Otros inhibidores

<p>Hydroxyphenyllactic acid is an antifungal metabolite, fungi such as Lactobacillus sp. SK007.</p>

CFI-401980 is a potent and selective, novel class of TTK inhibitor.

<p>Antitumor agent-38 inhibits cancer cell growth, causing cell cycle arrest at the S/G2/M phase without affecting microtubules or cell shape.</p>

5-Methyldihydrofolate is the primary biologically active form of folate used for DNA reproduction, the cysteine cycle, and the regulation of homocysteine.

Pecavaptan is a vasopressin receptor antagonist.

AS100 is a bioactive chemical.

(+)-Isomenthone, an isomer of L-Menthone, is a compound isolated from Ziziphora clinopodioides Lam.

N-Nitrosomethylisopropylamine, a type of N-nitrosamine, has been shown to induce tumor formation in mice.

GRL-8234 is a small-molecule BACE1 inhibitor that reverses memory impairments and age-related cognitive decline.

Cy5.5 DBCO, a click chemistry reagent, features a cycloalkyne group and serves as a linker for the Cyanine5.5 fluorophore. Its DBCO group facilitates copper-free, biocompatible click chemistry, characterized by rapid reaction kinetics and high stability [1].

<p>Piribedil N-oxide, a metabolite of the dopamine receptor agonist piribedil, represents a chemical compound involved in the metabolic processing of its parent compound, piribedil.</p>

<p>Capnoidine: a potential anti-inflammatory lead for diseases with limited treatments and major side effects.</p>

<p>(R)-FT709 is an active compound utilized in cancer research [1].</p>

<p>Cholesterol 24-hydroxylase-IN-2 is a potent inhibitor of cholesterol 24-hydroxylase (CH24H or CYP46A1), exhibiting an IC50 value of 5.4 nM, and has potential</p>

<p>AGN 193109 is a potent antagonist of retinoic acid receptors (RARs; Kd= 2, 2, and 3 nM for RARα, β, and γ, respectively), exhibiting selectivity for RARs over retinoid X receptors (RXRs; Kd= &gt;10,000 nM for human RXRα, β, and γ receptors). This compound effectively reverses cellular morphology changes and growth suppression induced by RAR agonists such as all-trans-RA, 13-cis-RA, and 9-cis-RA in ECE16-1 human endometrial ectocervical epithelial cells, particularly when used at a 10-fold molar excess. Furthermore, AGN 193109 downregulates the expression of cytokeratin K5-8, 13, 14, 16, 17, and 19 genes, indicating inhibition of retinoid action, specifically when co-administered with TTNPB but not as a standalone treatment. In vivo studies demonstrate teratogenic effects, including cleft palate, frontonasal dysplasia, and eye malformations in mouse fetuses following a single oral dose of 1 mg/kg.</p>

A1B11 is a selective SIRT2 inhibitor.

<p>Pterostilbene-isothiocyanate (PTER-ITC) demonstrates strong anticancer properties in vitro, particularly disrupting the interaction between β-catenin and TCF-4</p>

ICMT-IN-52 (compound 44) serves as an ICMT inhibitor with an IC50 value of 0.052 μM [1].

<p>5-Oxo Leukotriene B4 (5-oxo LTB4) serves as an intermediate metabolite in the production of 12-oxo LTB4.</p>

<p>NEU-730, a novel inhibitor of TbrPDEB1, shows modest inhibition of T. brucei proliferation.</p>

<p>Englitazone sodium is an antidiabetic agent and a novel NSCA and KATP channel blocker.</p>

<p>Azidoacetic Acid (2-Azidoacetic acid) (compound 92-1), a click chemistry reagent featuring an azide group, serves as a versatile small molecule tool in the synthesis of PROTAC [1].</p>

ICMT-IN-46 (compound 25) is a potent inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), exhibiting an IC50 value of 0.556 μM [1].

AGN-190121 is an RAR agonist that can synergize with RXR ligands to induce hypertriglyceridemia.

<p>Photosensitizer-2 (compound 1), an organic D-π-A sensitizer, exhibits antitumor properties and potent phototoxicity due to an acrylic acid moiety.</p>

Elisidepsin (PM02734), a cyclic depsipeptide, exhibits antineoplastic activity by inhibiting cancer cell proliferation and is under research for the treatment

<p>RPE65-IN-1 (Compound 16e) serves as a potent inhibitor of RPE65, applicable in studies related to retinopathy [1].</p>

<p>Arachidonoyl chloride, a derivative of arachidonic acid, serves as an intermediate in synthesizing arachidonic acid derivatives.</p>

<p>WAY-327131 is an active molecule.</p>

<p>N-didesmethyl Loperamide, an active metabolite of the peripheral μ1-opioid receptor agonist loperamide, impedes electrically induced contractions in isolated</p>

SC 67655 is a peptidomimetic that specifically suppresses human leukocyte antigen DRB10401-restricted T cell proliferation.

