RIP kinase

RIP kinase製品

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  • RIP kinase阻害剤 (21)
  • RIP kinase活性剤(2)
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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.
Antioxidants (Basel), 2024, 13(1)114
Heliyon, 2024, 10(1):e23426
J Cancer, 2024, 15(3):685-698
S8465 GSK'872 GSK'872 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.
Nat Commun, 2024, 15(1):1282
Redox Biol, 2024, 69:103008
Ecotoxicol Environ Saf, 2024, 270:115860
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.
Nature, 2024, 626(7998):411-418.
iScience, 2024, 27(2):108766
Cell, 2023, 186(13):2783-2801.e20
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.
Adv Sci (Weinh), 2024, 11(4):e2304987
Cell Rep Med, 2024, 5(2):101416
Cell Rep, 2023, 42(6):112566
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.
Nat Commun, 2024, 15(1):1669
Exp Mol Med, 2024, 56(2):408-421.
Cell Mol Life Sci, 2024, 81(1):88
S6511 RIPA-56 RIPA-56 is a highly-potent, selective, and metabolically stable RIP1 (RIPK1) inhibitor.
Ann Transl Med, 2022, 10(22):1245
J Oncol, 2022, 2022:2390078
Cancer Cell Int, 2020, 30;20:36
S8484 GSK2982772 GSK2982772 is an ATP competitive receptor-interacting protein-1 (RIP1) kinase inhibitor with the IC50 value of 1 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
S8642 GSK'963 GSK'963 is a chiral small-molecule inhibitor of RIP1 kinase with an IC50 of 29 nM in FP binding assays. It is >10 000-fold selective for RIP1 over 339 other kinases.
Sci Rep, 2024, 14(1):4409
Cell Host Microbe, 2021, S1931-3128(21)00192-X
Sci Transl Med, 2021, 13(622):eabb5445
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
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
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.
Research Square, 2024, 10.21203/rs.3.rs-3790060/v1
Phytomedicine, 2022, 102:154182
S8787 GSK'547 GSK'547 is a highly selective and potent inhibitor of RIP1 exhibiting a 400-fold improvement in mouse pharmacokinetic oral exposure compared with GSK'963
J Neuroinflammation, 2022, 19(1):109
S9786 Tuxobertinib (BDTX-189) Tuxobertinib (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.
J Transl Med, 2023, 21(1):89
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.
Cell Death Discov, 2023, 9(1):109
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
S8169 GSK481 GSK481 is a RIP1(Receptor Interacting Protein Kinase1) inhibitor. Inhibition of RIP1 has been shown to hinder cell necrotic death.
J Oncol, 2022, 2022:2390078
E2822 GSK2983559 active metabolite 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.
E2367 PK68 PK68 is a potent orally active and specific inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC50 of ~90 nM.
S8845 GSK3145095 GSK3145095 is a potent and orally active RIP1 kinase inhibitor with IC50 of 6.3 nM with potential antineoplastic and immunomodulatory activities.
E0301 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.

E2648 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.
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.
E1734New OD36 OD36 is an inhibitor of RIPK2 with an IC50 value of 5.3 nM. OD36 is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket.
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.
Antioxidants (Basel), 2024, 13(1)114
Heliyon, 2024, 10(1):e23426
J Cancer, 2024, 15(3):685-698
S8465 GSK'872 GSK'872 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.
Nat Commun, 2024, 15(1):1282
Redox Biol, 2024, 69:103008
Ecotoxicol Environ Saf, 2024, 270:115860
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.
Nature, 2024, 626(7998):411-418.
iScience, 2024, 27(2):108766
Cell, 2023, 186(13):2783-2801.e20
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.
Adv Sci (Weinh), 2024, 11(4):e2304987
Cell Rep Med, 2024, 5(2):101416
Cell Rep, 2023, 42(6):112566
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.
Nat Commun, 2024, 15(1):1669
Exp Mol Med, 2024, 56(2):408-421.
Cell Mol Life Sci, 2024, 81(1):88
S6511 RIPA-56 RIPA-56 is a highly-potent, selective, and metabolically stable RIP1 (RIPK1) inhibitor.
Ann Transl Med, 2022, 10(22):1245
J Oncol, 2022, 2022:2390078
Cancer Cell Int, 2020, 30;20:36
S8484 GSK2982772 GSK2982772 is an ATP competitive receptor-interacting protein-1 (RIP1) kinase inhibitor with the IC50 value of 1 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
S8642 GSK'963 GSK'963 is a chiral small-molecule inhibitor of RIP1 kinase with an IC50 of 29 nM in FP binding assays. It is >10 000-fold selective for RIP1 over 339 other kinases.
Sci Rep, 2024, 14(1):4409
Cell Host Microbe, 2021, S1931-3128(21)00192-X
Sci Transl Med, 2021, 13(622):eabb5445
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
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
S8787 GSK'547 GSK'547 is a highly selective and potent inhibitor of RIP1 exhibiting a 400-fold improvement in mouse pharmacokinetic oral exposure compared with GSK'963
J Neuroinflammation, 2022, 19(1):109
S9786 Tuxobertinib (BDTX-189) Tuxobertinib (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.
J Transl Med, 2023, 21(1):89
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.
Cell Death Discov, 2023, 9(1):109
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
S8169 GSK481 GSK481 is a RIP1(Receptor Interacting Protein Kinase1) inhibitor. Inhibition of RIP1 has been shown to hinder cell necrotic death.
J Oncol, 2022, 2022:2390078
E2822 GSK2983559 active metabolite 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.
E2367 PK68 PK68 is a potent orally active and specific inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC50 of ~90 nM.
S8845 GSK3145095 GSK3145095 is a potent and orally active RIP1 kinase inhibitor with IC50 of 6.3 nM with potential antineoplastic and immunomodulatory activities.
E0301 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.

E2648 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.
E1734New OD36 OD36 is an inhibitor of RIPK2 with an IC50 value of 5.3 nM. OD36 is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket.
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.
Research Square, 2024, 10.21203/rs.3.rs-3790060/v1
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.
E1734New OD36 OD36 is an inhibitor of RIPK2 with an IC50 value of 5.3 nM. OD36 is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket.

RIP kinase阻害剤の選択性比較

Tags: RIP kinase inhibitor|RIP kinase agonist|RIP kinase activator|RIP kinase inducer|RIP kinase antagonist|RIP kinase signaling pathway|RIP kinase assay kit