by-27

BY27, a potent and selective BET BD2 inhibitor (Ki: 3.1 nM) with anticancer activity, inhibits BD1/BD2 of BRD2, BRD3, BRD4, and BRDT, and suppresses tumor growth.

S-(+)-Ketoprofen ((S)-(+)-Ketoprofen) works by blocking the action of a substance in the body called cyclo-oxygenase. It belongs to a class of medicines called non-steroidal anti-inflammatory drugs (NSAIDs). Cyclo-oxygenase is involved in the production of chemicals in the body called prostaglandins. Prostaglandins are produced in response to injury or certain diseases and would otherwise go on to cause swelling, inflammation and pain. By blocking cyclo-oxygenase, S-(+)-Ketoprofen prevents the production of prostaglandins and therefore reduces inflammation and pain. Along with Peripheral analgesic action it possesses central analgesic action.S-(+)-Ketoprofen is a non-steroidal anti-inflammatory drug. It is manufactured by Menarini, under the tradename Keral. It is available in the UK, as S-(+)-Ketoprofen trometamol, as a prescription-only drug and in Latin America as Miracox, produced by Stein in Costa Rica. In Italy it is available as an over the counter-drug under the tradename Enantyum. In Lithuania it is available as over the counter-drug uder tradename Dolmen.

Tolnaftate (NP-27) is a synthetic antifungal agent used to treat skin infections caused by fungi.

Danofloxacin mesylate (CP 76136-27) is a synthetic antibacterial agent of the fluoroquinolone class that primarily inhibits bacterial DNA-gyrase.

Diuron is an orally active benzoylurea herbicide against annual, perennial broadleaf weeds, and grass weeds. Diuron inhibits the production of ATP and NADH, thereby impairing plant photosynthesis, and also increases ROS production and promotes DMBA/BBN-induced bladder cancer development.

Unifiram is a nootropic agent.1It increases acetylcholine (ACh) release in the rat cerebral cortexin vivoand induces a long-lasting increase in the amplitude of field excitatory postsynaptic potentials (fEPSPs) in the rat hippocampal CA1 region (EC50= 27 nM). It does not bind to serotonin (5-HT), dopamine, muscarinic, nicotinic, adrenergic, glutamate, histamine, opioid, or GABA receptors at 1 μM. Unifiram (0.1 mg/kg) improves memory in non-memory-impaired rats in a social learning test.2It also prevents memory deficits induced by the anticholinergic agent scopolamine, nicotinic receptor antagonist mecamylamine, GABABreceptor agonist baclofen, or α2-adrenergic receptor agonist clonidine in the passive avoidance test in mice when administered at a dose of 0.01 mg/kg and prevents memory deficits induced by the AMPA/kainate glutamate receptor antagonist NBQX at 0.1 mg/kg.1 1.Romanelli, M.N., Galeotti, N., Ghelardini, C., et al.Pharmacological characterization of DM232 (unifiram) and DM235 (sunifiram), new potent cognition enhancersCNS Drug Rev.12(1)39-52(2006) 2.Ghelardini, C., Galeotti, N., Gualtieri, F., et al.The novel nootropic compound DM232 (unifiram) ameliorates memory impairment in mice and ratsDrug Develop. Res.56(1)23-32(2002)

RFRP-3(human) acetate, a human GnIH peptide homolog, is a potent inhibitor of gonadotropin secretion by inhibiting Ca2+ mobilization. RFRP-3(human) acetate is a NPFF1 receptor agonist, it inhibits forskolin-induced production of cAMP with an IC50 of 0.7 n

hCAIX-IN-23 (Compound 27) is a human carbonic anhydrase (hCA) inhibitor with Ki values of 10.4 nM for hCA IX and 8.5 nM for hCA XII. It not only inhibits hCA activity but also releases NO, exerting dual anti-tumor effects. By reducing the expression of hCA IX and iron regulatory proteins, hCAIX-IN-23 regulates mitochondrial caspase activity and the ferroptosis pathway, thereby inducing apoptosis. This compound is utilized in research focused on renal cancer.

FLT3-IN-27 (compound 49) is an inhibitor of FLT3-ITD with an IC50 of 174 nM. It impedes cell growth by causing cell cycle arrest at the G1 phase, making it suitable for research in acute myeloid leukemia.

(6S)-CP-470711 (Compound 8) acts as an inhibitor of sorbitol dehydrogenase (SDH) in both humans and rats, exhibiting inhibitory concentrations (IC50) of 19 nM and 27 nM, respectively. Additionally, (6S)-CP-470711 has been shown to ameliorate diabetes in rats induced by Streptozotocin.

GP-515 HCl is an adenosine kinase inhibitor. In cultured rat myocardial myocytes (RMMs), GP-515 can induce the expression of vascular endothelial growth factor (VEGF). Under severe hypoxia (1% O(2)), GP-515 (20 microM) does not affect VEGF protein expression, but under mild hypoxic conditions, it increases VEGF expression by 27%.

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.

