Mcl1-IN-8 (Comp8) is a Mcl-1-PUMA interface inhibitor, with a Ki of 0.3 μM. Mcl1-IN-8 (Comp8) exhibits dual activity on reduce PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis in cancer cells.
DRAK2-IN-1, compound 16, is a potent, selective and ATP-competitive DRAK2 inhibitor with IC50and Kivalues of 3 nM and 0.26 nM, respectively. DRAK2-IN-1 also has inbitory effect on DRAK1 (IC50=51 nM).
GSK-843 (GSK'843) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 8.6 nM, and inhibits kinase activity with an IC50 of 6.5 nM.
PK68 is a potent and selective type II inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC50 of ~90?nM, displays inhibition of RIPK1-dependent necroptosis.
C25-140, a first-in-class, fairly selective TRAF6-Ubc13 inhibitor, directly binds to TRAF6, and blocks the interaction of TRAF6 with Ubc13. C25-140 lowers TRAF6 activity, reduces NF-κB activation, and combats autoimmunity.
PROTAC MDM2 Degrader-4 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-4 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
PROTAC MDM2 Degrader-2 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-2 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na+/H+ exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells.
RIPK1-IN-7 is a potent and selective RIPK1 inhibitor with a Kd of 4 nM and an enzymatic IC50 of 11 nM. RIPK1-IN-7 exhibits excellent antimetastasis activity in the experimental B16 melanoma lung metastasis model.
RET-IN-1 is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 552, has IC50s of 1 nM, 7 nM, and 101 nM for RET (WT), RET (V804M) , and RET (G810R), respectively .
GSK547 (GSK-547) is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIP1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer.
MitoTam bromide, hydrobromide is a tamoxifen derivative, an electron transport chain (ETC) inhibitor, spreduces mitochondrial membrane potential in senescent cells and affects mitochondrial morphology.
GSK2982772 is a potent, orally active and ATP competitive RIP1 kinase inhibitor with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively.
Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycete, acts as an XBP1 inhibitor, inhibits IRE1α-induced ATP-dependent XBP1 mRNA cleavage, with an IC50 of 80 nM.
BI-6C9 is a BH3 interacting domain (Bid) inhibitor, which prevents mitochondrial outer membrane potential (MOMP) and mitochondrial fission, and protects the cells from cell death.
TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination.
ZYZ-488 is a competitive apoptotic protease activating factor-1 (Apaf-1) inhibitor, which inhibits the activation of binding protein procaspase-9 and procaspase-3.
GGTI298 is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, strongly inhibiting the processing of geranylgeranylated Rap1A with little effect on processing of farnesylated Ha-Ras, with IC50 values of 3 and > 20 μM in vivo, respectively.
