Otros inhibidores

Khellinol, a vasodilator, has bronchodilatory action.

Setipafant is an antagonist of the platelet-activating factor.

15(R)-Prostaglandin D2 functions as a DP(2) receptor (Prostaglandin Receptor) agonist with potential roles in prostatic hormone signaling and exhibits anti-inflammatory properties. It enhances actin polymerization in human eosinophils and elevates cAMP levels in platelets [1].

GSK2188764 is an inhibitor of T. brucei IPMK, partially inhibits rTbIPMK activity.

BMS-250749 is a fluoroglycosylated fluoroindolocarbazole, it has antitumor activity.

BMS-332 is a dual inhibitor of the lipid kinases DGKα and DGKζ, demonstrating half-maximal inhibitory concentrations (IC50) of 0.005 μM for DGKα and 0.001 μM

PF-06456384 is a highly potent and selective NaV1.7 inhibitor with IC50 value of 0.01 nM.

p-SCN-Bn-HOPO: superior (89)Zr ImmunoPET chelator, low background, high tumor contrast, minimal bone uptake in BT474 breast cancer scans.

Elisartan is a non-peptide pro-drug of angiotensin II AT1 receptor antagonist HN-12206. It also shows anti-hypertension activities.

<p>Alclofenac (W-7320) aids chronic rheumatism by affecting acute phase proteins and L-tryptophan binding.</p>

Cannabipiperidiethanone, a synthetic cannabinoid structurally similar to JWH 250 and AM2233, has been detected in prohibited "herbal" blends in Japan. It exhibits affinity for CB1 and CB2 receptors with IC50 values of 591 nM and 968 nM, respectively. Compared to JWH 250, its affinities for CB1 and CB2 receptors are 2.3- and 9.4-fold lower, and 13- and 70-fold lower than (R)-(+)-WIN 55,212-2, respectively. Cannabipiperidiethanone is designated for forensic and research purposes only.

Manoalogue is a synthetic analog of manoalide and phospholipase A2 antagonist.

(R)-Necrocide 1 (compound (R)-38) is a potent anticancer agent with antiproliferative activity [1].

ICMT-IN-26 (compound 38) acts as an ICMT inhibitor with an IC50 value of 0.36 μM [1].

<p>oxytocin receptor partial agonist</p>

ICMT-IN-22 (compound 62) acts as an ICMT inhibitor with an IC50 value of 0.63 μM [1].

GSK2647544 inhibits Lp-PLA2, a pro-inflammatory enzyme from macrophages, orally active, calcium-independent.

<p>SC 53228 is a specific leukotriene B4 receptor antagonist.</p>

Giminabant is an antagonist of cannabinoid receptor antagonist (veterinary use).

SPM-242 racemate is an antagonist of S1P(3)-selective.

ICMT-IN-27, also known as compound 64, is an inhibitor of the enzyme ICMT, demonstrating potent activity with an IC50 value of 0.1 µM [1].

<p>RXFP1 receptor agonist-3 (Example 223) is an agonist of the RXFP1 receptor that inhibits cyclic AMP (cAMP) production in HEK293 cells stably expressing human</p>

<p>(2'S)-Nicotine-1-oxide, a nicotine metabolite, arises from the liver's metabolism of nicotine via the cytochrome P450 (CYP) isoform CYP2A6. It has been identified in human sperm and semen.</p>

<p>WAY-329600 is an active molecule.</p>

SUCNR1-IN-2 (Statement 35) serves as an inhibitor of both succinate and succinate receptor 1, utilized in research pertaining to neurodegenerative disorders,

Xeniafaraunol A (compound 31) is a potent inhibitor of the transient receptor potential melastatin 7 (TRPM7) channel [1].

ICMT-IN-11 (compound 48) serves as an ICMT inhibitor with an IC50 value of 0.031 μM [1].

<p>NSC363998 (free base), an orally active compound, suppresses rCGG90-induced neurotoxicity and is utilized in researching neurodegenerative disorders, including</p>

<p>15-OxoEDE, generated through the oxidation of 15-HEDE, effectively inhibits 5-LO in RBL-1 cells with an IC50 of 55 µM, approximately half as potent as 15(S)-HEDE. Additionally, another related oxo-eicosanoid, 5-oxoETE, is produced from 5(S)-HETE via a specific dehydrogenase, exhibiting significant inflammatory activity.</p>

<p>Acetylaleuritolic acid, a pentacyclic triterpenoid from Garcinia miniata leaves, inhibits P-388 leukemia.</p>

Dual photoCORM 1 (compound 5), a metal-free, photoactive, dual carbon monoxide releasing molecule (CORM), demonstrates efficient cellular uptake and enables

GGTI-297 is a potent, cell-permeable, and selective peptidomimetic inhibitor of GGTase I compared to Farnesyl Transferase (FTase).

