ht-29

Prexasertib (LY2606368) is a selective checkpoint kinase 1 (CHK1) inhibitor (Ki 0.9 nM, IC50<1 nM). Prexasertib causes double-stranded DNA breaks and replication mutations, leading to apoptosis. Prexasertib has antitumor 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.]

Sertindole (Lu 23-174) is an atypical antipsychotic that binds to dopamine D2 receptors and serotonin (5-HT) receptor subtypes 5-HT1D, 5-HT2A, and 5-HT2C, with Kds of 2.7, 20, 0.14, and 6 nM, respectively.

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

Apostatin-1 (Apt-1) is a novel TRADD inhibitor that binds to a pocket on the N-terminal TRAF2 binding domain of TRADD.

β-catenin-IN-2, a potent inhibitor of β-catenin, is suitable for use in colorectal cancer research.

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

SR 142948 is a neurotensin (NT) receptor antagonist.

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).

SNS-314 Mesylate (SNS-314) is an effective and specific Aurora A/B/C inhibitor (IC50: 9/31/3 nM). It is less inhibition of Trk A/B, Fms, Flt4, c-Raf, Axl, and DDR2.

Bromosporine is a broad spectrum inhibitor for bromodomains for BRD2/4/9 and CECR2 (IC50: 0.41/0.29/0.122/0.017 μM), respectively.

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

GSK-1520489A is an active PKMYT1 inhibitor.

KW-2450 free base is an orally bioavailable inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (IR) tyrosine kinases with potential antineoplastic activity. IGF-1R IR inhibitor KW-2450 free base selectively binds to and inhibits the activities of IGF-1R and IR, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-R1 and IR tyrosine kinases, overexpressed in a variety of human cancers, play significant roles in the stimulation of cellular proliferation, oncogenic transformation, and suppression of apoptosis.

Antitumor agent-87 is a potent compound exhibiting high antitumoral activity, with a Ki value of 0.23 µM for CYP1A1. It demonstrates antiproliferative effects and induces cell cycle arrest at the G2/M phase, underscoring its effectiveness as an antitumor agent.

IL-17A inhibitor 1 is a IL-17A inhibitor with IC50 of <9.45 nM in alphalisa assay. IL-17A inhibitor 1 inhibits HT-29 cells with IC50 of 9.3 nM.

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].

2-Methylcyclohexa-2,5-diene-1,4-dione exhibits inhibitory activity against cancer cells such as A2780, HT-29, HL-60, and K562 (IC50 = 2.8–12.1 µM) and antibacterial activity against Bacillus subtilis.

2,3-Dimethylhydroquinone exhibits inhibitory activity against cancer cells such as MDA-MB-231, HT-29, HT-1080, and HL-60 with an IC50 of 1.6–6.5 μM, and demonstrates antifungal activity against Candida krusei Berkouet.

TC13172 is a potent and covalent inhibitor that specifically targets the mixed lineage kinase domain-like protein (MLKL), exhibiting significant selectivity for MLKL over the closely related receptor-interacting serine/threonine kinase 1 (RIPK1) and RIPK3 at a concentration of 10 µM.TC13172 effectively inhibits necroptosis induced by the TSZ combination (TNF-α, a Smac mimetic, and Z-VAD-FMK) in HT-29 cells with a EC50 of 2 nM and, at 100 nM, blocks TSZ-induced oligomerization and plasma membrane translocation of MLKL.

PROTAC MLKL Degrader-2, a PROTAC that targets MLKL (Mixed Lineage Kinase), incorporates the PROTAC target protein ligand, E3 ligase ligand Thalidomide, and PROTAC Linker N-Methylpiperazine. The conjugate of the E3 ubiquitin ligase ligand and Linker is Thalidomide-N-Methylpiperazine. This compound exhibits antinecroptotic activity in human cell lines and effectively degrades MLKL in the HT-29 xenograft mouse model.

KPU-300 (compound 6b), functioning as a tubulin inhibitor, exhibits pronounced cytotoxic effects, boasting an IC 50 value of 7.0 nM against HT-29 cells.

Thalidomide-N-methylpiperazine functions as an E3 Ligase Ligand-Linker Conjugate and is instrumental in the synthesis of PROTAC MLKL Degrader-2. This compound demonstrates antinecroptotic activity in human cell lines and effectively degrades MLKL in the HT-29 xenograft mouse model.

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.