Keap1-IN-1 (Compound 27) is an inhibitor of Keap1, functioning by covalently modifying the Cys151 residue on the BTB domain of KEAP1, thereby disrupting the interaction between Keap and Nrf. It enhances the mRNA expression of the antioxidant response element (ARE) dependent gene NQO1, with an EC50 of 160 nM, and exhibits cytotoxicity in U2OS cells, with an EC50 of 527 nM.

Tetradifon is a broad-spectrum organochlorine acaricide insecticide and a potent inhibitor of the mitochondrial oligomycin sensitivity conferring protein (OSCP)，a subunit of ATP synthase. Tetradifon is utilized for controlling a variety of mite pests and inhibiting energy-related mitochondrial activities including ADP-stimulated respiration and ATPase activity with an IC50 range of 4.5-27 nmoL/mg mitochondrial protein; it exerts oligomycin-like effects by inhibiting oxidative phosphorylation, inducing significant oxidative stress, and interfering with bone metabolism, making it a compound of interest for researching mitochondrial function, bone remodeling mechanisms, and nephrotoxicity.

HDAC-IN-27 dihydrochloride (Compound 11h) is a potent, orally active, HDACI class-selective inhibitor, with IC50 values ranging from 0.43 to 3.01 nM for HDAC1-3. This compound exhibits both in vivo and in vitro anticancer activity. HDAC-IN-27 shows significant antiproliferative effects against acute myeloid leukemia (AML) cell lines by inducing apoptosis and histone acetylation (AcHH3 and AcHH4). It is useful for research on acute myeloid leukemia (AML).

AKT-IN-27 (4a) is a potential anticancer drug that functions by selectively targeting Akt-driven signaling pathways. It induces apoptosis by activating caspase-3, causing G2/M phase cell cycle arrest, and disrupting mitochondrial membrane potential. AKT-IN-27 (4a) is applicable in research on triple-negative breast cancer (TNBC).

ATX inhibitor 27 (Compound 31) is an ATX inhibitor. It demonstrates IC50 values of 13 nM against human autotaxin (hATX) and 23 nM against lysophosphatidylcholine (LPC). By inhibiting the ATX enzyme, ATX inhibitor 27 reduces LPA levels in the body. This compound is applicable in research related to ATX-LPA-associated conditions such as inflammation, neurodegenerative disorders, and cancer.

MDM2-IN-27 primarily targets the MDM2 protein with a Ki value of 0.4 nM. By blocking the negative regulation of p53 by MDM2, it activates the tumor-suppressing activity of p53 and induces apoptosis.

PROTACSARS-CoV-2 Mpro degrader-3 (Compound P2) exhibits antiviral activity by degrading the main protease (Mpro) of human coronaviruses (HCoV) with a DC50 of 27 μM. It effectively inhibits viral replication, with EC50 values of 4.6 μM for HCoV-229E and HCoV-OC43, and 0.71 μM for SARS-CoV-2.

SDH-IN-27 (Compound Q18) is a succinate dehydrogenase inhibitor (SDHI) with an IC50 of 9.7 mg/L. It induces hyphal morphological changes and lipid peroxidation, demonstrating antifungal activity against C. camelliae with an EC50 of 6.0 mg/L. SDH-IN-27 also acts as an ergosterol biosynthesis inhibitor (EBI) by binding to the active site of CYP51, ultimately resulting in the death of pathogenic fungal cells.

AChE/BChE-IN-27 is a brain-permeable dual inhibitor of AChE and BChE, with IC50 values of 3.72 μM and 9.65 μM, respectively, and a permeability coefficient (Pe) of 4.12. It exhibits significant antioxidant activity with an IC50 of 6.32 μM in DPPH assays and also demonstrates strong in vitro antioxidant capabilities. The compound shows metal-chelating properties and has neuroprotective potential against oxidative stress by significantly reducing intracellular reactive oxygen species (ROS). In vivo experiments reveal that AChE/BChE-IN-27 effectively restores AChE and BChE levels and improves cognitive function, indicating its potential application for Alzheimer’s disease (AD).

IDO1-IN-27 (Compound I-1) is an inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), displaying an IC50 of 0.3951 μM against recombinant hIDO1. It also inhibits hIDO1 expression in HeLa cells with an EC50 of 62 nM. By reducing the mRNA expression of pro-inflammatory factors (TNF-α, IL-6, and IL-1β), IDO1-IN-27 effectively stimulates T cell proliferation and simultaneously inhibits the growth of LLC cells.

VEGFR-2-IN-71 is a dual inhibitor of VEGFR2/tubulin. It suppresses tumor cell proliferation, induces apoptosis and cell cycle arrest, and inhibits angiogenesis in the chicken embryo chorioallantoic membrane (CAM) model. By targeting VEGFR2 and tubulin, VEGFR-2-IN-71 hinders tumor growth in the HGC-27 xenograft model. It exhibits low oral bioavailability in rats and is applicable in cancer research.

27-Hydroxy oncosterone is a metabolite that inhibits the proliferation of breast cancer (BC) cells, and it also prevents the proliferation of BC cells induced by cancerosterone and 27-Hydroxycholesterol.