dld-1

Panitumumab is a fully human IgG2 monoclonal antibody targeting the epidermal growth factor receptor EGFR).

Benproperine phosphate (Pirexyl phosphate) is a cough suppressant.

Tubulin inhibitor 6 (iHAP1) is an inhibitor of tubulin and a potent inhibitor of multiple cancer cell lines.

Temozolomide (TMZ) is a DNA alkylating agent with blood-brain barrier permeability and oral activity. Temozolomide has antitumor activity and antiangiogenic activity, and also induces apoptosis and autophagy. Temozolomide is stable under acidic conditions and hydrolyzes under neutral or slightly alkaline conditions.

Tamoxifen is an orally active selective estrogen receptor modulator (SERM) that acts as an estrogen antagonist in breast cells and an agonist in bone, liver, and uterine cells. It can be used to induce gene knockout and liver injury models in mice, and also exhibits multiple biological activities, including activation of Hsp90, induction of autophagy and apoptosis, and inhibition of EBOV and MARV viral infections.

HRO761 is a potent Werne r syndrome RecQ DNA deconjugase (WRN) inhibitor that can be used to study cancers such as colon and stomach cancer.

Tubulin inhibitor 8 is an inhibitor of tubulin and various cancer cell lines and inhibits tubulin polymerisation and K562 cell growth with an IC50 of 0.73 μM and 14 nM respectively.

TASIN-1 Hydrochloride (TASIN-1 HCl) is a selective inhibitor of truncated APC that acts by selectively killing colorectal cancer cells that express truncated APC by reducing cellular cholesterol levels and inducing apoptotic cell death through the ER stress/ROS/JNK signaling in colon cancer cells.

Hesperidin (Cirantin) is a flavanone glycoside found in citrus fruits with antioxidant, anti-inflammatory, anti-carcinogenic, and antihypertensive and lipid-lowering activity.

Baicalein (5,6,7-Trihydroxyflavone) is a xanthine oxidase inhibitor.

Jamaicin (AnCoA4), an isoflavone derived from the chickweed plant, is an inhibitor of the STIM1-Orai1 channel that blocks calcium influx, reduces its interaction with STIM1, and inhibits T-cell activation.

BAY-8002 is a potent dual MCT1/2 inhibitor (IC50 values are 3, 8, and 12 nM at rat (C6), human (DLD-1) and mouse (4T1) MCT1 respectively).

PARP-1-IN-3 is a potent PARP-1 inhibitor that inhibits PARP-1 and PARP-2 with IC50 values of 0.25 nM and 2.34 nM, respectively.PARP-1-IN-3 has potential anti-inflammatory activity, induces apoptosis, and arrests the cell cycle in the G2/M phase.PARP-1-IN-3 may be useful for the study of cancer-related diseases. cancer-related diseases.

6-Methoxykaempferol is a flavonoid found in brazilian propolis. 6-Methoxykaempferol has anti-proliferative activity against cancer cells, neuroprotective effects on isolated rat brain synaptosomes and reduces glutathione levels. 6-Methoxykaempferol exhibits some lipase activity and may be used in the treatment of cachexia. 6-Methoxykaempferol exhibits some lipase activity and can be used in the treatment of cachexia.

TASIN-1 is a small molecule inhibitor of mutant adenomatous polyposis coli (APC).

ZDLD13 is a β-carboline that exhibits potent anti-HCT116 activity inclusive of inhibition of invasion and migration, inhibition of colony formation, inducing of apoptosis as well as arresting of G1 phase in cell cycle. ZDLD13 is an orally active and selective inhibitor of CDK4/CycD3 (IC 50 = 0.38 μM) which exhibits significant inhibition of tumor growth in HCT116 tumor xenograft model [1].

Ethambutol is an oral anti-tuberculosis drug that inhibits arabinosyl transferase activity, thereby interfering with the synthesis of arabinogalactan and preventing cell wall formation to exert its antibacterial effect; it can also be used for animal models of hyperuricemia and optic neuropathy.

LDHA-IN-9 (Compound 1g) is an LDH-A inhibitor with an IC50 of 25 nM. It inhibits the proliferation of DLD-1 cells by inducing apoptosis, with a GI50 of 27 μM. In mouse models, LDHA-IN-9 exhibits antitumor activity without significant toxicity at a dose of 25 mg/kg.

SOS1-IN-17 (Compound 8d) is an orally active inhibitor targeting the SOS1-KRASG12C interaction, with an IC50 of 5.1 nM. It suppresses ERK phosphorylation in DLD-1 cells with an IC50 of 18 nM and demonstrates antiproliferative activity in KRASG12C-mutant Mia-Paca-2 cells, with an IC50 of 0.11 μM. In mouse models, SOS1-IN-17 shows antitumor efficacy against pancreatic cancer.

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.

PROTACSOS1 degrader-10 (Compound 11o) is a degrader of son of sevenless 1 (SOS1) that functions through CRBN- and protease-dependent mechanisms. It effectively degrades SOS1 in KRAS-mutated cancer cells SW620, A549, and DLD-1, with DC50 values of 2.23, 1.85, and 7.53 nM, respectively. Additionally, PROTACSOS1 degrader-10 inhibits the proliferation of SW620, A549, and DLD-1 cells, with IC50 values of 36.7, 52.2, and 107 nM, and suppresses ERK phosphorylation.

SB-T-1214 (SBT) is a taxane-based drug known for its ability to effectively suppress the expression of stem cell-related genes (Oct4, Sox2, and c-Myc) and induce apoptosis in drug-resistant tumorigenic CD133+/CD44+ colon cancer spheroids. In Pgp+ DLD-1 human colon tumor xenograft mouse models, SB-T-1214 successfully inhibits tumor growth. This compound is relevant for anti-tumor research, particularly against drug-resistant tumors such as colon, pancreatic, and renal cancers.

PRMT5-MTA-IN-4 (Compound 30) is a potent irreversible inhibitor of protein arginine methyltransferase 5 (PRMT5) with an IC50 of 8 nM. It obstructs arginine methylation, hinders ribosomal RNA processing, and suppresses cell cycle-related protein expression. This compound shows antiproliferative activity in various tumor cell lines, exemplified by an IC50 of 0.3 μM in DLD-1 cells. PRMT5-MTA-IN-4 holds potential for research into hematological malignancies such as acute myeloid leukemia and diffuse large B-cell lymphoma.

Myceliothermophin E is a polyketide-amino acid hybrid fungal metabolite that has been found inT. thermophilusand has anticancer and antimicrobial activities.1,2It is cytotoxic to DLD-1, Hep3B, HepG2, and HGC-27 cancer cells (IC50s = 0.32, 0.42, 0.26, and 0.08 μg/ml, respectively).1Myceliothermophin E is active against methicillin-resistant, but not -sensitive,S. aureus(MICs = 15.8 and >100 μM, respectively).2 1.Gao, Y.-L., Zhang, M.-L., Wang, X., et al.Isolation and characterization of a new cytotoxic polyketide-amino acid hybrid from Thermothelomyces thermophilus ATCC 42464Nat. Prod. Res.Epub ahead of print(2019) 2.Wang, X., Zhao, L., Liu, C., et al.New tetramic acids comprising of decalin and pyridones from Chaetomium olivaceum SD-80A with antimicrobial activityFront. Microbiol.102958(2020)