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.

β-Glucosidase 1A from Clostridium cellulovorans (EC 3.2.1.21) is an enzyme that targets the β1→4 glycosidic bond between two glucose molecules or glucose-substituted molecules, such as the disaccharide cellobiose. As a member of the cellulase family, β-Glucosidase participates in the breakdown of cellulose and related polysaccharides. Specifically, it functions as an exocellulase, displaying specificity for various β-D-glycoside substrates by catalyzing the hydrolysis of terminal, non-reducing β-D-glucoside residues, thereby releasing glucose.

β-Mannanase 26B, Clostridium cellulovorans (EC 3.2.1.78), is an enzyme that functions as a 4-β-D-mannan mannohydrolase. It catalyzes the random hydrolysis of (1->4)-β-D-mannosidic linkages in mannans, galactomannans, and glucomannans.

β-Mannanase 5A, Clostridium cellulovorans (EC 3.2.1.78), is an enzyme classified as a 4-β-D-mannan mannohydrolase. It catalyzes the random hydrolysis of (1->4)-β-D-mannosidic linkages in mannans, galactomannans, and glucomannans.

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.

EV206 is a potent Hsp70 inhibitor, demonstrating significant anti-proliferative activity. This compound induces apoptosis and promotes increased protein expression of cleaved PARP and caspase-3, indicating its potential anti-tumor activity.

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.

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.

PROTAC ATRdegrader-3 is a potent CRBN-based ATR PROTAC degrader with a DC₅₀ of 127 nM. This compound also degrades CHK1, with a corresponding DC₅₀ of 135 nM. PROTAC ATRdegrader-3 inhibits the proliferation, migration, and invasion of cancer cells, induces apoptosis, and causes S phase arrest and DNA damage. It effectively suppresses tumor growth in LoVo xenograft mouse models with negligible toxicity. PROTAC ATRdegrader-3 is applicable in research related to colorectal cancer.

PROTAC ATR degrader-4 is a PROTAC-derived ATR kinase degrader with a DC₅₀ of 6.18 μM and a Dmax of 71.42% in LoVo cells. It reduces ATR protein levels, causing nuclear envelope rupture, genomic instability, DNA damage, and apoptosis, and shows antitumor activity in xenograft mouse models, making it useful for research on ATM-deficient cancers. (Pink: ATM/ATR ligand; Blue: Cereblon ligand; Black: 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.

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.

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: .]

ATR-IN-32 is an orally active ATR inhibitor that effectively suppresses the proliferation of MIA PaCa-2 cells. It significantly inhibits tumor growth in mice bearing LOVO and HT-29 xenografts. ATR-IN-32 is applicable for studying cancers mediated by the ATR protein kinase, such as colorectal cancer and pancreatic cancer.

Tubulin-IN-56 is a tubulin inhibitor with cytotoxic effects on colon cancer cell lines (LS180, HCT116, SW620, LoVo). It downregulates βIII-tubulin expression and upregulates βIVa-tubulin expression within these cell lines. Additionally, Tubulin-IN-56 inhibits cell invasiveness and elevates intracellular ROS levels in colon cancer cell lines. This compound is applicable in colon cancer research.

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].