lovo

Clovoxamine (DU 23811) is a 5-hydroxytryptamine reuptake, serotonin and norepinephrine inhibitor with antidepressant and anticonvulsant activity.

E7820 (ER68203-00) is an angiogenesis inhibitor by suppressing integrin a2 (a cell adhesion molecule expressed on endothelial cells).

Effusanin A has antibacterial activity. It exhibits DNA-damaging activity in assay which employed DNA-repair deficient (RAD 52Y) and repair proficient (RAD +) yeast strains. Effusanin A shows inhibitory effects on DU145 cells with IC50 value of 3.16 micro

Thiocolchicine is an effective inhibitor of tubulin polymerization with an IC50 of 2.5 µM and a Ki of 0.7 µM. Thiocolchicine induces cell apoptosis. Thiocolchicine can be used as an ADC cytotoxin in ADC technology.

ATR-IN-18 is an orally active ATR kinase inhibitor (IC50: 0.69 nM). aTR-IN-18 exhibited anti-proliferative effects in LoVo cells (IC50: 37.34 nM). aTR-IN-18 showed anti-tumor effects.

Diaporthein B, a highly oxidized pimarane diterpene, demonstrates significant activity against M. tuberculosis with a MIC of 3.1 μg/mL and exhibits IC50 values ranging from 1.5-3 μM/L against HCT 116 and LoVo colon cancer cells [1].

ATR-IN-16 (compound 46) is a potent ATR kinase inhibitor with significant anticancer activity in LoVo cells, as evidenced by an IC50 value of 410 nM [1].

Bcl-2-IN-7 is a potent inhibitor of Bcl-2 (b-cell lymphoma-2), which can downregulate the expression of Bcl-2, increase the expression of p53, Bax, caspase-7 mRNA, and induce cell cycle arrest and apoptosis in MCF-7 cells of breast cancer. Bcl2-IN-7 showed good antitumor activity against MCF-7 cells (IC50: 20.17 μM), LoVo cells (IC50: 22.64 μM), HepG2 cells (IC50: 45.57 μM) and A549 cells (IC50: 51.50 μM).

Bcl-2-IN-6 is a potent inhibitor of Bcl-2 (b-cell lymphoma-2) that downregulates Bcl-2 expression and increases the expression of p53, Bax, and caspase-7 mRNA. bcl-2-IN-7 induces cell cycle arrest and apoptosis in breast cancer MCF-7 cells. bcl-2-IN-7 acts on MCF-7 cells ( Bcl2-IN-7 showed good antitumor effects on MCF-7 cells (IC50: 20.91 μM), LoVo cells (IC50: 22.30 μM), HepG2 cells (IC50: 42.29 μM) and A549 cells (IC50: 48.00 μM).

Induces p21 expression and S-phase arrest in cancer cells via ERK-mediated pathways. IC50 values are 0.89 and 12.6 μM for LoVo human colon cancer cell line and normal human fibroblasts respectively.

ATR-IN-15 (compound 1) is a highly potent, orally active ATR kinase inhibitor with an IC50 of 8 nM. It also exhibits inhibitory activity against human colon tumor cells LoVo, DNA-PK, and PI3K, with IC50 values of 47, 663, and 5131 nM, respectively [1].

Pestalotin is a fungal metabolite originally isolated from P. cryptomeriaecola with diverse biological activities. It induces reducing sugar release in embryoless rice endosperms when used at concentrations ranging from 3 to 100 mg L and enhances growth of rice seedlings (O. sativa) when used in combination with gibberellin A3 at concentrations ranging from 30 to 500 mg L. Pestalotin has antifungal activity, reducing the growth of C. albicans, C. neoformans, T. rubrum, and A. fumigatus (MICs = 12.5, 50, 50, and 50 μg ml, respectively). It is cytotoxic to HL-60, MKN45, LoVo, and A549 cells (IC50s = 64.87-182.92 μM). Pestalotin has been used as a standard for dereplication of natural products.

ATR-IN-23 (Compound 34), a potent and selective ATR inhibitor, exhibits an IC50 of 1.5 nM, has demonstrated antiproliferative effects on LoVo cells, and induces synthetic lethality in HT-29 cells, suggesting its utility in researching DNA damage response (DDR)-deficient cancers [1].

ATR-IN-17 is a potent inhibitor of ATR kinase with good anti-cancer effects in LoVo cells (IC50: 1 nM).

ASK120067 is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). ASK120067 is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC)[1]. In the in vitro kinase assay ASK120067 potently inhibits the EGFR L858R T790M and EGFR T790M resistant mutants with IC50 values of 0.3 nM and 0.5 nM, respectively, as well as the EGFRexon19del sensitizing mutant (IC50= 0.5 nM). The 50 of ASK120067 against wild-type EGFR (EGFRWT) is 6 nM[1].ASK120067 selectively inhibits the growth of EGFR-mutant cell lines and exhibits potent antiproliferative activity in the mutant EGFR NSCLC cells, with IC50 values of 12 nM, 6 nM and 2 nM against NCI-H1975 (T790M mutation), PC-9, and HCC827 cells (sensitizing mutations), respectively. However, it shows moderate or weak anti-growth activities in A431, LoVo and A549 cells (EGFRWT), with IC50 values ranging from 338 nM to 1541 nM[1].ASK120067 (0.1-100 nM) inhibits the phosphorylation of EGFR at Tyrosine residue 1068 and its downstream signaling proteins AKT and ERK in NCI-H1975 cells (EGFRL858R T790M) even at low dosage (0.1-1 nM). Additionally, ASK120067 inhibits p-EGFR and p-Akt and p-erk in EGFR WT A431 cell until the concentration reaches 10 to 100 nM[1]. ASK120067 (oral gavage; 5-20 mg kg; once daily; 21 days) results in significantly regressed tumor growth, with a tumor growth inhibition (TGI) rate of 85.7%, and administration of 10 mg kg ASK120067 causes dramatic tumor shrinkage with a TGI rate of 99.3%, exhibiting a similar potency with Osimertinib[1]. [1]. Tao Zhang, et al. Discovery of a novel third-generation EGFR inhibitor and identification of a potential combination strategy to overcome resistance. Mol Cancer. 2020 May 13;19(1):90.

ATR-IN-14 (compound 1) is a powerful ATR kinase inhibitor that significantly inhibits ATR signaling pathways following CHKI protein phosphorylation, with a remarkable inhibition rate of 98.03% at 25 nM. ATR-IN-14 also exhibits notable anticancer efficacy in LoVo cells, displaying an IC50 value of 64 nM [1].