RIP kinase

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S8037 Necrostatin-1 <1 mg/mL 51 mg/mL '<1 mg/mL
S2805 LY364947 <1 mg/mL 1 mg/mL <1 mg/mL
S6511 RIPA-56 <1 mg/mL 44 mg/mL 44 mg/mL
S8641 Necrostatin 2 racemate (Nec-1s) <1 mg/mL 56 mg/mL '9 mg/mL
E0301 Necrostatin-34 (Nec-34) <1 mg/mL 77 mg/mL <1 mg/mL
S8787 GSK'547 <1 mg/mL 29 mg/mL <1 mg/mL
S8484 GSK2982772 <1 mg/mL 75 mg/mL 30 mg/mL
S8642 GSK'963 <1 mg/mL 46 mg/mL 46 mg/mL
S8261 GSK583 <1 mg/mL 79 mg/mL '28 mg/mL
S8465 GSK'872 (GSK2399872A) <1 mg/mL 76 mg/mL '40 mg/mL
S8845 GSK3145095 <1 mg/mL 79 mg/mL 6 mg/mL
S9786 BDTX-189 <1 mg/mL 100 mg/mL ''''<1 mg/mL
S6078 ICCB-19 hydrochloride 58 mg/mL 58 mg/mL '''''58 mg/mL
S8775 HS-1371 <1 mg/mL 13 mg/mL 4 mg/mL
S8927 GSK2983559 (compound 3) <1 mg/mL 5 mg/mL <1 mg/mL
S9733 Mito-TEMPO ' mg/mL
S8169 GSK481 <1 mg/mL 75 mg/mL <1 mg/mL
S3238 Resibufogenin -1 mg/mL 100 mg/mL -1 mg/mL
S5584 Citronellol 31 mg/mL <1 mg/mL -1 mg/mL

亜型選択性的な製品

RIP kinase製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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.

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.

S6511

RIPA-56

RIPA-56 is a highly-potent, selective, and metabolically stable RIP1 (RIPK1) inhibitor.

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.

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.

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

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.

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.

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.

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.

S8845

GSK3145095

GSK3145095 is a potent and orally active RIP1 kinase inhibitor with IC50 of 6.3 nM with potential antineoplastic and immunomodulatory activities.

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.

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.

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.

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.

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.

S8169

GSK481

GSK481 is a RIP1(Receptor Interacting Protein Kinase1) inhibitor. Inhibition of RIP1 has been shown to hinder cell necrotic death.

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.

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.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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.

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.

S6511

RIPA-56

RIPA-56 is a highly-potent, selective, and metabolically stable RIP1 (RIPK1) inhibitor.

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.

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.

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

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.

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.

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.

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.

S8845

GSK3145095

GSK3145095 is a potent and orally active RIP1 kinase inhibitor with IC50 of 6.3 nM with potential antineoplastic and immunomodulatory activities.

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.

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.

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.

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.

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.

S8169

GSK481

GSK481 is a RIP1(Receptor Interacting Protein Kinase1) inhibitor. Inhibition of RIP1 has been shown to hinder cell necrotic death.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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.

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.

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