Other Inhibitors

<p>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.</p>

<p>Prostaglandin E1 ethanolamide, an analog of Prostaglandin E1 (PGE1), can potentially inhibit the GLI2-induced expression of target genes such as Gli1 and Ptch1, thereby reducing tumor growth [1].</p>

<p>ORM-13070 is a selective antagonist radioligand for the α2C adrenoceptor subtype. ORM-13070 C-11 is under investigation in clinical trial.</p>

<p>U 19052 is a Leukotriene D4 antagonist.</p>

<p>5'-Ethynyl-2'-deoxycytidine (EdC) functions as a nucleoside analog effectively inhibiting the replication of herpes simplex virus-1 (HSV-1) KOS strain with an ID50 of 0.2 μg/mL. Additionally, it decreases virus-induced cytopathogenic effects in PRK cells for HSV-1, HSV-2, and vaccinia virus strains, demonstrating MIC values between 0.2 to 5 μg/mL. EdC acts as a thymidylate synthetase inhibitor, selectively impacting the DNA incorporation rates of [1',2'-3H]deoxyuridine compared to [CH3-3H]deoxythymidine in PRK cells with ID50s of 3 and 120 μg/mL, respectively. It further inhibits thymidine synthetase and curtails L1210 cell proliferation, a process reversible by deoxythymidine (ID50s are 4.4 and 1,000 μg/mL, respectively). Also, EdC is utilized in monitoring DNA synthesis and cellular replication through click chemistry conjugation, linking its ethynyl group with the azido group of various fluorochromes.</p>

<p>CGP 57813 is a lipophilic compound, which can be used as an inhibitor of HIV-1 protease.</p>

<p>PARPYnD: Photoaffinity PARP probe; inhibits PARP2, PARP1, PARP6 (IC50: 6, 38, 230 nM); tags PARP1/2 with N3 fluorescent probe.</p>

<p>KMG-301AM, a fluorophore, allows for tracking mitochondrial changes over time with pseudo-colored imagery.</p>

<p>GNE-3476 is an NMDA PAM with low GluN2A efficacy, AMPAR activity, and weak at GluN2B receptors.</p>

<p>Docosapentaenoyl chloride, a more reactive derivative of the ω-3 fatty acid known as docosapentaenoic acid (DPA) found in fish oils, is an advanced substance stemming from its free fatty acid form.</p>

<p>Resorstatin is a bioactive chemical.</p>

TAMRA-probe 1 is a fluorescent probe for labeling.

<p>VPC 32183 (S) is an LPA1/LPA3 antagonist with no agonist effect on human/mammal LPA receptors.</p>

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

<p>Kdo Azide is a metabolic labeling reagent and a click chemistry reagent that contains an azide group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with alkyne-containing molecules. Additionally, it can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.</p>

<p>STING modulator-3, a 43.1 nM R232 STING inhibitor, doesn't affect IRF-3 or TNF-β in THP-1 cells.</p>

<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).</p>

<p>SCH-538415: Microbial acyl carrier protein synthase inhibitor, IC50 4.19µM; anti-Staphylococcus aureus.</p>

<p>Etidocaine Hydrochloride (W19053) is a long-acting anesthetic and a blocker of the voltage-gated sodium channel.</p>

<p>OR-486 is an inhibitor of catechol-O-methyl-transferase(COMT) and can be used to prepare the molybdenum (VI)- 3,5-Dinitrocatechol complex.</p>

<p>SRX246: potent CNS-penetrant V1a antagonist (Ki=0.3 nM), inactive at V1b/V2, negligible binding at 64 other receptor classes.</p>

<p>Emzeltrectinib is a potent tyrosine kinase inhibitor with antineoplastic activity .</p>

<p>1,1'-(Azodicarbonyl)dipiperidine (ADDP) serves as a widely employed reagent in the Mitsunobu reaction, facilitating the condensation between an alcohol and an acidic compound. Moreover, ADDP has found application in synthesizing agonists for the G protein-coupled receptor 120 (GPR120) with potential antidiabetic effects as well as in the creation of triple agonists for peroxisome proliferator-activated receptor α (PPARα), PPARγ, and PPARδ.</p>

<p>GGTI-2133: potent GGTase I inhibitor, IC50=38 nM; blocks inflammatory cell invasion in mice asthma.</p>

