116-A

Althiomycin is an antibiotic.

Brefeldin A (Cyanein) belongs to the class of macrolide antibiotics and is an ATPase inhibitor (IC50=0.2 μM). Brefeldin A can induce tumor cell differentiation and apoptosis, and also possesses autophagy inhibitory activity.

Arcyriaflavin A is derived from Eudistoma sp. It inhibits D1-CDK4, B-CDK1 and CaMKII with IC50 values ​​of 0.14μM, 1.13μM and 0.025μM, respectively. Arcyriaflavin A also inhibits HCT-116 and NCI-H460 cells with IC50 values ​​of 0.85μM and 0.59μM, respectively.

2-PCCA hydrochloride, a racemate, is a potent and selective GPR88 receptor agonist showing inhibition of GPR88-mediated cAMP production in HEK293 cells with an EC50 value of 116 nM.

Etoricoxib (MK-663) is a synthetic, nonsteroidal anti-inflammatory drug (NSAID) with antipyretic, analgesic, and potential antineoplastic properties. Etoricoxib specifically binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), resulting in inhibition of the conversion of arachidonic acid into prostaglandins. Inhibition of COX-2 may induce apoptosis and inhibit tumor cell proliferation and angiogenesis.

3'-Hydroxypterostilbene (3'-HPT), a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells with IC50s of 9.0, 40.2, and 70.9 μM for COLO 205, HCT-116, and HT-29 cells, respectively, by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene inhibits the p38MAPK , and PI3K/Akt/mTOR/p70S6K pathways and activates the ERK1/2, JNK1/2 MAPK pathways[1].

Hydroxyacetone is a dehydration product of ketones and glycerol, applicable for biochemical experiments and drug synthesis research.

RLX HCl is a narcissus ketone analogue with anticancer activity that inhibits tumour proliferation by suppressing the PI3K/Akt/FoxO3a signalling pathway in experimental colon cancer, downregulating the p110α and p85 subunits of PI3K in HCT-116 cells, and exhibiting antiproliferative effects.

FC-116 is a potent Tubulin inhibitor with antitumour activity and inhibits tumour growth in mice. FC-116 induces apoptosis in colorectal cancer (CRC) cells and promotes protein degradation.

Ganodermanontriol is a purified triterpene extracted from GL that inhibits proliferation of HCT-116 and HT-29 colon cancer cells without significantly compromising cell viability and suppresses β-catenin transcriptional activity and cyclin D1 protein levels in a dose-dependent manner. Ganodermanontriol also reduces Cdk-4 and PCNA while increasing E-cadherin and β-catenin accumulation in HT-29 cells, Ganodermanontriol markedly suppresses tumor growth in an HT-29 xenograft mouse model without adverse effects, highlighting its strong potential as a chemotherapeutic candidate for colorectal cancer research.

SI-2 hydrochloride (EPH 116 hydrochloride) is a highly promising inhibitor of SRC-3 SMI: SRC-3 (PPI)(IC50 values of 3-20 nM for breast cancer cell death), with acceptable oral availability.

1A-116 is a specific inhibitor of Rac1 .

Buparlisib Hydrochloride (BKM120 HCl) is a specific and orally bioavailable pan-class I PI3K inhibitor that competitively inhibits PI3K/AKT kinase at the nanomolar level and suppresses cancer cell growth, making it suitable for studying breast cancer, glioblastoma, and solid tumours.

Otenzepad (AF-DX 116) is a selective M2 mAChR antagonist with IC50 values of 386 nM in rat heart and 640 nM in rabbit peripheral lung.

Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 values of 10 nM for JAK1, 28 nM for JAK2, 810 nM for JAK3, and 116 nM for TYK2.

PROTACKSP-IN-1 (Compound 21) is a spindle protein (KSP) degrader as a PROTAC, effectively degrading KSP in HCT-116 cells with a DC50 value of 114.8 nM. It inhibits the proliferation of HCT-116 with an IC50 of 10 nM, causes G2/M phase cell cycle arrest, and induces apoptosis in HCT-116. Additionally, PROTACKSP-IN-1 demonstrates antitumor activity in mouse models.

LSD1/HDAC-IN-2 (Compound 20c) acts as an inhibitor targeting both LSD1 and several HDACs, specifically HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, with IC50 values of 39.0, 1.4, 1.0, 1.3, 2.9, and 16.0 nM, respectively. This compound effectively inhibits the proliferation of cancer cells, notably colorectal cancer cells. LSD1/HDAC-IN-2 induces cell cycle arrest at the G2/M phase, inhibits cell migration, and triggers apoptosis in HCT-116 and HT-29 cells. Additionally, it demonstrates antitumor activity in mouse models without causing significant toxicity at a dose of 20 mg/kg.

MAPK-IN-3 (Compound 4a) is an antiproliferative agent demonstrating significant inhibitory effects on KYSE 30, HCT 116, and HGC 27 cell lines, with IC50 values of 0.57 μM, 3.27 μM, and 2.28 μM, respectively. This compound arrests the cell cycle via a p53-dependent mechanism and induces apoptosis through a p53-independent pathway. It reduces the expression of cell cycle-related proteins, such as Cyclin D1 and Cyclin B1, while increasing pro-apoptotic proteins like cleaved PARP, cleaved caspase-7, and cleaved caspase-9. MAPK-IN-3 also decreases anti-apoptotic proteins such as Bcl-2, elevates ROS levels in KYSE 30 cells, and enhances the expression of ROS-related MAPK pathway members, including p-ERK, p-p38, and p-JNK.

NPC26 is a small molecule that disrupts mitochondrial function and exhibits antitumor activity. It shows significant antiproliferative and cytotoxic effects on CRC cell lines (HCT-116, DLD-1, and HT-29). NPC26 induces mitochondrial permeability transition pore (mPTP) opening, generates reactive oxygen species (ROS), and triggers cell death. Additionally, NPC26 kills CRC cells by activating the AMP-activated protein kinase (AMPK) signaling pathway.

MAT2A-IN-16 is a MAT2A inhibitor that effectively suppresses the proliferation of MTAP-/-HCT-116 cells, with an IC50 value of 20 nM.

Scr-IN-1 (Compound 4e) is a tyrosine kinase inhibitor demonstrating inhibitory activity against HCT-116 and MIA-PaCa-2 cells, with IC50 values of 0.16 μM and 1.16 μM, respectively. It shows selectivity towards HCT-116 cells and MIA-PaCa-2 cells, with a selectivity index (SI) greater than 625 and 86. Scr-IN-1 induces apoptosis in HCT-116 colon cancer cells without altering the proportion of necrotic cells and is a potential novel SRC kinase inhibitor for HCT-116 cells. This compound is suitable for cancer research.

STING-IN-15 (compound 66) is a potent STING inhibitor, effectively suppressing human and mouse STING with IC50 values of 116 nM and 96.3 nM, respectively. In the REX1 D18N mouse model, STING-IN-15 significantly reduces tissue damage and inflammation.

Antitumor agent-125 is a novel platinum (IV) prodrug. It activates the mitochondria-dependent apoptosis pathway and induces ferroptosis in HCT-116/OXA cells.

TopoisomeraseII/EGFR-IN-1 is a dual inhibitor of topoisomerase II and EGFR, exhibiting strong cytotoxic activity against the MCF-7, A549, and HCT-116 cell lines. It also demonstrates significant apoptotic activity, making it useful for cancer research.