dis, 2022, 13(1):313-328
S6078 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.
S6511 RIPA-56 RIPA-56 is a highly-potent, selective, and metabolically stable RIP1 (RIPK1) inhibitor.
Cancer Cell Int, 2020, 30;20:36
Biochem Biophys Res Commun, 2020, 10.1016/j.bbrc.2020.02.072
S8037 Necrostatin-1 Necrostatin-1 (Nec-1) is a specific RIP1 (RIPK1) inhibitor and inhibits TNF-α-induced necroptosis with EC50 of 490 nM in 293T cells. Necrostatin-1 also blocks IDO and suppresses autophagy and apoptosis.
Cell Metab, 2022, S1550-4131(22)00054-7
Bone Res, 2022, 10(1):26
Cell Death Dis, 2022, 13(2):147
S8169 GSK481 GSK481 is a RIP1(Receptor Interacting Protein Kinase1, RIPK1) inhibitor. Inhibition of RIP1 has been shown to hinder cell necrotic death.
S8261 GSK583 GSK583 is a highly potent and selective inhibitor of RIP2 kinase with IC50 of 5 nM. GSK583 also inhibits both TNF-α and IL-6 production with IC50 of ~200 nM in explant cultures.
Cancer Res, 2020, canres.530.2020
J Neuroinflammation, 2020, 17(1):364
S8465 GSK'872 (GSK2399872A) GSK'872 (GSK2399872A) is a potent and selective RIP3 kinase inhibitor which binds RIP3 kinase domain with high affinity (IC50=1.8 nM) and inhibits kinase activity with IC50 of 1.3 nM. It has minimal cross-reactivity.
Cell Metab, 2022, S1550-4131(22)00054-7
J Cell Biol, 2022, 221(6)e202109038
Cell Death Dis, 2022, 13(2):188
S8484 GSK2982772 GSK2982772 is an ATP competitive receptor-interacting protein-1 (RIP1) kinase (RIPK1) inhibitor with the IC50 value of 16 nM. It has exquisite kinase specificity and excellent activity in blocking many TNF-dependent cellular responses.
Antioxidants (Basel), 2021, 10(9)1347
Mol Cell Biochem, 2021, 10.1007/s11010-021-04136-y
Exp Ther Med, 2021, 21(2):163
S8641 Necrostatin 2 racemate (Nec-1s) Necrostatin 2 racemate (Nec-1s, 7-Cl-O-Nec1, Necrostatin-1 stable, Necrostatin 1S) is a stable variant of Necrostatin-1. It is a more specific RIPK1 inhibitor lacking the IDO-targeting effect, with >1000-fold more selective for RIPK1 than for any other kinase out of 485 human kinases.
PLoS One, 2022, 17(4):e0257408
Biochem Biophys Res Commun, 2022, 611:151-157
Commun Biol, 2022, 5(1):47
S8642 GSK'963 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.
Sci Transl Med, 2021, 13(622):eabb5445
Cell Host Microbe, 2021, S1931-3128(21)00192-X
S8775 HS-1371 HS-1371 is a potent RIP3 kinase inhibitor with an IC50 of 20.8 nM. It binds to the ATP binding pocket of RIP3 and inhibits ATP binding to prevent RIP3 enzymatic activity in vitro.
Oncogene, 2021, 10.1038/s41388-021-01869-4
S8787 GSK'547 GSK'547 is a highly selective and potent inhibitor of RIP1 (RIPK1) exhibiting a 400-fold improvement in mouse pharmacokinetic oral exposure compared with GSK'963
J Neuroinflammation, 2022, 19(1):109
S8845 GSK3145095 GSK3145095 is a potent and orally active RIP1 kinase inhibitor with IC50 of 6.3 nM with potential antineoplastic and immunomodulatory activities.
S8927 GSK2983559 (compound 3) GSK2983559 (compound 3, RIP2 kinase inhibitor 1, RIPK2-IN-1) is a potent inhibitor of receptor interacting protein 2 (RIP2) kinase with good kinase specificity.
Aging (Albany NY), 2021, 13(7):10450-10467
Cancer Research on Prevention and Treatment, 2020, (7): 492-497
S9733 Mito-TEMPO Mito-TEMPO (MT), a mitochondria-targeted superoxide dismutase mimetic, protects against the early phase of acetaminophen (APAP) hepatotoxicity by inhibiting peroxynitrite formation. Mito-TEMPO treatment inhibits APAP-induced RIP3 kinase expression.
Front Cell Dev Biol, 2022, 10:806081
Food Chem Toxicol, 2022, 163:112966
Toxicol Appl Pharmacol, 2022, 439:115929
S9786 BDTX-189 BDTX-189 is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations with Kd of 0.2 nM, 0.76 nM, 13 nM and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. BDTX-189 exhibits anticancer activity.
S3238 Resibufogenin Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.
Phytomedicine, 2022, 102:154182
S5584 Citronellol Citronellol (Dihydrogeraniol, (±)-β-Citronellol), a constituent of rose and geranium oils, is used in perfumes and insect repellents. Citronellol can cause necrotic apoptosis of NCI-H1299 cells by up-regulating TNF-α, RIP1 / RIP3 activities, and down-regulating caspase-3 / caspase-8 activities. Citronellol also results in a biphasic increase in ROS production at 1 h and at 12 h in NCI-H1299 cells.
E0301New Necrostatin-34 (Nec-34) Necrostatin-34 (Nec-34) is a small molecule inhibitor of RIPK1 kinase with an IC50 of 0.13 μM in L929 cells.
S2805 LY364947 LY364947 (HTS 466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM in a cell-free assay, shows 7-fold selectivity over TGFβR-II.
Cell Rep, 2022, 38(5):110329
Front Immunol, 2022, 13:853894
Aging Dis, 2022, 13(1):313-328
S6078 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.
