Other Inhibitors

<p>TFIIH Modulator-19 induces the dimerization of trichothiodystrophy group A protein to modulate TFIIH transcriptional activity.</p>

<p>TIS108为一种抑制三唑型独脚金内酯生物合成的化合物。它抑制拟南芥的胚胎发生并降低水稻中2′-epi-5-deoxystrigol (epi-5DS)的含量。</p>

<p>U 66985 is a Platelet-activating factor (PAF) receptor antagonist that inhibit the electrophysiological effects of PAF.</p>

RP-52770 is a bioactive chemical.

7-Keto-25-hydroxy Cholesterol, an oxysterol and proposed metabolite of 7-keto cholesterol and 7-dehydro cholesterol, binds to and activates Smoothened (Smo) at the conserved extracellular cysteine-rich domain (CRD) in a reporter assay. Additionally, it enhances the number of EGF high affinity binding sites in normal rat kidney (NRK) cells.

<p>10-SAHSA, an endogenous lipid recently discovered, is part of the FAHFAs, a group of branched fatty acid esters of hydroxy fatty acids. It specifically consists of stearic acid esterified to 10-hydroxy stearic acid. Notably, PAHSAs, closely related to 10-SAHSA, are significantly present in the adipose tissue of AG4OX mice that are glucose tolerant due to the overexpression of the Glut4 glucose transporter in their adipose tissue. Similar to other FAHFAs, which are known to improve glucose tolerance, promote insulin secretion, and possess anti-inflammatory properties, 10-SAHSA is considered a potential bioactive lipid with implications for metabolic syndrome and inflammation management.</p>

14-Pentadecenoic acid, a 15-carbon long-chain fatty acid with an alkene functional group on the terminal carbon of its aliphatic tail, has been observed to undergo oxidation due to the growth of M. cerificans at the expense of the parent alkene. This compound is utilized in the creation of fibrous scaffold biomaterials for tissue engineering purposes and in constructing metallomesogenic side-chain polymers for coating capillary columns in gas chromatography applications.

RXFP1 receptor agonist-6 (Example 7) serves as an agonist for the RXFP1 receptor and effectively suppresses cAMP production in HEK293 cells that stably express

ES 8891 is an inhibitor of renin.

3-Acetyl-6-bromocoumarin is a coumarin derivative that has exhibited potent antioxidant activity, demonstrated at a rate of 56% [1].

<p>3-Formylsalicylic acid acts as a non-competitive inhibitor of estrone sulfatase, with IC50 and Ki values of 150 nM and 120 nM, respectively, inhibiting the enzyme responsible for converting estrone sulfate into estrone. Additionally, this compound is utilized in the synthesis of Schiff bases.</p>

1,3-Dioleoyl-2-stearoyl glycerol, a triacylglycerol, features oleic acid at the sn-1 and sn-3 positions and stearic acid at the sn-2 position, and is identified in butterfat.

Fmoc-D-Lys(N3)-OH is an azide-containing click chemistry reagent utilized in biochemical research [1].

Oxonantenine, an acetylcholinesterase inhibitor, is an oxoaporphine alkaloid from Annona glabra with plant metabolite roles.

Compound 133, also known as Anti-osteoporosis agent-7, is a potential anti-osteoporosis agent that exhibits significant inhibition of osteoclast formation.

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

MF 13 exhibits tumor apoptosis activity.

11-Deoxy-16,16-dimethyl Prostaglandin E2 (11-deoxy-16,16-dimethyl PGE2) is a stable synthetic analog of Prostaglandin E2 (PGE2), acting as an agonist for both EP2 and EP3 receptors. It effectively inhibits gastric acid secretion and ulcer formation in rats, with ED50 values of 1 mg/kg and 0.021 mg/kg, respectively. This compound is also 900 times more potent than Prostaglandin F2α (PGF2α) in inducing contraction of human respiratory tract smooth muscle in vitro.

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

<p>Manoalogue is a synthetic analog of manoalide and phospholipase A2 antagonist.</p>

Anticancer agent 113 possesses anticancer activity [1].

<p>Hydroxy darunavir, a metabolite of the HIV-1 protease inhibitor darunavir, is generated through isobutyl aliphatic hydroxylation of darunavir.</p>

ICMT-IN-8 (compound 30) serves as an inhibitor of ICMT, exhibiting an IC50 value of 0.652 μM [1].

<p>Palmitoleic acid alkyne, an ω-terminal alkyne derivative of palmitoleic acid, facilitates click chemistry applications. This compound has played a crucial role in examining protein palmitoylation processes. Specifically, the cis form of palmitoleic acid alkyne selectively tags wild-type Wnt3a protein within mouse fibroblast L-cells expressing Wnt3a and its secretion in conditioned media, distinguishing itself from the trans form and proving ineffective against the S209A mutant Wnt3a.</p>

Indomethacin acyl glucuronide, a metabolite of the COX inhibitor indomethacin (1), embodies an essential byproduct formed during the metabolic processing of indomethacin.