Naa50-IN-1 (Compound 4a) is a potent inhibitor of N-α-Acetyltransferase 50 (Naa50), demonstrating an IC50 of 7 mM, with potential applications in cancer

WAY-616296 has potential anticholesterol activity and can be used in the study of diabetes, hypertension, psoriasis and obesity.

<p>TLR7/8 agonist 8 (compound 24m) is a potent dual agonist for toll-like receptors 7 and 8 (TLR7/8), exhibiting half-maximal effective concentrations (EC50s) of</p>

PD-1/PD-L1-IN-22 is a small molecule inhibitor of PD-1/PD-L1 protein-protein interactions that blocks PD-1/PD-L1 interactions (IC50: 0.732 μM).

CeMMEC1 is a compound derived from N-methylisoquinolinone that inhibits the second bromodomain of TAF1.

Vamagloxistat is a glycolate oxidase inhibitor utilized to mitigate hyperoxaluria and reduce the formation of kidney stones [1].

<p>Rp-Adenosine-5'-O-(1-thiodiphosphate) (Rp-ADP-α-S), a sulfur-containing isomer of the nucleotide derivative ADP-α-S, acts as an inhibitor of phosphorylase</p>

Myt1-IN-3 is a potent inhibitor of Myt1 (IC50 <10 nM) [1].

Cyclic Phosphatidic Acids (cPAs) are naturally occurring lysophosphatidic acid (LPA) analogs, characterized by a 5-membered ring formed between the sn-2 hydroxy group and the sn-3 phosphate. Carba-derivatives of cPA (ccPA) modify the sn-2 (2-ccPA) or sn-3 (3-ccPA) linkage, hindering the conversion of cPA into LPA. Oleoyl 3-Carbacyclic Phosphatidic Acid (3-ccPA 18:1) incorporates the 18:1 fatty acid oleate at the sn-1 position on the glycerol backbone, acting as a cyclic LPA analog. This compound, at a concentration of 25 μM, blocks MM1 cells' transcellular migration through mesothelial cell monolayers induced by fetal bovine serum (by 90.1%) or LPA (by 99.9%), without impeding cell proliferation. Additionally, 3-ccPA 18:1, in the 0.1-1.0 μM range, notably suppresses autotaxin, which plays a vital role in various cancer cell behaviors including survival, growth, migration, invasion, and metastasis.

<p>CC-90005 is a potent, selective oral PKC-θ inhibitor with an IC50 of 8 nM, preferential over PKC-δ, and inhibits T cell activation.</p>

11-Keto Fluprostenol, a potent analog of prostaglandin F2α (PGF2α), primarily interacts with the FP receptor. It is a structurally modified derivative of prostaglandin D2 (PGD2) designed to enhance its potency and extend its half-life. The compound is produced by oxidizing fluprostenol at the C-11 position, which results in 11-keto fluprostenol. This modification allows 11-keto Fluprostenol to exhibit moderate affinity for the CRTH2/DP2 receptor, though it shows negligible activity at the DP1 receptor, distinguishing its action from that of PGD2.

Satigrel is a new antiplatelet agent. It also inhibits platelet accumulation in prosthetic arterial grafts.

M5N36: selective Cdc25C inhibitor, IC50: 0.15µM A, 0.19µM B, 0.06µM C; halts cell growth, boosts p-CDK1/2.

Ebopiprant (OBE-022) is an oral, selective PGF2α antagonist for preterm labor, safer than indomethacin.

KH064 is a sPLA2-IIA inhibitor of oral activity.

<p>Manoalide: sesterpenoid, PLA2/PLC inhibitor, anti-inflammatory, antibacterial.</p>

<p>PAN12314 (Compound 5a) is a 5-HT4R partial agonist with cognition-enhancing effects in animals, lacking a formal name.</p>

AG-28262 besylate is a VEGFR-2 Inhibitorwhich may affect alanine aminotransferase gene expression and enzymatic activity in the liver.

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

CJ-463, a selective uPA blocker, shows strong anti-tumor effect, especially at 100mg/kg, potentially treating lung cancer.

N-Acetylanonaine may be used as a substrate for the identification, differentiation, and characterization of aminoacylase(s)/amidohydrolase(s).

LY 213024 is an antagonist of leukotriene B4 receptor.

Org 33201 is a potent aromatase inhibitor.

