RIP kinase Inhibitor

RIPK1-IN-4 (compound 8) is a potent and selective type II kinase inhibitor of receptor interacting protein 1 (RIP1) kinase and binds to a DLG-out inactive form of RIP1 with an IC₅₀s of 16 nM and 10 nM for RIP1 and ADP-Glo kinase.

GSK2983559 free acid (compound 3) is an orally active and potent receptor interacting protein 2 (RIP2) kinase inhibitor. GSK2983559 free acid can block many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples.

Zharp1-211 is a RIPK1 kinase inhibitor with an EC₅₀ of 53 nM and a K_d of 8.7 nM. Zharp1-211 reduces IFN-γ-induced STAT1 activation. Zharp1-211 can be used in the research of graft-versus-host disease and colon cancer.

PROTAC RIPK degrader-6 (Example 1) is a RIPK2 PROTAC degrader that recruits cereblon. PROTAC RIPK degrader-6 recruits the CRBN E3 ubiquitin ligase complex and induces the degradation of RIPK2 kinase via the ubiquitin-proteasome pathway, thereby blocking NOD1/NOD2-mediated pro-inflammatory signaling pathways of NF-κB and MAPK. PROTAC RIPK degrader-6 can be used in research related to RIPK2-mediated autoinflammatory diseases and cancer.

HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC₅₀ of 10.5 nM. HTH-01-091 also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 can be uesd for breast cancer research.

Flizasertib (GDC-8264) is an orally active, reversible and selective RIP1 inhibitor with K_i^app values of 0.00071 μM and 0.0013 μM for human and cynomolgus monkey RIP1 kinase, respectively. Flizasertib blocks RIP1 autophosphorylation but does not affect RIP1 protein stability. Flizasertib inhibits pro-inflammatory cytokines (CCL3, CCL4, and IL-1β) production. Flizasertib results in inhibition of colitis and ileitis. Flizasertib can be used in the research of cardiac surgery-associated acute kidney injury.

RIPK1-IN-17 is an orally active, selective RIPK1 inhibitor (K_d = 17 nM) and shows no significant inhibition to RIPK3. RIPK1-IN-17 specifically inhibits necroptosis rather than apoptosis by inhibiting RIPK1, RIPK3, and MLKL phosphorylation. RIPK1-IN-17 protects mice from hypothermia and death. RIPK1-IN-17 can be used for the study of necroptosis-related diseases such as inflammatory response syndrome (SIRS).

RIPK1 Human Pre-designed siRNA Set A contains three designed siRNAs for RIPK1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Necrostatin 2 S enantiomer is the S enantiomer of Necrostatin 2 (HY-14622). Necrostatin 2 S enantiomer inhibits TNF-α-induced necroptosis in Jurkat T cells. Necrostatin 2 S enantiomer can be used for the research of ischemic brain injury (stroke).

RIPK3-IN-3 (compound 20) is a selective inhibitor of RIP kinase RIPK3 (IC₅₀=10 nM). RIPK3 mediates the phosphorylation of Mixed Lineage Kinase (MLKL) and causes necroptosis, while RIPK3-IN-3 inhibits p-MLKL oligomerization and thereby inhibits necroptosis. RIPK3-IN-3 also downregulates CXCL5 secretion and inhibits AsPC-1 cell migration and invasion.

TP-030-2, a chemical probe, is a RIPK1 inhibitor (human K_i=0.43 nM; mouse IC₅₀=100 nM).

RIP1 kinase inhibitor 1 (compound 22) is a highly potent, orally available, and brain-penetrating RIP1 kinase inhibitor (pK_i=9.04).

Necroptosis-IN-1, an analog of Necrostatin-1, is a potent necroptosis inhibitor. Necroptosis-IN-1 is a RIPK inhibitor.

Ripk1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Ripk1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

RIPK1-IN-19 is a selective RIPK1 inhibitor (IC₅₀=15 nM). RIPK1-IN-19 does not show obvious activity against RIPK2, RIPK3, and RIPK4. RIPK1-IN-19 displays potent protective activity in TNFα-induced systemic inflammatory response syndrome (SIRS) model and Imiquimod (IMQ)-induced psoriasis model. RIPK1-IN-19 can be used in research on inflammation and immune system diseases.

GSK3145095 is a RIP1 kinase inhibitor with an IC₅₀ of 6.3 nM .

GNE684 is a potent inhibitor of potent receptor interacting protein 1 (RIP1), with mean K_i^app values of 21 nM, 189 nM and 691 nM for human mouse and rat RIP1, respectively.

KWCN-41 is a selective and efficient inhibitor of RIPK1 kinase with an IC₅₀ value of 88 nM. KWCN-41 specifically inhibits cell necrosis but does not inhibit apoptosis. KWCN-41 also has anti-inflammatory effects.

SZM679 is a potent, orally active and selective RIPK1 inhibitor with K_d values of 8.6 nM and >5000 nM for RIPK1 and RIPK3, respectively. SZM679 reverses the tumor necrosis factor-induced systemic inflammatory response. SZM679 decreases the Tau hyperphosphorylation, neuroinflammation, and the RIPK1 phosphorylation level in the hippocampus and cortex. SZM679 can be used in research of Alzheimer's disease (AD).

RIP2 kinase inhibitor 2 is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043437 A1, compound example 9.