1a116

1A-116 is a specific inhibitor of Rac1 .

3-arylisoquinolinamine derivative is a compound with antitumor activity.

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.

Candesartan Cilexetil (TCV-116) is an angiotensin II receptor antagonist (IC50: 0.26 nM). Upon hydrolysis to candesartan during gastrointestinal absorption, it selectively competes with angiotensin II for binding to the angiotensin II receptor subtype 1 (AT1) in vascular smooth muscle, blocking angiotensin II-mediated vasoconstriction and inducing vasodilatation.

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].

Galanin (1-16), mouse, porcine, rat, is a hippocampal galanin receptor agonist (Kd = 3 nM) exhibiting high biological activity on locus coeruleus neurons.

Isobarbaloin (Barbaloin-A) (Aloin) is a natural anthracycline from Aloe vera, is a tyrosinase inhibitor.

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.

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.

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.

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.

Magnesium lactate is a magnesium donor and buffering agent.

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.

T-1-DOCA is an EGFR inhibitor with IC50 values of 56.94 nM for EGFRWT and 269.01 nM for EGFRT790M. It has the capability to induce apoptosis (cellapoptosis) in HCT-116 cells.

TGF-β2-IN-1 is a selective inhibitor of TGF-β2. It exhibits potent antiproliferative effects on HCT-116, Caco-2, and HT-29 cells, with IC50 values of 6.84, 10.21, and 9.47 μM, respectively. TGF-β2-IN-1 inhibits TGF-β2 signaling in a dose-dependent manner by suppressing receptor and cytokine expression. This compound is useful for colorectal cancer research.

9β-Hydroxyhexahydrocannabinol is a synthetic cannabinoid derivative. It exhibits cytotoxicity against various tumor cell lines, including HCT-116, MCF-7, K562, MIAPaCa-2, PANC-1, A549, PC-3, and SW-620, with IC50 values ranging from 15.23 to 33.74 μM. This compound can be utilized in cancer research.

ARM1 is a potent inhibitor of aminopeptidase and epoxide hydrolase. The IC50 values are 7.61 µM for aminopeptidase and 12.4 µM for epoxide hydrolase.

YKL-1-116 is an effective, selective, and covalent CDK7 inhibitor.

ABT-116 is a transient receptor potential vanillin type 1 antagonist.

Carotenoid mixture is a mixture of carotenoids that contains the antioxidative and anti-inflammatory carotenoid capsanthin and the antioxidative vitamin A precursor β-carotene , as well as additional carotenoids and carotenoid esters.1,2,3,4 1.Kim, J.S., Lee, W.M., Rhee, H.C., et al.Red paprika (Capsicum annuum L.) and its main carotenoids, capsanthin and β-carotene, prevent hydrogen peroxide-induced inhibition of gap-junction intercellular communicationChem. Biol. Interact.254146-155(2016) 2.Narisawa, T., Fukaura, Y., Hasebe, M., et al.Prevention of N-methylnitrosourea-induced colon carcinogenesis in rats by oxygenated carotenoid capsanthin and capsanthin-rich paprika juiceProc. Soc. Exp. Biol. Med.224(2)116-122(2000) 3.Horie, S., Okuda, C., T., Y., et al.Purified canola lutein selectively inhibits specific isoforms of mammalian DNA polymerases and reduces inflammatory responseLipids45(8)713-721(2010) 4.Negishi, H., Ueda, Y., and Azuma, M.Antioxidant fat-soluble vitamins and lipid peroxides in serumJ. Clin. Biochem. Nutr.26227-234(1999)

Tunicamycin 15:1 is a mixture of tunicamycin structural isomers that contain a 15-carbon N-acyl chain with variable branching patterns. The N-acyl chain incorporated into tunicamycins, like tunicamycin 15:1, is derived from the same pool of cellular branched-chain fatty acids (BCFAs) inStreptomycesand directly impacts the biological activity of each individual tunicamycin variant.1,2,3Purified tunicamycin 15:1 withiso,anteiso, or a mixture ofisoandanteisobranching configurations inhibit bacterial phospho-MurNAc-pentapeptide transferase (MraY) with IC50values of 0.05, 0.36, and 0.09 μM, respectively.2 1.Price, N.P.J., Jackson, M.A., Hartman, T.M., et al.Branched chain lipid metabolism as a determinant of the N-Acyl variation of Streptomyces natural productsACS Chem. Biol.16(1)116-124(2021) 2.Hering, J., Dunevall, E., Snijder, A., et al.Exploring the active site of the antibacterial target MraY by modified tunicamycinsACS Chem Biol.15(11)2885-2895(2020) 3.Duksin, D., and Mahoney, W.C.Relationship of the structure and biological activity of the natural homologues of tunicamycinJ. Biol. Chem.257(6)3105-3109(1982)

Tunicamycin 17:1 is a mixture of tunicamycin structural isomers that contain a 17-carbon N-acyl chain with variable branching patterns. The N-acyl chain incorporated into tunicamycins, like tunicamycin 17:1, is derived from the same pool of cellular branched-chain fatty acids (BCFAs) inStreptomycesand directly impacts the biological activity of each individual tunicamycin variant.1,2,3Purified tunicamycin 17:1 withisooranteisobranching configurations inhibits bacterial phospho-MurNAc-pentapeptide transferase (MraY) with IC50values of 0.12 and 0.9 μM, respectively.2 1.Price, N.P.J., Jackson, M.A., Hartman, T.M., et al.Branched chain lipid metabolism as a determinant of the N-Acyl variation of Streptomyces natural productsACS Chem. Biol.16(1)116-124(2021) 2.Hering, J., Dunevall, E., Snijder, A., et al.Exploring the active site of the antibacterial target MraY by modified tunicamycinsACS Chem Biol.15(11)2885-2895(2020) 3.Duksin, D., and Mahoney, W.C.Relationship of the structure and biological activity of the natural homologues of tunicamycinJ. Biol. Chem.257(6)3105-3109(1982)

1. β,β-Dimethylacrylshikonin (Dimethylacrylshikonin) is a promising agent for developing an improved strategy for radiotherapy against tumors. (a) Injection of Dimethylacrylshikonin combined with IR treatment significantly suppressed tumor growth of the HCT-116 xenograft. (b) Dimethylacrylshikonin significantly suppressed the growth of H(22) transplantable hepatoma, and induced the activation of caspase-3 . (c) Dimethylacrylshikonin inhibited growth of gastric cancer SGC-791 cells by inducing ERK signaling pathway. 2. Dimethylacrylshikonin inhibits the proliferation of MCF-7 cells in vitro by inducing apoptosis through the downregulation of Bcl-2, upregulation of Bax and partial inactivation of the NF-κB pathway.

Picroside III is a cyclic enol ether terpene glycoside isolated from the traditional Chinese medicine hu huang lian.Picroside III has the potential to repair intestinal mucosal damage and reduce intestinal inflammation in mice.