SARS-CoV-2 3CLpro-IN-2 is a potent inhibitor of the 3CL protease pair and has shown research potential for SARS-CoV-2 disease.

A-794278 is a bioactive chemical.

1,2,3-Tri-13(E)-docosenoyl glycerol, a triacylglycerol featuring 13(E)-docosenoic acid at the \(sn-1\), \(sn-2\), and \(sn-3\) positions, transiently elevates heart triglyceride levels in weanling rats when administered as 15% of a calcium-deficient diet, with levels returning to baseline after 28 days.

DCLK1-IN-2 (Compound I-5) is a potent inhibitor of DCLK1, exhibiting an IC50 of 171.3 nM, and demonstrates significant antiproliferative effects on SW1990 cell

Nordefrin ((±)-Cobefri), a derivative of Norepinephrine, acts as a vasoconstrictor [1].

Tyropeptin A-4 is used as a proteasome inhibitor.

<p>TNH, a dimeric compound, possesses the ability to penetrate living cells and facilitate the recruitment of proteins into cellular structures [1].</p>

<p>CGP 20376: Benzothiazole anthelmintic, modulates eosinophil burst, antifibrillatory, dose-dependent effects.</p>

1-Stearoyl-2-lauroyl-rac-glycerol, a diacylglycerol, features stearic acid at the sn-1 position and lauric acid at the sn-2 position. It serves as a substrate for the rat diacylglycerol lipase DDHD2.1.

JWH 030 is a potent naphthoyl pyrrole cannabimimetic, exhibiting higher affinity for the CB1 receptor (EC50= 30.5 nM in rats, Ki= 87 nM in mice) compared to CB2 (EC50= 552 nM in human CB2 receptors). The compound demonstrates significant in vivo potency in mouse models, specifically in spontaneous activity and tail flick assays (antinociception) with an ED50 value of 26.8 μM/kg. Furthermore, JWH 030 dose-dependently reduces electrically-induced contractions in the mouse vas deferens, with an IC50 of 3.38 nM, highlighting its effective modulatory effects. This compound is designated for forensic or research applications.

Prostaglandin K2 (PGK2), a 9,11-diketone derivative, results from PGE2 or PGD2 oxidation. Its biological presence remains speculative; however, it demonstrates resistance to in vitro metabolism by 15-hydroxy PGDH.

<p>1,1'-Ethylidene-bis-(L-tryptophan) is a potential impurity in L-tryptophan commercial products, promoting EoL-3 eosinophilic leukemia cell proliferation, enhancing eosinophil cationic protein release from human peripheral blood eosinophils, and boosting IL-5 production in human T cells. At 40 µg/kg, it triggers fascia thickening, mast cell infiltration, inflammation, and fibrosis in mouse superficial adipose and panniculus carnosus tissues, serving as an eosinophilia-myalgia syndrome research model.</p>

N-Arachidonoyl-L-serine (ARA-S), a recently isolated endocannabinoid with a distinct activity profile that diverges from typical endocannabinoids, does not interact with central cannabinoid (CB1), peripheral cannabinoid (CB2) receptors, or vanilloid receptor 1 (VR1). Unlike other compounds, ARA-S (5 mg/kg) counteracts the lowering of blood pressure induced by a 10 mg/kg intravenous bolus of abnormal cannabidiol (Abn-CBD) in anesthetized rat models. Additionally, akin to Abn-CBD, ARA-S induces relaxation in isolated rat mesenteric arteries and abdominal aorta and promotes phosphorylation of Akt and mitogen-activated protein kinase (MAPK) in human umbilical vein endothelial cells (HUVEC). The mechanisms through which ARA-S and Abn-CBD exert their effects on vascular systems show variations and merit deeper investigation.

Xenognosin is a biochemical.

AMB639752 is a potent inhibitor of diacylglycerol kinase alpha (DGKα) that reinstates restimulation-induced cell death (RICD) in SAP-deficient lymphocytes

<p>Nabazenil is a synthetic cannabinoid receptor agonist which has anticonvulsant properties.</p>

<p>TLR7 agonist 15 (compound 16b) is a potent activator of mouse macrophages and hPBMCs, demonstrating an EC50 of 18 nM.</p>

1,3-Dilinoleoyl glycerol, a diacylglycerol, incorporates linoelaidic acid at both the sn-1 and sn-3 positions. This compound emerges from the collision-induced decomposition of synthetic linoleic ammoniated triglycerides.

