hct-8

Everolimus (SDZ-RAD) is a potent mTOR inhibitor that binds to FKBP-12. It is used alone or in combination with calcineurin inhibitors.

Olomoucine II is an inhibitor of cyclin-dependent kinases (CDKs; IC50s = 7.6, 0.1, 19.8, 0.45, and 0.06 μM for Cdk1, -2, -4, -7, and -9, respectively).1It is selective for CDKs over 10 additional kinases (IC50s = >100 μM for all) but does inhibit ERK2 (IC50= 32 μM) and the ATP-binding cassette transporter B1 (ABCB1; IC50= 6.4 μM).1,2Olomoucine II inhibits proliferation of a variety of cancer cells, including those expressing wild-type p53 or mutant p53 (mean IC50s = 7.4 and 10.1 μM, respectively), and it acts synergistically with daunorubicin to inhibit proliferation of HCT-8 cells that endogenously express ABCB1. Olomoucine also inhibits replication of herpes simplex virus 1 (HSV-1), HSV-2, vaccinia virus, human adenovirus type 4 (Ad4), and human CMV (IC50s = 5, 4.7, 3.8, 2.4, and 3.2 μM, respectively) but not measles virus or influenza virus (IC50s = >20 μM for both).3

B-Raf IN 8 (compound 7g) is a potent inhibitor of B-Raf (IC50 = 70.65 nM) with antitumor activity, demonstrating IC50 values of 9.78, 13.78, 18.52, and 29.85 μM against hepatocellular carcinoma (HEPG-2), colon carcinoma (HCT-116), mammary gland (MCF-7), and human prostate cancer (PC-3) cells [1].

PI3K mTOR Inhibitor-8 is a dual inhibitor of PI3K (PI3Kα IC50: 0.46 nM) and mTOR (mTOR IC50: 12 nM). PI3K mTOR Inhibitor-8 blocks the cell cycle of HCT-116 cells in G1 S phase and induces apoptosis. apoptosis).

Acetomycin is a γ-lactone microbial metabolite originally isolated from S. ramulosus that has anticancer activity. It inhibits proliferation of HCT-8 human colon and L1210 mouse leukemia cancer cells.

Angiogenesis Inhibitor 3 (Compound 8) is a potent substance that effectively inhibits the growth of HUVEC and HCT-15 cells, demonstrating IC50 values of 1.00 and 0.71 μM, respectively. It not only induces apoptosis in these cells but also exhibits significant anticancer activity by suppressing cancer cell invasion. Furthermore, this compound successfully inhibits angiogenesis in zebrafish embryos [1].

FDW028 is a selective and potent fucosyltransferase 8 (FUT8) inhibitor with anti-tumor activity that drives B7-H3 lysosomal degradation via defucosylation and CMA pathways. FUT8 can be used to study metastatic colorectal cancer (mCRC).

Compound 6h (Anticancer Agent 139) exhibits potent anticancer activity, engaging in a π-cationic interaction with Lys352 of Tubulin and demonstrating high efficacy against SNB-19, OVCAR-8, and NCI-H460 with PGIs of 86.61, 85.26, and 75.99, respectively. Moreover, it shows moderate activity against a range of other cancer cell lines — HOP-62, SNB-75, ACHN, NCI ADR-RES, 786-O, A549 ATCC, HCT-116, and MDA-MB-231 — with PGIs between 51.88 and 67.55 [1].

Compound Z10 (PKM2 activator 6) serves as both a PKM2 activator and a PDK1 inhibitor, exhibiting dissociation constants (K D ) of 121 μM and 19.6 μM, respectively. It promotes apoptosis in colorectal cells while suppressing their proliferation and migration, additionally inhibiting glycolysis. Compound Z10 demonstrates inhibitory effects on the proliferation of various cell lines, including DLD-1, HCT-8, HT-29, and MCF-10A, with half-maximal inhibitory concentrations (IC 50 ) of 10.04 μM, 2.16 μM, 3.57 μM, and 66.39 μM, as recorded in reference [1].

SLU-10482, an antiparasitic agent, effectively reduces C. parvum parasitic load in HCT-8 cells with an EC50 value of 0.07 µM. It exhibits lower affinity for human ether-a-go-go (hERG; Kd = 43 µM) compared to its counterpart, SLU-2633. When administered in vivo at dosages of 5 and 15 mg/kg twice daily, SLU-10482 significantly decreases fecal oocyst counts in mice infected with C. parvum.

8-Prenylnaringenin is a phytoestrogen with high estrogenic activity,

Flemiphilippin A has antioxidant activity, it shows DPPH radical scavenging activity with effective half maximal concentration (EC50) of 18.36 ug mL. Flemiphilippinin A (5 ug mL) exhibits some level of antitumor activity against human hepatocellular carci

Hellebrigenin has anti-hepatoma activities, it induces cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells through inhibition of Akt. Hellebrigenin exhibites moderate to strong activity against human HL-60, SF-295, MDA-MB-435, and HCT-8 cancer cell strains without hemolysis of mouse erythrocytes.

Periplocymarin is a cardiac glycoside with anticancer potential isolated from Periploca sepium and Periploca graeca.

11alpha,12alpha-Oxidotaraxerol palmitate shows selective cytotoxicity against HCT-8, Bel-7402, BGC-823, A549 and A2780.

Chlorovaltrate K shows moderate cytotoxicity against lung adenocarcinoma (A 549), metastatic prostate cancer (PC-3M), colon cancer (HCT-8) and hepatoma (Bel 7402) cell lines with IC50 values of 0.89-9.76 uM.

Jatamanvaltrate B shows cytotoxicity against lung adenocarcinoma (A549), metastatic prostate cancer (PC-3M), colon cancer (HCT-8),and hepatoma (Bel7402) cell lines.

Volvaltrate B shows cytotoxic activity against the lung adenocarcinoma (A549), metastatic prostate cancer (PC-3M), colon cancer (HCT-8), and hepatoma (Bel7402) cell lines, with IC50 values of 8.5, 2.0, 3.2, and 6.1 uM, respectively.

8-epi-Helenalin, a sesquiterpene lactone with anti-tumor properties, is derived from Inula britannica L. var. chinensis (Rupr.) Reg. It demonstrates cytotoxic activity against a range of cancer cell lines, with ED50 values of 12.2 μM for HL-60, 53.8 μM for A549, 9.1 μM for MCF7, 8.7 μM for HCT-15, 18.7 μM for SK-OV-3, and 8.3 μM for Malme-3M, indicating its potential for anti-tumor research [1].