A1B11 is a selective SIRT2 inhibitor.

Droxinavir Free Base is an experimental protease inhibitor researched by Pharmacia as a treatment for HIV infection.

TASP0412098 is a potent, selective CRTH2 antagonist with oral activity.

CP-664511 is an alpha4beta1/ vascular cell adhesion molecule-1 (VCAM-1) inhibitor with therapeutic potential for allergic airway disease.

JWH-176 is a cannabimimetic indene hydrocarbon, exhibiting high affinity for the central cannabinoid (CB1) receptor (Ki= 26 nM), originally synthesized to investigate hydrogen bonding and aromatic stacking's roles in CB1 receptor docking studies. Intended for forensic and research applications, this compound's design facilitates the exploration of CB1 receptor interactions.

<p>12-Bromododecanoic acid, a halogenated derivative of lauric acid, serves in the synthesis of clickable myristic acid derivatives and functions as a model fatty acid ligand for elucidating the X-ray crystal structure of bovine β-lactoglobulin-ligand complexes. This compound, at a concentration of 10 µg/ml, has been shown to diminish virion DNA in the culture supernatant of primary hepatocytes from a duckling model of hepatitis B virus (HBV) infection and exhibits inhibitory activity against HIV replication in CEM-SS T cells with an EC50 value of 38 µM.</p>

<p>LVN84663 is a valuable reagent for identifying blood coagulating protease, first documented in patent DE 3516579.</p>

6-Azidohexanoic acid, a six-carbon saturated fatty acid featuring an ω-terminal azide group, serves as a versatile linker for bioconjugation via copper(I)-catalyzed cycloaddition reactions (click chemistry). This functionality enables its initial acylation to a compound, forming a derivative that can subsequently be conjugated to another compound through click chemistry, facilitating the synthesis of complex molecules.

DDR1/2 Inhibitor-2 (Example 31) serves as an inhibitor of DDR1/DDR2, exhibiting IC50 values below 100 nM.

<p>"(1R,4R)-N-desmethyl Sertraline, a metabolite of the selective serotonin reuptake inhibitor (SSRI) sertraline, plays a key role in its pharmacological effects."</p>

Omiloxetine, an SSRI developed by Ferrer Internacional, was shelved in 2005 after preclinical trials.

L-Allooctopine competitively inhibits D-octopine [1].

CZh226: Potent, selective PAK4 inhibitor (Ki=9 nM), weak on PAK1 (Ki=3112 nM), hinders A549 cell migration and invasion in vitro.

<p>WAY-658494 is an (active) compound.</p>

<p>Berotralstat HCl is a selective plasma kallikrein inhibitor, reducing pain and swelling in HAE by blocking bradykinin release.</p>

<p>1-Palmitoyl-2-lauroyl-rac-glycerol, a diacylglycerol, features palmitic acid at the sn-1 position and lauric acid at the sn-2 position.</p>

Anticancer agent 61, an oral drug, inhibits HepG2, Bel-7402, MCF-7 cell growth; IC50: 1.12, 1.97, 1.08 μM respectively. Stops tumor growth.

BMS-187308 is an endothelin-A (ETA) selective antagonist.

4'-Azidothymidine 5'-triphosphate targets HIV-1 reverse transcriptase and human DNA polymerases alpha & beta.

<p>Activated T Subunit is employed in synthesizing exon-jumping oligomer conjugates that target specific sites within the human anti-muscular atrophy protein gene</p>

FR-181877: nonprostanoid PGI2 agonist, ADP-induced platelet aggregation inhibitor (IC50=0.081μM), orally bioavailable (56%), long half-life (4.3h) in rats.

1,3-Dimyristoyl-2-eicosapentaenoyl glycerol (MEM) is a triacylglycerol with myristic acid at the sn-1 and sn-3 positions and eicosapentaenoic acid at the sn-2 position. The presence of myristoyl groups in MEM does not impact the oxidative stability of eicosapentaenoic acid (EPA) during prolonged storage at 25°C.

Asem F-18 is a radiolabeled antagonist for imaging the α7-nicotinic acetylcholine receptor with PET .

GHK-Cu acetate, a complex of the tripeptide Gly-His-Lys and a copper(II) ion, exhibits wound healing and anti-inflammatory properties. It enhances fibroblast proliferation, collagen production, and the release of pro-matrix metalloproteinase-2 (MMP-2) and glycosaminoglycans (GAGs), while also increasing decorin expression in rat wound tissue. Furthermore, at a concentration of 10 µM, it reduces levels of reactive oxygen species (ROS), interleukin-6 (IL-6), and tumor necrosis factor-alpha (TNF-α) in LPS-stimulated RAW 264.7 cells. Additionally, GHK-Cu at 10 µg/g mitigates LPS-induced reductions in lung superoxide dismutase (SOD) activity and glutathione (GSH) levels, decreases the accumulation of cells and total protein in bronchoalveolar lavage fluid (BALF), and thus, attenuates acute lung injury in mice.