<p>C.I. Vat Black 27 is a black dye.</p>

<p>1-(2-fluorophenyl)-3-[5-(2-methoxyphenyl)-1,3,4-thiadiazol-2-yl]urea is a chemical compound.</p>

<p>RO116-4875/608 is bioactive chemical.</p>

<p>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.</p>

<p>JNJ-17029259 is an orally selective, potent inhibitors of the vascular endothelial growth factor receptor-2 (VEGF-R2).</p>

<p>ICMT-IN-51 (compound 43) serves as an ICMT inhibitor with an IC50 value of 0.55 μM [1].</p>

<p>Antiproliferative Agent-39 (Compound 12) effectively inhibits the proliferation of various cancer cell lines, including A549, SNU-638, Col2, HT1080, and MCF-7,</p>

<p>ICMT-IN-45 (compound 24) serves as an ICMT inhibitor, demonstrating an IC50 value of 0.132 μM [1].</p>

<p>CD08108 is a MC1R agonist.</p>

<p>hDDAH-1-IN-2 is an orally active human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1) inhibitor.</p>

<p>Xenognosin is a biochemical.</p>

<p>C16((±)-2'-hydroxy) dihydro Ceramide (d18:0/16:0) is a lipid molecule that can be used in life science related research. The CAS number of C16((±)-2'-hydroxy) dihydro Ceramide (d18:0/16:0) is 190249-36-6.</p>

<p>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.</p>

<p>ICMT-IN-30 (compound 67) is an ICMT inhibitor with an IC50 value of 0.27 μM [1].</p>

<p>Corey lactone aldehyde benzoate serves as a versatile, chiral intermediate in the synthesis of prostaglandins and their analogs.</p>

<p>CYP11A1-IN-1 (compound 30) is a selective inhibitor of the enzyme CYP11A1, displaying an IC50 ranging from 201-2000 nM.</p>

<p>TBC-3486 is a novel potent inhibitor of integrin α4, being 200-fold more potent in inhibiting α4β1 than α4β7.</p>

Bt2cGMP sodium is a cGMP analog, activates PKG, inhibits platelet [3H]-arachidonate, and induces analgesia via K+ channels.

<p>GYKI-16084 is a postsynaptic alpha2 receptor blocker with potential efficacy in the treatment of benign prostatic hyperplasia.</p>

<p>Mioflazine hydrochloride anhydrous is a nucleoside transport inhibitor that acts on adenosine to improve sleep.</p>

<p>S-Octylglutathione is a competitive inhibitor of glutathione S-transferase (GST) [1].</p>

<p>FTI-2600 is a farnesyltransferase inhibitor.</p>

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

<p>WAY-301398 (6-methoxynaphthalene) can bind to protein kinase C (PKC).</p>

<p>PD-321852, a Chk1 inhibitor, boosts gemcitabine's effect in pancreatic cancer cells, varying from minimal in Panc1 to &gt;30-fold in MiaPaCa2.</p>

<p>Biotin-PEG3-amide-C2-CO-Halofuginone is a derivative of halofuginone applicable in cancer research [1].</p>

<p>WAY-312084 is an active compound.</p>

<p>1,2-O-Dioctadecyl-rac-glycerol, a saturated dialkyl glyceryl ether featuring octadecyl groups at the sn-1 and sn-2 positions, closely resembles the structure of diacylglycerol. This similarity allows its use in model lipid bilayers to explore the dynamics of different biological membrane compositions.</p>

<p>Ipflufenoquin, an insecticide, effectively combats primary apple scab infections. Its application is optimal between the stages of half an inch of green and fruit set [1].</p>

<p>H-D-Aha-OH (hydrochloride), a click chemistry reagent, contains an azide group.</p>

<p>UDP-GalNAz disodium (UDP-N-azidoacetylgalactosamine disodium) serves as an analogue to UDP-GalNAc, the substrate for various N-acetylgalactosaminyltransferases that catalyze the transfer of GalNAc onto saccharide or peptide acceptors. As a click chemistry tool, UDP-GalNAz features an azide group enabling it to partake in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with alkyne-bearing molecules. Additionally, it can engage in strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.</p>