S6511 RIPA-56 RIPA-56 is a highly-potent, selective, and metabolically stable RIP1 (RIPK1) inhibitor.
Cancer Cell Int, 2020, 30;20:36
Biochem Biophys Res Commun, 2020, 10.1016/j.bbrc.2020.02.072
S8037 Necrostatin-1 Necrostatin-1 (Nec-1) is a specific RIP1 (RIPK1) inhibitor and inhibits TNF-α-induced necroptosis with EC50 of 490 nM in 293T cells. Necrostatin-1 also blocks IDO and suppresses autophagy and apoptosis.
Cell Metab, 2022, S1550-4131(22)00054-7
Bone Res, 2022, 10(1):26
Cell Death Dis, 2022, 13(2):147
S8169 GSK481 GSK481 is a RIP1(Receptor Interacting Protein Kinase1, RIPK1) inhibitor. Inhibition of RIP1 has been shown to hinder cell necrotic death.
S8261 GSK583 GSK583 is a highly potent and selective inhibitor of RIP2 kinase with IC50 of 5 nM. GSK583 also inhibits both TNF-α and IL-6 production with IC50 of ~200 nM in explant cultures.
Cancer Res, 2020, canres.530.2020
J Neuroinflammation, 2020, 17(1):364
S8465 GSK'872 (GSK2399872A) GSK'872 (GSK2399872A) is a potent and selective RIP3 kinase inhibitor which binds RIP3 kinase domain with high affinity (IC50=1.8 nM) and inhibits kinase activity with IC50 of 1.3 nM. It has minimal cross-reactivity.
Cell Metab, 2022, S1550-4131(22)00054-7
J Cell Biol, 2022, 221(6)e202109038
Cell Death Dis, 2022, 13(2):188
S8484 GSK2982772 GSK2982772 is an ATP competitive receptor-interacting protein-1 (RIP1) kinase (RIPK1) inhibitor with the IC50 value of 16 nM. It has exquisite kinase specificity and excellent activity in blocking many TNF-dependent cellular responses.
Antioxidants (Basel), 2021, 10(9)1347
Mol Cell Biochem, 2021, 10.1007/s11010-021-04136-y
Exp Ther Med, 2021, 21(2):163
S8641 Necrostatin 2 racemate (Nec-1s) Necrostatin 2 racemate (Nec-1s, 7-Cl-O-Nec1, Necrostatin-1 stable, Necrostatin 1S) is a stable variant of Necrostatin-1. It is a more specific RIPK1 inhibitor lacking the IDO-targeting effect, with >1000-fold more selective for RIPK1 than for any other kinase out of 485 human kinases.
PLoS One, 2022, 17(4):e0257408
Biochem Biophys Res Commun, 2022, 611:151-157
Commun Biol, 2022, 5(1):47
S8642 GSK'963 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.
Sci Transl Med, 2021, 13(622):eabb5445
Cell Host Microbe, 2021, S1931-3128(21)00192-X
S8775 HS-1371 HS-1371 is a potent RIP3 kinase inhibitor with an IC50 of 20.8 nM. It binds to the ATP binding pocket of RIP3 and inhibits ATP binding to prevent RIP3 enzymatic activity in vitro.
Oncogene, 2021, 10.1038/s41388-021-01869-4
S8787 GSK'547 GSK'547 is a highly selective and potent inhibitor of RIP1 (RIPK1) exhibiting a 400-fold improvement in mouse pharmacokinetic oral exposure compared with GSK'963
J Neuroinflammation, 2022, 19(1):109
S8845 GSK3145095 GSK3145095 is a potent and orally active RIP1 kinase inhibitor with IC50 of 6.3 nM with potential antineoplastic and immunomodulatory activities.
S8927 GSK2983559 (compound 3) GSK2983559 (compound 3, RIP2 kinase inhibitor 1, RIPK2-IN-1) is a potent inhibitor of receptor interacting protein 2 (RIP2) kinase with good kinase specificity.
Aging (Albany NY), 2021, 13(7):10450-10467
Cancer Research on Prevention and Treatment, 2020, (7): 492-497
S9733 Mito-TEMPO Mito-TEMPO (MT), a mitochondria-targeted superoxide dismutase mimetic, protects against the early phase of acetaminophen (APAP) hepatotoxicity by inhibiting peroxynitrite formation. Mito-TEMPO treatment inhibits APAP-induced RIP3 kinase expression.
Front Cell Dev Biol, 2022, 10:806081
Food Chem Toxicol, 2022, 163:112966
Toxicol Appl Pharmacol, 2022, 439:115929
S9786 BDTX-189 BDTX-189 is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations with Kd of 0.2 nM, 0.76 nM, 13 nM and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. BDTX-189 exhibits anticancer activity.
S3238 Resibufogenin Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.
Phytomedicine, 2022, 102:154182
S5584 Citronellol Citronellol (Dihydrogeraniol, (±)-β-Citronellol), a constituent of rose and geranium oils, is used in perfumes and insect repellents. Citronellol can cause necrotic apoptosis of NCI-H1299 cells by up-regulating TNF-α, RIP1 / RIP3 activities, and down-regulating caspase-3 / caspase-8 activities. Citronellol also results in a biphasic increase in ROS production at 1 h and at 12 h in NCI-H1299 cells.
E0301New Necrostatin-34 (Nec-34) Necrostatin-34 (Nec-34) is a small molecule inhibitor of RIPK1 kinase with an IC50 of 0.13 μM in L929 cells.
Tags: RIP kinase inhibitor|RIP kinase agonist|RIP kinase activator|RIP kinase inducer|RIP kinase antagonist|RIP kinase signaling pathway|RIP kinase assay kit