<p>ICMT-IN-18 (compound 35) serves as an ICMT inhibitor with an IC50 value of 0.066 μM [1].</p>

Nabitan hydrochloride: synthetic antiemetic and analgesic, binds CB1/CB2 receptors, lowers eye pressure, may treat glaucoma.

<p>S 16020-2 is an olivacine derivative, and DNA topoisomerase II inhibitor endowed with a remarkable antitumor activity against various experimental tumors.</p>

<p>WAY-354436 is an active molecule.</p>

Ebio1, a selective activator of the voltage-gated potassium channel KCNQ2, enhances channel conductance by promoting the formation of an expanded gate at a saturation voltage of +50 mV, leading to increased channel activity [1].

<p>Amesergide is a serotonin antagonist.</p>

<p>Smo antagonist, IC50=5 nM; reduces AML cell leukemia potential and self-renewal in mice.</p>

Eltrombopag (LGD-4665, GSK2285921, SB559448) is an oral TPO receptor agonist for thrombocytopenia treatment.

12-oxo-9(Z)-Dodecenoic acid, an ω-oxoacid metabolite derived from the ω-6 PUFA linoleic acid and the ω-3 PUFA α-linolenic acid, is synthesized in plants through

<p>PD 117302: nonpeptide, kappa-opioid agonist, anti-arrhythmic, anticonvulsant, impacts locomotion, diuresis.</p>

<p>Pentabromopseudilin (PBrP), a marine antibiotic derived from Pseudomonas bromoutilis and Alteromonas luteoviolaceus, demonstrates antimicrobial, antitumor, and</p>

<p>Heneicosapentaenoic Acid (HPA), a 21:5 ω-3 fatty acid, is found in minute quantities in green algae and fish oils, resembling eicosapentaenoic acid (EPA) but with an added carbon on the carboxyl end, positioning the initial double bond at the Δ6 location. HPA serves as a tool for examining the impact of double bond positions within n-3 fatty acids, as it is incorporated into phospholipids and triacylglycerol in vivo as efficiently as EPA and docosahexaenoic acid (DHA), while significantly inhibiting the synthesis of arachidonic acid from linoleic acid. Moreover, the ethyl ester variant of heneicosapentaenoic acid offers a more lipophilic and stable alternative to the free acid form.</p>

<p>AA74-1 is a potent, selective APEH inhibitor that significantly enhances T-cell proliferation by inhibiting APEH activity [1].</p>

<p>Osivelotor is an allosteric modulator of hemoglobin S (HbS) [1].</p>

SUN49199, "NaV1.7 Blocker-13," selectively inhibits NaV1.7, not NaV 1.2/1.3/1.6, stronger in humans. No official name yet.

RO116-4875/608 is bioactive chemical.

BN 52256 helps reduce arrhythmias.

Cyclic HPMPC: Potent antiviral, raises O2 in mice with lethal vaccinia, lowers guinea pig CMV replication.

<p>Alpha-GalNAc-TEG-N3 is a click chemistry reagent renowned for its high yield, specificity, and simplicity. This reagent exhibits significant potential for facilitating connections among nucleic acids, lipids, proteins, and various molecules, demonstrating its widespread application across numerous research domains [1].</p>

AL 8810 methyl ester, a prostaglandin F(2α) analog and receptor agonist, competitively antagonizes FP receptor agonist Fluprostenol effects. It lacks significant potency against TP, DP, EP(2), EP(4) receptor subtypes in cell lines [1].

WAY-634964 is an active molecule.

Piperidione is a cough-suppressing agent [1].

<p>(E)-5-Octadecene ((E)-Octadec-5-ene) serves as a sex pheromone or a chemically related compound, disrupting the sexual attraction of female Chilo suppressalis</p>

Anticancer Agent 101, a tetracaine derivative, exhibits anti-cancer activity [1].

<p>Dasiglucagon is a stable human glucagon peptide analog that is rapid and effective in the treatment of severe hypoglycemia.</p>

Flopristin, a semi-synthetic antibiotic of the streptogramin A class, is a fluorinated derivative of pristinamycin IIB.

Mpro 61 is a potent non-covalent inhibitor of SARS-CoV-2 main protease.