1-Myristoyl-3-palmitoyl-rac-glycerol, a diacylglycerol, features myristic acid at the \(sn\)-1 position and palmitic acid at the \(sn\)-3 position.

"1-Lauroyl-2-palmitoyl-rac-glycerol is a diacylglycerol featuring lauric acid (at the sn-1 position) and palmitic acid (at the sn-2 position)."

Compound 43, also known as compound 3, is a 6-methoxyflavonol glycoside exhibiting anti-inflammatory activity.

<p>SOS1-IN-8 is an inhibitor of SOS1 and acts on SOS1-G12D (IC50: 11.6 nM) and SOS1-G12V (IC50: 40.7 nM).</p>

Antiproliferative Agent-41 (Compound 14), classified as indanorine [1], functions as an antiproliferative compound.

<p>Indacrinone is an investigational diuretic.</p>

Dityrosine, an oxidation product of protein formed through the intermolecular cross-linking of tyrosyl radicals from the reactive oxygen species (ROS) and tyrosine interaction, is associated with decreased hippocampal expression of NMDA receptor subunits Nr1, Nr2a, and Nr2b when administered intragastrically at 320 µg/kg per day, leading to memory impairments in mice as evidenced by their performance in a novel object recognition test. Additionally, it raises fasting blood glucose levels while reducing plasma insulin levels and the pancreatic expression of insulin synthesis-related genes Ins2, Pdx1, and MafA. Increased dityrosine levels have been positively linked to a range of diseases, including autism spectrum disorder, cataracts, Alzheimer's disease, Parkinson's disease, atherosclerosis, and cystic fibrosis.

C12 3'-sulfo Galactosylceramide (d18:1/12:0) is a lipid molecule that can be used in life science related research. The CAS number of C12 3'-sulfo Galactosylceramide (d18:1/12:0) is 852100-88-0.

<p>Compound 3 (MRV03-069) is a selective inhibitor of colibactin-activated peptidase (ClbP), effectively impeding colibactin's genotoxic effects on eukaryotic</p>

CP21: Iron chelator (3:1 ratio), anti-malarial; inhibits prostaglandin I2, protects rat aorta, HT22 cells. Enhances iron excretion in rabbits.

ICMT-IN-50 (compound 3) serves as an inhibitor of ICMT with an IC50 value of 0.31 µM [1].

PPO-IN-3 (Compound 8ad) is a potent PPO inhibitor, exhibiting a Ki value of 0.67 nM and possessing post-emergence herbicidal properties suitable for weed

<p>NIR-H2O2: Cell-permeable, NIR fluorescent sensor; activates with H2O2 for clear NIR signal.</p>

Cyclopentenyl uracil 是一种无细胞毒性的尿苷激酶 (uridine kinase) 抑制剂，可有效阻断完整小鼠体内宿主和肿瘤组织对循环尿苷的回收。

DU172 is the tyrosine-targeted covalent adenosine A1 receptor antagonist.

AZD6126 (ANG-453), a water-soluble prodrug converted to N-acetylcolchinol in vivo, potentially treats solid tumors by inhibiting angiogenesis and tubulin.

L-159884 is a radiolabelled, nonpeptide angiotensin II antagonist that is useful for angiotensin II, AT1 receptor imaging

<p>TRA 418 is a TP antagonist.</p>

C17 dihydro Ceramide (d18:0/17:0) is a lipid molecule that can be used in life science related research. The CAS number of C17 dihydro Ceramide (d18:0/17:0) is 1388156-40-8.

<p>Chloramine-T serves as a versatile reagent in numerous synthetic procedures, including aminohydroxylation, allylic amination, as a nitrogen source in aziridination reactions of alkenes and olefins, and for the deprotection of thio groups in sulfur-containing molecules. Additionally, it plays a role in the synthesis of Factor Xa inhibitors. At a concentration of 0.2% w/v, Chloramine-T acts as an effective antiseptic agent with bactericidal properties against S. epidermidis, S. aureus, E. faecalis, E. coli, P. mirabilis, and E. cloacae.</p>

1dinor-12-oxo-Phytodienoic acid (dinor-OPDA) serves as an intermediate in the biosynthesis of jasmonic acid from hexadecatrienoic acid, playing a crucial role in the jasmonate pathway in plants. This pathway oxygenates and modifies certain unsaturated fatty acids to produce plant hormones critical for processes such as senescence, flower development, mechanotransduction, and response to herbivory. Additionally, dinor-OPDA can be incorporated into glycerolipids and galactolipids, including specific arabidopsides.

