ht-1080

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

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

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.

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.

Cetzole (Compound 1) acts as an inducer of ferroptosis (iron-dependent cell death) through the accumulation of ROS, leading to cell death. The compound exhibits varying half-maximal cytotoxic concentrations (CC50) against several cell lines: 2.56 μM in NCI-H522, 10.31 μM in NCI-H522 GFP-SCL7A11 #8, 2.71 μM in NCI-H522 RV-GFP, 3.07 μM in HT-1080, 14.9 μM in NARF2, and 6.28 μM in MDA-MB-231. This highlights Cetzole's potential for research in cancer therapeutics.

Melatonin-Tamoxifen Conjugate (compound 16c) is an anticancer drug conjugate made of Melatonin and Tamoxifen, serving as an effective antagonist of ERα (IC50 = 863 nM). In cells expressing the hMT1 receptor, it binds to MLT receptors (Ki = 3.1 nM) and exhibits the ability to promote β-arrestin activation (EC50 = 914 nM) and ERK activation (EC50 = 98 nM). The IC50 values for Melatonin-Tamoxifen Conjugate in MCF-7, MDA-MB-231, and HT-1080 cell lines are 6.8 μM, 6.4 μM, and 1.7 μM, respectively.

NYY-6a is a ferroptosis (Ferroptosis) inhibitor, demonstrating significant suppression of RSL3-induced ferroptosis in 786-O and HT-1080 cells, with EC50 values of 52 nM and 50 nM, respectively. As a radical-trapping antioxidant (RTA), NYY-6a effectively reduces lipid peroxidation, comparable to ferrostatin-1 and liproxstatin-1, making it useful for research into ferroptosis-related pathologies.

UAMC-4821 is a ferroptosis inhibitor with an IC50 of 5.2 nM. It effectively scavenges free radicals, inhibits lipid peroxidation, and prevents ML162-induced ferroptosis, providing protective effects on HT-1080 cells. With favorable pharmacokinetic properties in mice, UAMC-4821 presents an oral bioavailability of 63% and demonstrates blood-brain barrier permeability.

GPX4 9i is a ferroptosis inducer that exhibits cytotoxicity towards HT-1080 cells, with an IC50 of 0.007 µM. This cytotoxic effect can be mitigated by the use of the ferroptosis inhibitor, ferrostatin-1.

QHL-1618 is a drug conjugate activated by the tumor microenvironment. It effectively inhibits tumor growth in various models, such as HT-1080 and CT-26 xenografts.

Mutant IDH1-IN-7 is a highly selective inhibitor of Isocitrate Dehydrogenase 1 (IDH1) with R132H mutation (IC50 = 0.26 μM, Kd = 2.1 μM) and R132C mutation (IC50 = 1.1 μM). It does not inhibit wild-type IDH1, IDH2-wt, or IDH2R140Q. Moreover, Mutant IDH1-IN-7 reduces the production of 2-hydroxyglutarate (2-HG) in U87-MG R132H cells (EC50 = 0.55 μM) and exhibits moderate antiproliferative effects on U87-MG R132H and HT-1080 cells.

GPX4-IN-18 (Compound 17) is a ferrocene-containing inhibitor of glutathione peroxidase 4 (GPX4), and it also acts as a ferroptosis inducer. It enhances the production of reactive oxygen species (ROS) and malondialdehyde (MDA) levels in OS-RC-2 clear cell renal carcinoma cells. In HT-1080 cells, GPX4-IN-18 induces ferroptosis with IC50 values of 0.007 μM (without iron inhibitor-1) and 1.486 μM (with iron inhibitor-1). Additionally, GPX4-IN-18 reduces tumor volume and intratumoral GPX4 levels in an OS-RC-2 xenograft mouse model.

Erastin2 is a ferroptosis inducer and inhibitor of the system xc- cystine/glutamate transporter.[1][2] It inhibits glutamate release in CCF-STTG1 cells (IC50 = 0.0035 µM) and induces cell death in HAP1 cells at 5 µM, an effect blocked by ferrostatin-1 or deferoxamine.[1][2] Erastin2 also induces ferroptotic cell death in HT-1080 cells (EC50 = 0.15 µM), an effect blocked by β-mercaptoethanol (EC50 > 20 µM).[3] Additionally, it increases lipid peroxidation in HT-1080 cells at 1 µM.

Paclitaxel octadecanedioate is a prodrug form of paclitaxel that is comprised of paclitaxel conjugated to 1,18-octadecanedioic acid.1 Unlike paclitaxel, it does not promote tubulin polymerization in vitro when used at a concentration of 10 μM. A 5:1 mixture of paclitaxel octadecanedioate:human serum albumin (HSA) is cytotoxic to HT-1080, PANC-1, and HT-29 cells (IC50s = 12, 2.48, and 8.62 nM, respectively). This mixture reduces tumor growth and increases survival in an HT-1080 mouse xenograft model in a dose-dependent manner. |1. Callmann, C.E., Leguyader, C.L.M., Burton, S.T., et al. Antitumor activity of 1,18-octadecanedioic acid-paclitaxel complexed with human serum albumin. J. Am. Chem. Soc. 141(30), 11765-11769 (2019).

PRLX-93936 is a selective Ras pathway protein inhibitor that modulates RAS/JNK pathway-associated protein phosphorylation, induces caspase-dependent apoptosis and cell cycle arrest, and exhibits anticancer activity.