<p>Dihydropleuromutilin, a semisynthetic antibiotic derived from pleuromutilin, exhibits antimicrobial efficacy against S. aureus, M. hominis, M. gallisepticum, and M. hyorhinis, with minimum inhibitory concentrations (MICs) of 0.5, 0.3, 0.3, and 2 µg/ml, respectively.</p>

Sphingomyelin (chicken egg) (SMs (chicken egg)) is a sphingolipid from eggs and is a major component of the plasma membrane.

<p>rTRD01 is a TDP-43 ligand that selectively binds to the RRM1 and RRM2 domains of TDP-43, exhibiting a dissociation constant (Kd) of 89 µM for TDP-43 102–269.</p>

<p>MMV009085 is a potent inhibitor of the Plasmodium falciparum hexose transporter (Pf HT1), with potential as an anti-malarial agent.</p>

AZD4619 is a potent, selective and reversible orally bioavailable agonist of PPARα receptor.

2-Thio-UTP tetrasodium, a potent agonist for P2Y2, P2Y4, and P2Y6 receptors, serves as a crucial compound in cancer research [1].

Orexin antagonist 4: potent, selective for OX2R (IC50=4.27 nM); less for OX1R (IC50=295 nM).

TAS2R14 agonist is a potent partial agonist of TAS2R14, displaying an EC50 value of 116.6 ± 23.6 nM [1].

LEI105 is a potent, highly selective, and reversible inhibitor of DAGL-α and DAGL-β.

Sunepitron is a combined α2-adrenergic receptor antagonist and 5-HT1A receptor agonist.

Niceritrol (Cardiolipol) is a niacin ester that reduces cholesterol and triglycerides in total plasma and in the VLD and LD lipoprotein fractions.

3-Hydroxy-2-(palmitoyloxy)propyl stearate is a non-volatile compound isolated from the less polar fractions of the brown macroalga Fucus virsoides J.

SLIGRL-NH2 TFA, also known as Protease-Activated Receptor-2 Activating Peptide TFA, is a Protease-Activated Receptor-2 (PAR-2) agonist [1].

5-Methoxy DET, a synthetic tryptamine designer drug, structurally resembles the potent hallucinogen N,N-DMT. It inhibits serotonin uptake (IC50 of 2.4 µM) and activates 5-HT2A receptors (EC50 of 8.11 nM). This compound is designed for forensic and research applications.

<p>(±)-HIP-A is an excitatory amino acid transporter blocker.</p>

3-Azidopropanol, a click chemistry reagent featuring an azide group, holds significant potential for facilitating bindings among nucleic acids, lipids, proteins, and various molecules. Its application across numerous research domains stems from advantageous traits like high yield, specificity, and simplicity [1].

Lysophosphatidylcholine C19:0 (1-Nonadecanoyl-2-hydroxy-sn-glycero-3-phosphocholine), an acyl chain lipid, enhances IL-1beta secretion [1].

TLR7/8 agonist 9 (Compound 25a), exhibiting EC50 values of 40 nM and 23 nM for hTLR7 and hTLR8 respectively, demonstrates anti-tumor properties and enhances the

<p>(aS)-PH-797804 is a selective inhibitor of p38 MAPK, demonstrating inhibitory concentration (IC50) values of 26 nM for p38α and 102 nM for p38β. This compound exhibits anti-inflammatory activity [1] [2].</p>

<p>1,3-Dioleoyl glycerol, a diacylglycerol with oleic acid at the sn-1 and sn-3 positions, activates protein kinase C (PKC) by approximately 30% at a concentration of 50 μM.</p>

<p>SOMCL-863 is a selective and orally bioavailable c-Met inhibitor. It shows antitumor activity both in vitro and in vivo.</p>

<p>WAY-271999 is an active molecule.</p>

<p>11(S)-HEDE, obtained through the chromatographic separation of (±)11-HEDE, lacks any documented biological activity in scientific literature.</p>

KNI 174 is a new type of anti‐AIDS drug used as an HIV‐1 protease inhibitor

ICMT-IN-33 (compound 73) functions as an ICMT inhibitor with an IC50 value of 0.46 μM [1].

LY 134046 is an inhibitor of phenylethanolamine-N-methyltransferase (PNMT).

<p>Phenylarsine Oxide (Oxophenylarsine) is a membrane-permeable tyrosine phosphatase inhibitor with an IC50 value of 18 µM that stimulates 2-deoxyglucose transport</p>

RIPK1-IN-8 is an aminoimidazolopyridine and is a selective and potent inhibitor of RIPK1 (IC50: 4 nM).RIPK1-IN-8 has research potential in inflammatory diseases