rip kinase

Necrostatin-1 (Nec-1) is a specific RIP1 inhibitor and necrotic apoptosis inhibitor, which inhibits TNF-α-induced necrotic apoptosis and also inhibits IDO.

Necrostatin-5 (Nec-5) is a selective RIP1 kinase inhibitor and cell necrosis inhibitor that prevents the death of Fadd-deficient Jurkat cells treated with TNF-α, with an EC50 of 240 nM.

GSK2593074A (GSK'074) is a programmed necrosis inhibitor that displays inhibitory effects on RIP1 and RIP3.

RIPK1-IN-9 is a potent and selective inhibitor of RIPK1, a dihydronaphthone compound, which inhibits U937 and L929 cells with an IC50 of 2 nM and 1.3 nM, respectively.

PK68 is an effective and selective inhibitor of type II receptor-interacting kinase 1 (RIPK1, IC50 = 90 nM). PK68 can be used for research on the treatment of inflammatory disorders and cancer metastasis.

RIPK1-IN-7 is a potent and selective inhibitor of RIPK1 (Kd of 4 nM and enzymatic IC50 of 11 nM), exhibiting excellent antimetastasis activity in the experimental B16 melanoma lung metastasis model.

GSK3145095 is an orally active inhibitor of RIPK1 with IC50 of 5 nM, with potential immunomodulatory activities and antineoplastic.

LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I.

OD36 is a selective and potent RIPK2 inhibitor with an IC50 of 5.3 nM.OD36 inhibits ALK2 signaling and osteogenic differentiation (KD: 37 nM), and binds efficiently to the ALK2 kinase ATP pocket.

GSK872 HCl(1346546-69-7 free base) (GSK2399872A) is an effective and specific RIP3 kinase inhibitor. It binds RIP3 kinase domain with high affinity (IC50: 1.8 nM) and inhibits kinase activity (IC50: 1.3 nM).

GSK963 (Racemate), a structurally distinct, potent and selective inhibitor of RIP1 kinase(IC50=29 nM).

GSK2983559 active metabolite (RIPK2-IN-1) is a potent, selective receptor-interacting protein-2 (RIP2) kinase inhibitor.

OD36 hydrochloride (OD-36 hydrochloride) is a potent RIPK2 inhibitor with an IC50 of 5.3 nM.OD36 hydrochloride is a macrocyclic inhibitor that binds efficiently to the ATP pocket of the ALK2 kinase and effectively antagonizes mutant ALK2 signaling and osteogenic differentiation.OD36 hydrochloride targets ALK2. OD36 hydrochloride targets ALK2 with a KD of 37 nM.

RIPK3-IN-1 is a selective and potent RIPK3 inhibitor (IC50: 9.1 nM) that inhibits the activities of c-Met kinase, RIPK1 and RIPK2.RIPK3-IN-1 has potential tumorigenic activity and can be used to study apoptosis.

HS-1371 is a novel kinase inhibitor of receptor-interacting protein kinase 3 (RIP3) with an IC50 of 20.8 nM.

SZM-1209 is a potent and specific RIPK1 inhibitor with oral activity, displaying a dissociation constant (Kd) of 85 nM. It demonstrates substantial anti-necroptotic efficacy with an EC50 of 22.4 ± 8.1 nM and possesses therapeutic effects against systemic inflammatory response syndrome (SIRS) and acute lung injury (ALI) [1].

SZM679 is an orally active, selective RIPK1 inhibitor displaying potent affinity with a dissociation constant (Kd) of 8.6 nM for RIPK1, while exhibiting minimal activity towards RIPK3, with a Kd of >5000 nM. It effectively counteracts tumor necrosis factor-induced systemic inflammation, reduces Tau hyperphosphorylation, diminishes neuroinflammation, and lowers RIPK1 phosphorylation in the hippocampus and cortex. SZM679 is utilized in Alzheimer's disease (AD) research [1].

RIPA-56 is an inhibitor of RIP1

RIP1 Kinase Inhibitor 4 (Compound 3) is an effective inhibitor of RIP1K, exhibiting an EC50 of ≤ 1000 nM [1].

RIP1 kinase inhibitor 5 (example 1) is a potent regulator of tumor immunity, inhibiting RIP1 and similarly to SIR1-365 (compound 13), suppresses necrosis and ferroptosis [2].

RIP1 Kinase Inhibitor 6 is a potent and selective inhibitor of RIP1 kinase, demonstrating inhibitory activity with an IC50 of less than 100 nM in a human R1P1 kinase assay[1].

RIP1 Kinase Inhibitor 7 (Compound 41) serves as a potent inhibitory agent for receptor interacting protein 1 kinase (RIP1) with an IC50 of under 100 nM. Additionally, it demonstrates an EC50 ranging from 1 to 100 nM in cell necrosis assays [1].

RIPK2 3-IN-1 is a potent inhibitor of both RIPK2 and RIPK3 kinases, exhibiting IC50 values of 3 nM for RIPK2 and 117 nM for RIPK3. Additionally, in a 14-TriLAN-Gly NOD1 THP-1 cell-based NF-κB reporter assay, RIPK2 3-IN-1 demonstrates an IC50 value of 14 ± 4 nM against RIPK2 [1].

RIPK3-IN-4 (Compound 42) is a RIPK3 inhibitor that mitigates necroptosis, inflammatory responses, and HK-2 cell damage. It alleviates acute kidney injury by attenuating Cisplatin- and I R-induced kidney damage, along with associated inflammatory responses and necroptosis [1].