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. |
|
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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
|
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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. |
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S6511 |
RIPA-56
|
RIPA-56 is a highly-potent, selective, and metabolically stable RIP1 (RIPK1) inhibitor. |
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Cancer Cell Int, 2020, 30;20:36
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Biochem Biophys Res Commun, 2020, 10.1016/j.bbrc.2020.02.072
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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. |
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Cell Metab, 2022, S1550-4131(22)00054-7
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Bone Res, 2022, 10(1):26
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Cell Death Dis, 2022, 13(2):147
|
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S8169 |
GSK481
|
GSK481 is a RIP1(Receptor Interacting Protein Kinase1, RIPK1) inhibitor. Inhibition of RIP1 has been shown to hinder cell necrotic death. |
|
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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
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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
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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
|
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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
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Cell Host Microbe, 2021, S1931-3128(21)00192-X
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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. |
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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. |
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Phytomedicine, 2022, 102:154182
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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. |
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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. |
|
|