hct116

ABT-737 is a BH3 mimetic and an inhibitor of Bcl-2, Bcl-xL, and Bcl-w (EC50=30.3 nM 78.7 nM 197.8 nM). ABT-737 exhibits antitumor activity and anti-aging activity.

Etoposide (VP-16-213) is a topoisomerase II inhibitor that inhibits DNA synthesis by forming a complex with topoisomerase II and DNA (IC50=60.3 μM). Etoposide has antitumor activity and induces apoptosis and autophagy.

Volasertib (BI 6727) (BI-6727) is a potent inhibitor of PLK1 (IC50: 0.87 nM), inducing mitotic arrest and apoptosis. It also inhibits PLK2 PLK3 (IC50s: 5 56 nM).

BS194 is as a potent cyclin-dependent protein kinases (CDKs) inhibitor.

(-)-Epigallocatechin Gallate (EGCG) is a phenolic antioxidant polyphenol flavonoid found in plants such as green and black tea, which inhibits telomerase and DNA methyltransferase, blocks the activation of EGF receptors and HER-2 receptors, inhibits cellular oxidation, and prevents free radical damage to cells.

Trametinib (GSK1120212) is a MEK inhibitor that inhibits MEK1 and MEK2 (IC50=0.7 0.9 nM) with ATP non-competitive and oral activity. Trametinib activates autophagy and induces apoptosis.

Pevonedistat (MLN4924) is a potent and selective NEDD8 activating enzyme (NAE) inhibitor (IC50=4.7 nM) with therapeutic potential for myelodysplastic syndromes (MDS) and antitumor activity.

Capsaicin ((E)-Capsaicin) is a natural product extracted from Capsicum annuum, and is a TRPV1 agonist (EC50=0.29 μM). Capsaicin has antitumor, anti-inflammatory, antioxidant and neuroprotective activities.

Fludarabine (Fludarabinum) is a fluorinated purine analog, an inhibitor of nucleic acid synthesis and an inhibitor of STAT1 activation. Fludarabine has antitumor activity and can be used for the treatment of leukemia and lymphoma.

Cetuximab (C225) is a monoclonal antibody that is an inhibitor of human epidermal growth factor receptor (EGFR) (Kd=0.201 nM). Cetuximab has antitumor activity, inhibiting tumor cell proliferation and inducing apoptosis.

SFI003 is a novel SRSF3 inhibitor that exerts anticancer activity against colorectal cancer by modulating the SRSF3 DHCR24 ROS axis and driving apoptosis in CRC cells through the SRSF3 DHCR24 reactive oxygen species (ROS) axis.

Dorsomorphin (BML-275) is an AMPK inhibitor (Ki=109 nM) that is selective and ATP-competitive. Dorsomorphin inhibits the BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy, and possesses antitumor activity.

Defactinib (VS-6063) is a second-generation inhibitor of FAK that inhibits FAK phosphorylation at the Tyr397 site. Defactinib has potential antitumor activity.

Stattic (STAT3 Inhibitor V) is a STAT3 inhibitor (IC50=5.1 μM) that selectively inhibits STAT3 activation, dimerization, and nuclear translocation. Stattic has antitumor activity and induces apoptosis.

TNIK-IN-5 is an potent TNIK inhibitor (IC50= 0.05 μM). TNIK-IN-5 potently inhibits Wnt signaling in intact cells. TNIK-IN-5 exhibits excellent in vitro anti-colorectal cancer activity.

Proteasome inhibitor IX (PS-IX) is an inhibitor of chymotrypsin-like activity of the 20S proteasome (IC50 ~1 μM). Proteasome inhibitor IX shows potent anticancer activity. Proteasome inhibitor IX exhibits HCT116 p53+ + cells growth inhibitory activity(IC50 = 1.49 μM).

MS-444 (BE-34776) is a smooth muscle myosin light chain kinase (MLCK) and HuR inhibitor with antitumor activity for triple-negative breast and colorectal cancer.

TNIK-IN-2 is an inhibitor Traf2- and Nck-interacting protein kinase (TNIK, IC50 = 1.33 μM)) which is a downstream signal protein of the Wnt β-catenin pathway.

(E)-[6]-Dehydroparadol ((6)-Dehydroparadol), an oxidative metabolite of [6]-Shogaol, is a potent Nrf2 activator.

ZDLD20 is an orally active and selective CDK4 inhibitor, a β-carboline analog with anti-HCT116 and anticancer activity that inhibits colony formation, inhibits invasion and migration, induces apoptosis, and prevents the G1 phase of the cell cycle.

MC2590 is a potent and selective histone deacetylase (HDAC) inhibitor that inhibits HDAC1-3, -6, -8, and -10 activities, induces cell cycle arrest, and promotes apoptosis.

Emodin (Frangula emodin) is a naturally occurring anthraquinone present in the roots and barks of numerous plants; exerts antiproliferative effects in Y cells that are regulated by different signaling pathways.

Curcumin (Natural Yellow 3) is a phenolic natural product, an inhibitor of histone acetyltransferase p300 CREB (IC50=25 μM) with specificity. Curcumin has a wide range of pharmacological activities such as antitumor, anti-inflammatory and antioxidant.

Myricetin (Cannabiscetin) is a natural flavonoid and MEK1 inhibitor. Myricetin has hypoglycemic, antioxidant, hepatoprotective, anti-tumor and anti-inflammatory activities.