1-Myristoyl-3-docosanoyl-rac-glycerol is a diacylglycerol with myristic acid at the sn-1 position and docosanoic acid at the sn-3 position.

RXFP1 receptor agonist-1 (Example 2), an agonist of the RXFP1 receptor, suppresses cAMP production in HEK293 cells that constitutively express the human RXFP1,

ACT-280778 is a potent L/T calcium channel blocker.

<p>N1-Azido-spermine trihydrochloride (Spermine[HHHN3]) is a click chemistry agent featuring an azide group.</p>

FPL-63012AR is a D1-receptor agonist.

<p>AtPCO4-IN-1 is a selective AtPCO4 inhibitor, exhibiting an IC50 value of 264.4 μM [1].</p>

7-(Dimethylamino)-4-methylcoumarin, a coumarin derivative, is utilized in the research of fluorescent brightener solutions [1].

CAY10592 is a selective PPARδ agonist with EC50s of 30 nM in rats and 53 nM in humans, improves lipid profiles and insulin sensitivity in models.

<p>QZ59S-SSS acts as a potential inhibitor of human P-glycoprotein and may be used to improve the efficacy of cancer chemotherapy.</p>

<p>GSK1842799, a selective S1P1 agonist for MS, shows &gt;1000x selectivity over S1P3 &amp; good oral bioavailability.</p>

BN 52256 helps reduce arrhythmias.

1,3-Dilinoleoyl-2-stearoyl glycerol, a triacylglycerol, incorporates linoleic acid at the sn-1 and sn-3 positions and stearic acid at the sn-2 position. This compound is present in soybean oil and both transitional and mature human milk.

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

Potent α7L-GlyR & PSAM4-5-HT3 agonist (EC50: 0.3/0.5 nM). Reduces cortical neuron activity; induces contralateral rotation in mice (LED 0.1 mg/kg).

<p>6-N-Phthalimidoy hexanoic acid (compound FH) is a hapten featuring a carboxyl group at its spacer arm terminus, facilitating reaction with proteins' free amine groups. This compound is capable of conjugation with carrier proteins for use in antigen design [1].</p>

L-Biotin, or simply biotin, is a water-soluble vitamin crucial for carboxylation reactions in various enzymes.

Sontigidomide (Compound 5) is an antineoplastic agent that demonstrates over 80% inhibition of MOLM-13 cell proliferation at a concentration of 1 μM after 3

MNI-caged-L-glutamate, a derivative of glutamate conjugated with a 4-methoxy-7-nitroindolinyl (MNI) photoprotective group, remains pharmacologically inactive at neuronal glutamate receptors at concentrations up to mM. Upon light exposure (300 - 380 nm excitation), it rapidly releases L-glutamate by cleaving the MNI group within submicroseconds. This characteristic enables the investigation of fast synaptic glutamate receptor mechanisms in situ.

14-Methyl palmitic acid methyl ester is a methylated fatty acid methyl ester identified in A. indica leaf extract, S. alboflavus TD-1, and as a less prominent constituent in biodiesel from C. sorokiniana microalgae. It acts as a volatile agent emanating from maize, impeding the growth of F. verticillioides in a dose-responsive manner. Additionally, this compound is utilized as a reference standard for quantifying 14-methyl palmitic acid in diverse foods via GC-MS. [Matreya, LLC. Catalog No. 1614]

Photoclick myristic acid, a saturated fatty acid derivative, features a terminal clickable alkyne moiety and a photoactivatable diazirine group at the 10th carbon position. This compound facilitates the study of protein lipidation through its application as a probe in long-chain saturated fatty acids.

11(S)-HETE, an (S) enantiomer of 11(R)-HETE and a type of oxylipin, is non-enzymatically synthesized from arachidonic acid. Compared to its counterpart, 11(S)-HETE levels are found to be elevated in both isolated human plasma and serum, as well as in LPS-stimulated isolated human plasma. Notably, patients with allergic rhinitis exhibit a decrease in 11(S)-HETE levels in their serum following one year of double-mite subcutaneous immunotherapy (DM-SCIT), correlating with an enhanced quality of life, particularly in aspects related to rhinoconjunctivitis.

<p>AcBut, a cleavable linker utilized in the synthesis of Ozogamicin, facilitates the production of agent-linker conjugates for antibody-drug conjugates (ADC) [1].</p>

<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>

<p>ICMT-IN-38 (Compound 42) is an ICMT inhibitor, demonstrating an IC50 value of 0.049 μM [1].</p>

27-Hydroxy Cholestenone, an oxysterol, exhibits elevated levels in Cyp46a-/- mouse brain. It serves as an intermediate in synthesizing dafachronic acid ligands, targeting the DAF-12 nuclear hormone receptor.

