ht1080 cells

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

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.

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).

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.

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

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].

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.

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].

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].

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].