ht-1080

Ammonium iron(III) citrate (Ferric ammonium citrate) is a physiological form of non-ferritin-bound iron that causes intracellular iron overload leading to cellular ferroptosis and enhances protein production.

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.

Isoliquiritin apioside, isolated from Glycyrrhizae radix rhizome, significantly decreases PMA-induced increases in MMP9 activities and suppresses PMA-induced activation of MAPK and NF-κB. Isoliquiritin apioside auppresseses invasiveness and angiogenesis o

1. ISOGINKGETIN (4',4'''-Dimethylamentoflavone), a compound derived from the leaves of Ginkgo biloba, to up-regulate adiponectin secretion with potency comparable to that of rosiglitazone, a known modulator of adiponectin production. 2. Isoginkgetin has anti-tumor activity, the mechanistic basis is splicing inhibition , thus, pre-mRNA splicing inhibitors may represent a novel avenue for development of new anti-cancer agents.3. Isoginkgetin can inhibit tumor cell invasion by regulating phosphatidylinositol 3-kinase/Akt-dependent matrix metalloproteinase-9 expression. 4. Isoginkgetin (0.3mg/kg ip for 3d) can reduce the level of O2·- in plasma and erythroeyte and sometimes increase the activity of SOD in anoxic rats, the action being stronger than aspirin.

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).

TMBIM6 antagonist-1 (BAX-inhibitor-1) is a bax inhibitor

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

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

5'-Fluoroindirubinoxime (5'-FIO) is a potent FLT3 inhibitor( IC50 : 15 nM).

SRS11-92 (AA9) is a ferroptosis inhibitor and a derivative of ferrostatin-1

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.

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.

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.

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.

Ridaforolimus (AP23573) is a small molecule and non-prodrug analogue of the lipophilic macrolide antibiotic rapamycin with potential antitumor activity. Ridaforolimus binds to and inhibits the mammalian target of rapamycin (mTOR), which may result in cell cycle arrest and, consequently, the inhibition of tumor cell growth and proliferation. Upregulated in some tumors, mTOR is a serine/threonine kinase involved in regulating cellular proliferation, motility, and survival that is located downstream of the PI3K/Akt signaling pathway.

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.

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

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.

3-Methylcarbazole (NSC-10154) is an carbazole alkaloid compound with anticancer effects.

2,3-Dimethylhydroquinone exhibits inhibitory activity against cancer cells such as MDA-MB-231, HT-29, HT-1080, and HL-60 with an IC50 of 1.6–6.5 μM, and demonstrates antifungal activity against Candida krusei Berkouet.

Ferroptosisinducer-4 (Compound 5) is a phospholipid-based ferroptosis inducer featuring a terminal double bond at the sn-2 position. It exhibits significant cytotoxicity towards HT-1080 cells with an IC50 value of 18 μM. The toxicity mechanism involves the generation of lipid peroxides and oxidative damage to the cell membrane induced by the terminal double bond. Ferroptosisinducer-4 can be utilized in studies pertaining to the regulation of ferroptosis.

GDCNF-11, an HSP90-based HIM-PROTACGPX4 degrader, facilitates the ubiquitination and degradation of GPX4 through the HSP90 chaperone complex. This reduction in endogenous GPX4 induces ferroptosis in HT-1080 cells, with a DC50 value of 0.08 μM.