RIP kinase

Inhibitory Selectivity

RIP kinase Products

Catalog No. Information Product Use Citations Product Validations
S8037

Necrostatin-1

Necrostatin-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 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

Nec-1s (7-Cl-O-Nec1)

Nec-1s (7-Cl-O-Nec1, Necrostatin-1 stable) 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.

S8845New

GSK3145095

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

S8927New

GSK2983559 (compound 3)

GSK2983559 is a potent inhibitor of receptor interacting protein 2 (RIP2) kinase with good kinase specificity.

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

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.

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.

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.

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.

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.

S8169

GSK481

GSK481 is a RIP1(Receptor Interacting Protein Kinase1, RIPK1) inhibitor. Inhibition of RIP1 has been shown to hinder cell necrotic death.

S3238New

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, 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.

Catalog No. Information Product Use Citations Product Validations
S8037

Necrostatin-1

Necrostatin-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 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

Nec-1s (7-Cl-O-Nec1)

Nec-1s (7-Cl-O-Nec1, Necrostatin-1 stable) 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.

S8845New

GSK3145095

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

S8927New

GSK2983559 (compound 3)

GSK2983559 is a potent inhibitor of receptor interacting protein 2 (RIP2) kinase with good kinase specificity.

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

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.

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.

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.

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.

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.

S8169

GSK481

GSK481 is a RIP1(Receptor Interacting Protein Kinase1, RIPK1) inhibitor. Inhibition of RIP1 has been shown to hinder cell necrotic death.

Catalog No. Information Product Use Citations Product Validations
S3238New

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, 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.