ht1080 cells

Indacaterol (Onbrez; Arcapta) is a β2-Adrenergic Agonist. The mechanism of action of indacaterol is as an Adrenergic beta2-Agonist.

Erastin is an iron death activator that acts on the mitochondrial VDAC in a ROS- and iron-dependent manner. Erastin has anti-tumor activity and acts selectively on tumor cells with RAS-carcinogenic mutations.

RSL3 (RSL3 1S) is an inhibitor of GPX4, and inhibits system xc- that blocks GSH synthesis (IC50=100 nM). RSL3 is a VDAC-independent activator of ferroptosis that is selective for tumor cells carrying oncogenic RAS.

Ferrostatin-1 (Fer-1) is a potent and selective inhibitor of iron death. Ferrostatin-1 potently inhibits Erastin-induced iron death in HT-1080 cells with an EC50 of 60 nM. Ferrostatin-1 also exhibits antioxidant and antifungal activities.

AGI-14100 is a novel and orally available mIDH1 inhibitor.AGI-14100 is used for the treatment of primary human myeloid leukemia.

FA16 is a selective, metabolically stable ferroptosis inducer with an IC50 value of 1.26 μM.FA16 is a derivative of 2-(trifluoromethyl)benzimidazole.FA16 inhibits the cystine/glutamate inverse transporter protein (system Xc-)-mediated exchange of intracellular glutamate for extracellular cystine.FA16 significantly inhibited tumor growth in a HepG2 xenograft tumor model. HepG2 xenograft tumor model significantly inhibited tumor growth.

Cabozantinib (XL184) is a multi-targeted tyrosine kinase receptor inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50=0.035/1.3/4.6/7/11.3 nM). Cabozantinib exhibits both antitumor and antiangiogenic activity.

Indacaterol maleate (QAB149) is an ultra-long-acting β-adrenoceptor agonist.

PROTAC RAR Degrader-1, an RAR degrader, consists of a cIAP1 ligand binding group, a linker, and an RAR ligand binding group. It achieves maximal RAR degradation at a concentration of 30 μM in HT1080 cells. Degradation inducers that utilize cIAP1 are known as specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].

ZX782 acts as a GPX4 protein degrader and an inducer of ferroptosis (Ferroptosis), targeting GPX4 for destruction via both the ubiquitin-proteasome system and the autophagy-lysosome pathway. Following the degradation of GPX4 induced by ZX782, there is a significant increase in the accumulation of lipid reactive oxygen species (ROS) in HT1080 cells.

Crelosidenib is a potent and selective mutant IDH inhibitor with IC50s of 6.27 nM, 3.71 nM, 36.9 nM, and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q, and IDH2 R172K mutases, respectively, and low inhibitory activity against the wild-type IDH enzyme.

Cabozantinib hydrochloride (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt4 (IC50s: 0.035, 1.3, 4.6, 7 and 6 nM).

mIDH1-IN-1 (compound 43) is a potent and selective inhibitor of mIDH1 (isocitrate dehydrogenase 1 mutant) with an IC50 of 961.5 nM, and it effectively inhibits the production of 2-HG (2-hydroxyglutarate) in HT1080 cells. It also exhibits significant anti-proliferative effects on IDH1 mutant U-87 cells (IC50: 41.8 nM). mIDH1-IN-1 is an anti-tumor agent used to study IDH1 mutant solid tumors.

Telaglenastat (CB 839) (IC50 of 24 nM), an effective, specific, and oral inhibitor, which is bioavailable glutaminase, for recombinant human GAC.

PROTAC GPX4 Degrader-1 (DC-2) is a PROTAC-based compound that efficiently degrades GPX4, demonstrating a degradation concentration (DC 50) of 0.03 μM in HT1080 cells [1].

IHMT-IDH1-053 (compound 16) is an irreversible inhibitor highly selective for the IDH1 R132H mutant, with an IC50 of 4.7 nM. It preferentially targets IDH1 mutants over wild-type IDH1 and IDH2, in both their wild-type and mutant forms. In 293T cells transfected with the IDH1 R132H mutant, IHMT-IDH1-053 reduces 2-hydroxyglutarate (2-HG) production with an IC50 of 28 nM. The compound binds to the R132H protein at an allosteric site near the NADPH binding region, forming a covalent linkage with Cys269. Additionally, IHMT-IDH1-053 inhibits the growth of both the HT1080 cell line and primary acute myeloid leukemia (AML) cells harboring IDH1 R132 mutations [1].

Antiproliferative agent-40 (Compound 9) effectively inhibits the proliferation of HT1080 and MCF-7 cancer cells, with IC50 values of 52 μM and 8.2 μM, respectively [1].

GPX4-IN-10 (compound I20) is a non-covalent inhibitor of GPX4. It induces ferroptosis and inhibits the growth of HT1080 cells.

GPX4-IN-12 (compound I22) is a non-covalent inhibitor of GPX4. It induces ferroptosis and inhibits the growth of HT1080 cells.

PROTAC GPX4 degrader-3 is a potent GPX4-targeting PROTAC degrader, exhibiting a DC50 of 0.019 μM (24 h) and an IC50 of 0.024 μM in HT1080 cells.

p-Hydroxy-5,6-dehydrokawain (4'-Hydroxydehydrokawain) is isolated from Kawain.

Physalin A is an anti-inflammatory compound isolated from P. alkekengi with anti-fibrotic effects, regulating the Nrf2 pathway through ERK and p38 to induce detoxification enzymes. Physalin A blocks the activation of the NF-kappaB signaling pathway. Physalin A reduces mammosphere formation by reducing the expression of the GLI1 gene and the YAP1 gene.