ht29

Prexasertib (LY2606368) is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity.

CAN508 is a potent ATP-competitive CDK9 cyclin T1 inhibitor with an IC50 of 0.35 μM. It also competitively inhibits Cdk2-cyclin E with respect to ATP, with Ki and IC50 values of 13.3 μM and 20 μM, respectively. CAN508 exhibits a 38-fold selectivity for CDK9 cyclin T over other CDK cyclin complexes. [Antitumor activity.]

PROTAC BRAF-V600E degrader-1 (Compound 23) selectively induces degradation of BRAF-V600E but not wildtype BRAF.

Indolelactic acid is a metabolite of tryptophan in Azotobacter vinelandii cultures.

Oxaliplatin (L-OHP) is a DNA alkylating agent, an inhibitor of DNA synthesis. Oxaliplatin causes DNA cross-linking damage, preventing DNA replication and transcription and leading to cell death. Oxaliplatin induces autophagy.

Nigericin sodium salt is an antibiotic, an NLRP3 activator, and a cationic ion carrier. Nigericin sodium triggers the activation of the NALP3 inflammasome, which inhibits Golgi function and suppresses the growth of Gram-positive bacteria.

Pevonedistat (MLN4924) is a potent and selective NEDD8 activating enzyme (NAE) inhibitor (IC50=4.7 nM) with therapeutic potential for myelodysplastic syndromes (MDS) and antitumor activity.

PX-478 is a HIF-1α inhibitor with selectivity, oral activity, and blood-brain barrier permeability. PX-478 has antitumor activity and also protects pancreatic β-cell function in diabetes mellitus and is used in type 2 diabetes mellitus research.

JPH203 (KYT-0353) is a potent and specific inhibitor of L-type amino acid transporter protein 1 (LAT-1). JPH203 inhibits cellular uptake of leucine, inhibits cell proliferation, induces apoptosis, and possesses anti-inflammatory and anti-tumor activities.

CCT020312 (0-9 µM, 24 h) treatment of medium HT29 cells for 24 h resulted in a concentration-dependent loss of P-S608-pRB signaling with linear response values between 1.8 and 6.1 µM.

Daniquidone (Batracylin) is a potent dual inhibitor of DNA topoisomerase I and DNA topoisomerase II with cytotoxic and antiproliferative activity that induces DNA fragmentation for the study of neoplasms, immune disorders, and lymphatic disorders.

4-Nitrobenzoic acid (4Nitrobenzoic acid) is a pharmaceutical intermediate often found in the production of folic acid, DABA, PABA and dyes.

Irinotecan (CPT-11), a derivative of camptothecin, is an inhibitor of DNA topoisomerase I (Topo I). Irinotecan has antitumor activity by preventing DNA strand reattachment through binding to the Topo I complex, resulting in double-stranded DNA breaks and cell death.

Tanespimycin (KOS 953) (17-AAG) is an inhibitor of Hsp90 that selectively inhibits BT474 tumor cell Hsp90 (IC50: 5 nM).

RHPS4 (RHPS 4 methosulfate) is a potent inhibitor of Telomerase at submicromolar.

GB-110 selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM. GB-110 is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist.

GB-110 hydrochloride selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM. GB-110 hydrochloride is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist.

NSC601980 demonstrates antitumor potency, as evidenced by its ability to inhibit cell proliferation in the COLO 205 and HT29 cancer cell lines, achieving Log GI 50 values of -6.6 and -6.9, respectively, in yeast screening experiments.

STAT3-IN-1 selective and orally active inhibitor of STAT3(in HT29 and MDA-MB 231 cells, with IC50 values of 1.82 μM and 2.14 μM , respectively), induces tumor apoptosis.

MS432 is a highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2.

Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase and a potent first-in-class anti-cancer agent, inducing cell apoptosis and inhibiting the growth of TNBC cancer cell lines (IC50s: 10 nM - 20 nM).

CCT070535 inhibits TCF-dependent transcription at the TCF level, displaying GI50 values of 17.6 μM in HT29 (APC mutation), 11.1 μM in HCT116 (oncogenic β-catenin), 11.8 μM in SW480 (APC mutation), and 13.4 μM in SNU475 (Axin mutation) cells.

p53-MDM2-IN-6, an LSM-83177 hydrazone analog, acts as an efficacious p53-MDM2 inhibitor with an IC50 of 11.08 µg mL. This compound inhibits the p53-MDM2 interaction leading to an increase in p-53 levels while concurrently decreasing GST enzyme expression. It halts the cell cycle at the S phase and induces early and late apoptosis (Apoptosis), exhibiting antiproliferative activity against the HT29 cell line with an IC50 of 10.44 µg mL. p53-MDM2-IN-6 holds promise for research in colorectal cancer.

Claturafenib (PF-07799933) is a brain-permeable, selective, all-mutant BRAF inhibitor with broad inhibitory effects on pERK levels in HT29 cells.Claturafenib has shown antitumor activity in preclinical studies in both BRAF V600- and non-V600-mutant cancers and can be used in combination with MEK inhibitors.