gi-50

KRC-108 is a multiple kinase inhibitor. KRC-108 is a potent inhibitor of Ron, Flt3 and TrkA as well as c-Met. KRC-108 inhibited oncogenic c-Met M1250T and Y1230D more strongly than wild type c-Met. The anti-proliferative activity of KRC-108 was measured by performing a cytotoxicity assay on a panel of cancer cell lines. The GI(50) values (i.e., 50% inhibition of cell growth) for KRC-108 ranged from 0.01 to 4.22 μM for these cancer cell lines. KRC-108 was also effective for the inhibition of tumor growth in human HT29 colorectal cancer and NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice. This molecule should serve as a useful lead for inhibitors targeting kinases and may lead to new therapeutics for the treatment of cancer. (source: Invest New Drugs. 2012 Apr;30(2):518-23. doi: 10.1007/s10637-010-9584-2. Epub 2010 Nov 16. ).

RKS262 is a specific cyclin/CDK inhibitor. RKS262 was identified by structural optimization of Nifurtimox which is currently undergoing phase II clinical trials to treat high-risk neuroblastoma. In a NCI(60) cell-line assay RKS262 exhibited significant cytotoxicity in ovarian cancer cells and a variety of other cell lines exceeding effects of commercial drugs such as cisplatin, 5-FU, cyclophosphamide or sapacitabine. Various leukemia cell-lines were most sensitive (GI(50): ~ 10 nM) while several non-small cell lung cancer cell lines and few cell lines from other tissues were relatively resistant (GI(50) > 1 µM) to RKS262 treatment.

Antiproliferative agent-6 (compound 8a) is a potent antitumor compound exhibiting antiproliferative activity. It inhibits cancer cell lines HCT116, MCF-7, H460, and non-tumor aneuploid immortal keratinocyte HaCaT cells with GI50 values of 0.5 μM, 2 μM, 0.7 μM, and 3.5 μM, respectively.

S100A2-p53-IN-1 (compound 51), an inhibitor of S100A2-p53 interactions, targets S100A2, a Ca 2+ binding protein involved in cell signaling and commonly upregulated in pancreatic cancer, and effectively inhibits the growth of the MiaPaCa-2 pancreatic cancer cell line, showing a growth inhibition (GI 50) range of 1.2-3.4 μM [1].

RJ-34, an aristolactam analogue, demonstrates strong antitumor effects across a wide range of cancer cell lines, with subnanomolar GI 50 values (GI 50 <0.1 nM) observed for A431, MES-SA, MES-SA DX5, HCT-15, and HCT-15 CLO2 cells [1].

Glutinol acetate shows significant cytotoxic activity against four human cancer cell lines (HL-60, SK-OV-3, A549, and HT-29), with GI(50) in the range of 11.1-17.9microM; it also has anti-inflammatory effect, exhibits moderate inhibitory activity of TNF-alpha secretion in the lipopolysaccharide (LPS)-stimulated murine RAW264.7 macrophage cell line.

NSC601980 demonstrates antitumor potency, as evidenced by its ability to inhibit cell proliferation in the COLO 205 and HT29 cancer cell lines, achieving Log GI 50 values of -6.6 and -6.9, respectively, in yeast screening experiments.

Anserinone B, a benzoquinone with antifungal and antibacterial properties, inhibits radial growth by 50% and 37% against S. fimicola and A. furfuraceus, respectively. Additionally, it demonstrates moderate cytotoxicity across the National Cancer Institute's 60 human tumor cell lines, with a GI 50 value of 4.4 µg/mL.

Glochidonol exhibits strong inhibitory effects against three human tumor cell lines, MCF-7, NCI-H-460 and SF-268, the GI(50) values of 9.0 +/- 3.7, 4.9 +/- 0.2 and 9.8 +/- 0.5, respectively; it also exerts its antiproliferative activity through the involv

Mollicellin H, a secondary metabolite from the fungus C. brasiliense, exhibits an array of biological activities such as immunomodulation, cytotoxicity, and anti-tumor properties. It demonstrates growth inhibitory effects (GI 50 s) on various human cell lines, including breast cancer (Bre04) at 5.1 μg/mL, lung (Lu04) at 6.5 μg/mL, and neuroma (N04) at 2.5 μg/mL [1].

USP8-IN-1 is an inhibitor of USP8 with an IC 50 of 1.9 μM. USP8-IN-1 inhibits H1975 cell growth with a GI 50 of 82.04 μM [1].

Samuraciclib (CT7001) is a potent, selective, and orally active CDK7 inhibitor with an ATP-competitive nature, effectively inhibiting CDK7 with an IC50 of 41 nM. It demonstrates 45-fold, 15-fold (IC50 of 578 nM), 230-fold, and 30-fold selectivity over CDK1, CDK2, CDK5, and CDK9, respectively. Samuraciclib inhibits the growth of breast cancer cell lines with GI50 values of 0.2-0.3 μM and possesses anti-tumor effects [1] [2].

AM9405 is a novel peripherally active cannabinoid type 1 (CB1) and serotonin type 3 receptor agonist. It inhibits twitch contraction of the ileum and colon with IC50 values of 45.71 nM and 0.076 nM, respectively. AM9405 significantly slowed mouse intestinal motility under physiological conditions and reversed hypermotility, reducing pain in mouse models that mimic symptoms of functional GI disorders, such as stress-induced diarrhea and writhing test.

Ardisiacrispin A (Deglucocyclamin) has cytotoxic activity toward HepG2 cancer cell with the GI(50) value of 1.56μM, it could inhibit the proliferation of Bel-7402 cells by inducing apoptosis and disassembling microtubule.Ardisiacrispin(A+B) exhibit prominent abilities to inhibit the proliferation of HL-60 cells by blocking the cell cycle at S phase and inducing apoptosis.

Antitumor agent-107 (compound 5h) is an anticancer agent exhibiting potent inhibitory activity against leukemia cell lines (GI50 = 0.32-1.34 μM) and demonstrating broad-spectrum antitumor effects across various human cancer cell lines (GI50 = 0.35-9.43 μM) [1].