C24 (2'(R)-hydroxy) dihydro Ceramide (d18:0/24:0) is a lipid molecule that can be used in life science related research. The CAS number of C24 (2'(R)-hydroxy) dihydro Ceramide (d18:0/24:0) is 164989-36-0.

EXP3892 is an angiotensin II receptor antagonist.

Abikoviromycin has an antiviral activity.

VU0531245 is a potent inhibitor of the SLACK (Sequence Like A Calcium-activated K+) channel, exhibiting an IC50 of 2.1 μM [1].

<p>LMP7-IN-2 is an inhibitor of LMP7 and may be utilized in the treatment of associated inflammatory diseases and disorders [1].</p>

<p>"20α-Dihydro Prednisolone, a prednisolone metabolite, is detected in cattle urine post-adrenocorticotropic hormone (ACTH) administration but absent in both naturally stressed and non-stressed cattle."</p>

ICMT-IN-29, also known as compound 66, effectively inhibits ICMT with an IC50 value of 0.019 μM [1].

XR9051 Hydrochloride, a potent modulator of P-glycoprotein-mediated multidrug resistance (MDR), inhibits the binding of cytotoxics to P-glycoprotein.

<p>TG11-77 hydrochloride is a potent, selective, and water-soluble EP2 receptor antagonist that is brain-permeable, demonstrating a KB value of 9.7 nM.</p>

Compound 6i, an anticancer agent, exhibits promising activity against breast adenocarcinoma [1].

<p>Porcn-IN-2 (Example 107) is a potent Wnt pathway inhibitor, exhibiting an IC50 of 0.05 nM.</p>

TRPC3/6-IN-2 is a potent inhibitor of TRPC3 and TRPC6, exhibiting IC50 values of 16 nM for TRPC3 and 29.8 nM for TRPC6, respectively [1].

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

T-0201 (TA 0201): Potent, long-acting, oral selective ETA antagonist; blocks ET-1-induced contraction in rabbit arteries.

<p>Phe-Pro-Ala-pNA is a chromogenic substrate utilized for assessing tripeptidyl peptidase activity.</p>

WAY-299375 is a research-active molecule targeting amyloid diseases and synucleinopathies.

Δ7(Z)-C14-HSL (Compound 12), an immunosuppressive agent, inhibits the proliferation of mouse splenic cells, exhibiting an IC 50 of 17 μM. It holds promise for exploring its role as a molecular mechanism in TNF-R-driven immune diseases, including autoimmune disorders like psoriasis, rheumatoid arthritis, and type 1 diabetes [1].

RO5068760, a selective MEK1/2 inhibitor, effectively targets a range of tumors, particularly B-RafV600E mutants, with an IC50 of 0.025 μM.

<p>NNMT-IN-4 (compound 38) is a selective, uncompetitive inhibitor of nicotinamide N-methyltransferase (NNMT) with in vitro biochemical and cell-based assay IC50</p>

SB-682330A is a Raf kinase inhibitor.

JTT 130 is an agent of hypolipidemic. It inhibits microsomal triglyceride transfer protein.

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

<p>AS-99, a potent ASH1L inhibitor with anti-leukemia effects, blocks cell growth and triggers apoptosis. IC50: 0.79µM; Kd: 0.89µM.</p>

BMS-561392 formate, the formate derivative of BMS-561392, functions as a TNF alpha-converting enzyme (TACE) inhibitor and an ADAM17 blocker. It is utilized in the research of inflammatory bowel disease [1] [2].

1-Palmitoyl-2-linoleoyl-3-stearoyl-rac-glycerol, a triacylglycerol, comprises palmitic acid (at the sn-1 position), linoleic acid (at the sn-2 position), and stearic acid (at the sn-3 position). This compound is present in mature human milk and various plant oils.

<p>Furegrelate sodium (U-63557A) is an orally active thromboxane synthase inhibitor with an IC50 of 15 nM in platelets.</p>

Calcium polystyrene sulfonate, an ion-exchange resin, lowers potassium for hyperkalemia research.

<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>

VT-1598 tosylate is a selective, orally active antifungal compound that targets CYP51. It demonstrates efficacy against C. auris.

WEHI-345 analog is an Src inhibitor.

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

BDW568, a prodrug of BDW-OH, serves as a stimulator of interferon genes (STING) agonist.

(-)-15-Deoxyspergualin trihydrochloride exhibits potent antitumor properties and demonstrates significant inhibition activity against mouse leukemia L-1210 [1].

BTZO-15 is a novel ARE activator, ameliorating DSS- and TNBS-induced colitis in rats.