O-1057 free base is a water-soluble cannabinoid receptor agonist with antinociceptive properties. RESEARCH USE ONLY.

APJ receptor agonist 7 (compound 37) is an orally active APJ (apelin receptor) agonist (Ki: 0.059 μM). arrestin (EC50: 0.063 μM).

BePI can be a specific intercalator of both double and triple-helical DNA.

BCN-endo-PEG4-NHS is an ADC linker comprising 4 polyethylene glycol (PEG) units and features the lyophilic bidentate macrocyclic ligand, endo-BCN. This structure enables the synthesis of macrocyclic complexes and allows endo-BCN to engage in click chemistry reactions with azide-group-containing molecules to form stable triazoles without the need for catalysts.

10(Z)-Pentadecenoic acid methyl ester is the methyl ester derivative of the fatty acid known as 10(Z)-pentadecenoic acid. This compound serves as a standard for quantifying pentadecenoic acid in vernix caseosa, as indicated by Matreya, LLC. Catalog No. 1210.

2-Hydroxy arachidic acid methyl ester, a hydroxylated fatty acid methyl ester identified in sediment samples from the Harney River and in petroleum ether extracts of I. eriocarpa, serves as a volatile flavoring compound in anhydrous milk fat (AMF). Its presence is diminished upon treatment with lipases lipozyme-435 and TL-IM in a time-dependent fashion. [Matreya, LLC. Catalog No. 1710]

Biotin-PEG4-MeTz, a click chemistry reagent, features a terminal methyltetrazine (MeTz) group for reaction with trans-cyclooctene, facilitating the preparation of biotinylated conjugates [1].

<p>5-Methoxy EiPT, a tryptamine-based designer drug, exhibits structural similarity to 5-methoxy DiPT and 5-methoxy MiPT. Although analytical methods for its identification exist, its biological activity remains unreported. This product is intended for forensic and research applications.</p>

GT-2394 is a histamine H3 receptor agonist.

Betulinic glycine amide, a pentacyclic triterpenoid derivative of betulinic acid, serves as a precursor for synthesizing derivatives with anticancer and antiviral activity.

WAY-634964 is an active molecule.

N-(2-Hydroxyphenyl)picolinamide is an active molecular compound.

CCG-203586 is a novel potent glucosylceramide synthase (GCS) inhibitor.

PCSK9-IN-15 (compound 5) is a potent inhibitor of proprotein convertase subtilisin/kexin 9 (PCSK9, K D <200 nM) that plays a crucial role in cholesterol

NEPP-11 is a selective JNK signaling pathway inhibitor.

O-allyl-AP is a neuroprotective and proliferative agent with significantly higher stimulatory effect than that of allopregnanolone.

YKL-5-124 TFA is a potent, selective, irreversible and covalent inhibitor of CDK7 (IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively).

RORγt Inverse agonist 3 is a potent, selective and orally active inverse agonist of RORγ(EC50s of 0.22 μM and 0.15 μM for hRORγ and RORγt (human IL-17 cells),

Behenamide MEA, a bioactive chemical compound, demonstrates biological activity.

MK-8141 is a renin inhibitor. It displays some antihypertensive efficacy in hypertensive patients.

BMS-538305 is a potent, selective inhibitor of dipeptidyl peptidase IV (DPP-IV).

Spirotetramat is an insecticide that demonstrates efficacy against C. pyrinymphs in vitro (LC50= 6.51-12.53 mg AI/L) and achieves a 99.2% mortality rate in C. pyrinymphs within European pear (P. communis) fields 15 days post-application at a dosage of 27 g/hectare. Additionally, it reduces embryonic viability and nymph survival in O. insidiosus. Spirotetramat exhibits aquatic toxicity by altering protein levels in organisms, specifically by increasing glutathione peroxidase (GPX) and superoxide dismutase (SOD) levels, decreasing malondialdehyde (MDA) levels, and causing lethality in Chinese toad (B. gargarizans) tadpoles (LC50= 6.98 mg/L). Its formulations are utilized in agricultural insect control. Spirotetramat is marketed exclusively for research and analytical applications, formulated for controlled laboratory settings without the availability of bulk sizes.

Potent and selective 5-HT4 receptor antagonist

<p>1,3-Dipalmitoyl-2-oleoyl glycerol, a triacylglycerol, incorporates palmitic acid in the sn-1 and sn-3 positions and oleic acid in the sn-2 position. This compound is present in cocoa butter, Chinese tallow butter, and the palm stearin fraction of palm oil.</p>