lovo

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.

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

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

Punicalagin is a major ellagitannin found in pomegranates that is reported to produce antioxidant, anti-inflammatory, and anticancer effects. It has been shown to prevent high-fat diet-induced obesity-associated accumulation of cardiac triglyceride and ch

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.

Emodin (Frangula emodin) is an 11β-HSD1 inhibitor with a selective IC50 of 186 and 86 nM against 11β-HSD1 in humans and mice, respectively. Emodin has antiviral, anti-inflammatory, and anti-cancer effects. Emodin can improve metabolic disorders in diet-induced obese mice.

Decylubiquinone (DUb) is a coenzyme Q10 analog with anticancer activity, inhibiting breast cancer growth and metastasis, enhancing mitochondrial function in synaptosomes, and inhibiting tumor-induced angiogenesis.

WEE1-IN-10 (compound 77) is a Wee1 kinase inhibitor that inhibits the growth of LOVO cells (IC50=0.524 μM) and can be used to study diseases caused by abnormal Wee1 activity, such as pancreatic cancer, malignant melanoma, and malignant glioma.

Veonetinib (example 3) is an effective inhibitor of tyrosine kinase , exhibiting IC50 values of 0.1 μM and 0.4 μM in A549 cells and LOVO cells, respectively.

PROTAC PARP1 degrader-3 (Compound C6) is a PROTAC degrader specifically targeting PARP1, with a DC50 of 58.14 nM. It demonstrates cytotoxicity in SW-620 and LOVO cancer cells, with IC50 values of 1.63 μM and 2.84 μM, respectively. In BRCA-mutated colon cancer cells, PROTAC PARP1 degrader-3 exhibits synergistic effects with SN-38, with a combination index (CI) of 0.487.

CDK1-IN-7 (compound M7) is a potent CDK1 inhibitor. It effectively suppresses the proliferation and migration of HCT116 and Lovo cells, making it a valuable tool for colorectal cancer research.

SHP2protein degrader-3 is an AUTAC protein degrader specifically targeting SHP2. It induces dose-dependent degradation of SHP2 in HeLa cells, with a DC50 of 3.22 μM, and demonstrates significant antitumor activity with an IC50 of 5.59 μM. The degradation mechanism is mediated via LC3-dependent autophagy, which can be inhibited by lysosomal inhibitors. SHP2protein degrader-3 also induces apoptosis in various tumor cell lines, including cervical cancer cells (HeLa), liver cancer cells (HepG2 and Huh-7), and colon cancer cells (LoVo). [SHP2ligand: ; LC3 Ligand: ; Linker: .]

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.

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-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].

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].

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].

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

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).

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.

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).

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-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].

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