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NecroX-7 is a small molecule necrosis modulator and potent antioxidant molecule, which can be bound to some types of radicals and especially NAPQI; inhibits osteoclast differentiation by suppressing NF-κB activity and c-Fos expression, reduces hepatic necrosis secondary to IR injury in vivo; decreases t-BHP- and APAP-induced cell death and ROS/RNS formation in HepG2 human hepatocarcinoma and primary mouse hepatocytes, also protects mice from APAP-induced liver injury and lethality by binding directly to NAPQI.




SW-106065 is a novel pharmacologic inducer of apoptosis in MPNST (malignant peripheral nerve sheath tumors); inhibits ATP consumption of sMPNST and other models of MPNST with EC50 of 1 uM, shows no toxicity to normally dividing Schwann cells or mouse embryonic fibroblasts; reduces MPNST burden in a mouse allograft model.




JPH203 (KYT-0353) is a potent, selective L-type amino acid transporter 1 (LAT1, SLC7A5) inhibitor with IC50 of 60 nM (leucine uptake inhibition), but not LAT2; inhibits cell growth in HT-29 cells with IC50 of 4.1 uM, also inhibits (14)C-leucine uptake in mouse renal proximal tubule cells expressing LAT1 and inhibits cell growth with IC50 of 0.14 and 16.4 uM, respectively; significant inhibits HT-29 tumor growth in vivo.

Solid Tumors

Phase 1 Clinical



cRIPGBM (RIPGBM derivative cRIPGBM, RIPGBM-18) is a metabolite of RIPGBM induces apoptosis in GBM CSCs (EC50=68 nM in GBM 1 cells) by interacting with RIPK2 (Kd=2.3 uM); induces caspase 1-dependent apoptosis, reduces the formation of a prosurvival RIPK2/TAK1 complex and increases the formation of a proapoptotic RIPK2/caspase 1 complex.


355406-76-7 RIPGBM is a cell type-selective, small molecule inducer of apoptosis in GBM cancer stem cells (CSCs) with EC50 of 220 nM (GBM 1 cells); RIPGBM is converted to an apoptosis-inducing derivative (cRIPGBM/RIPGBM-18) selectively in GBM CSCs; cRIPGBM induces apoptosis in GBM CSCs by interacting with RIPK2; significantly suppress tumor formation in vivo in orthotopic intracranial GBM CSC tumor xenograft mouse model.

Flavokawain B

1775-97-9 Flavokawain B is a natural chalcone that can induce apoptosis in androgen receptor-negative, hormone-refractory prostate cancer cell lines (IC50=3-50 uM), via up-regulation of death-receptor 5 and Bim expression; induces apoptosis in human myeloid leukemic cells by modifying NF-κB, possesses potential anti-inflammation and anti-cancer activities; also exhibits significant inhibition of the neurogenic nociceptive induced by intraplantar injections of glutamate and capsaicin in mice.


697235-38-4 Silvestrol is a potential anticancer rocaglate derivative from Aglaia foveolata, induces apoptosis in cancer cells through the mitochondrial/apoptosome pathway; effectively targets the cyclin/CDK/Rb pathway, and additionally induces cytotoxicity via intrinsic apoptosis, exhibits low nanomolar potency both in MCL cell lines and primary MCL tumor cells; demonstrates B-cell selective activity in chronic lymphocytic leukemia and acute lymphoblastic leukemia in vitro and in vivo.

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