<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>1,2,3-Tri-11(Z)-eicosenoyl glycerol, a triacylglycerol with 11(Z)-eicosenoic acid at the sn-1,sn-2, and sn-3 positions, serves as an internal standard for quantifying triacylglycerols in seed and olive oils.</p>

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

<p>Necrostatin-1 (Nec-1) (inactive control), an inactive analog of Necrostatin-1, functions as a potent inhibitor of necroptosis [1].</p>

<p>Ciprostene, a PGI2 stable analog, is less potent, induces hypotension, tachycardia, and inhibits platelet aggregation in monkeys.</p>

<p>Deacetylanisomycin is a potent growth regulator in plants Anisomycin and protein synthesis inhibitor. It is an inactive derivative of Anisomycin.</p>

<p>STING agonist-3: non-nucleotide, selective, anti-tumor with pEC50=7.5, pIC50=9.5, could enhance cancer therapy.</p>

<p>2-C-Methylene-myo-inositol oxide (NSC 45109), an inositol derivative, promotes pseudohyphal growth in Saccharomyces species [1].</p>

<p>10,11-Dihydro-10,11-dihydroxy Carbamazepine, a metabolite of the anticonvulsant carbamazepine and the antiepileptic prodrug oxcarbazepine, is produced through the biotransformation of carbamazepine via a carbamazepine 10,11-epoxide intermediate by epoxide hydrolase, and from oxcarbazepine via a 10,11-dihydro-10-hydroxy carbamazepine intermediate. This compound has been detected in wastewater effluent, highlighting its environmental presence following pharmaceutical use.</p>

<p>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>

<p>1,2-Didocosanoyl-3-myristoyl-rac-glycerol, a triacylglycerol, features docosanoic acid at both the sn-1 and sn-2 positions, and myristic acid at the sn-3 position.</p>

<p>Y-27152 is a prodrug of the KATP (Kir6) channel opener Y-26763 and is a long-acting K+ channel opener.</p>

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

<p>EZH2-IN-8 inhibits EZH2, potentially useful in cancer research, as per patent WO2021129629A1.</p>

<p>Acifluorfen-methyl, a photobleaching herbicide [1], functions as an inhibitor of the enzyme protoporphyrinogen oxidase (Protox), which is crucial for heme and</p>

<p>Cyclotheonellazole A inhibits elastase (IC50=0.034nM) &amp; chymotrypsin (IC50=0.62nM), a natural macrocyclic peptide.</p>

<p>AP-24567 is a CYP3A4-mediated metabolite.</p>

<p>DAO-IN-1 (compound 10) is a potent DAO (D -amino acid oxidase) inhibitor that ameliorates schizophrenia by increasing D -serine levels in the brain.</p>

<p>SRI 6409-94, a teratogenic analogue of Ro 13-6298, is orally active and utilized as a molecular tool to investigate the impact of retinol's three-dimensional</p>

<p>Sodium zirconium cyclosilicate (UXSi-9) is a cation exchanger and a K+ binder used in the treatment of hyperkalemia.</p>

<p>Windaus ketone functions as a vitamin D (VD) synthesis inhibitor.</p>

<p>Serine Hydrolase Inhibitor-21 (compound 8), a pyridine-based serine hydrolase inhibitor, exhibits a K i of 429 nM against BuChE, and shows promise for Alzheimer</p>

<p>E235, an activator of the transcription factor 4 (ATF4), enhances the integrated stress response (ISR) and DNA damage response, thereby reducing cell viability</p>

<p>S07-1066, an aldo-keto reductase 1C3 (AKR1C3) inhibitor, enhances doxorubicin (DOX) cytotoxicity by selectively inhibiting AKR1C3-mediated reduction of DOX and</p>

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

<p>AD 0261 is a radical scavenger. It has a strong inhibitory action on the generation of lipid peroxides and superoxide anions.</p>

<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>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>

<p>4-Hydroxy Omeprazole sulfide, a metabolite of the proton pump inhibitor omeprazole, has been detected in wastewater effluent.</p>

<p>UK 55444 is a potent calcium antagonist.</p>

<p>AKR1C3-IN-6: Strong AKR1C3 inhibitor (IC50: 0.31 μM); weak on AKR1C2 (IC50: 73.23 μM); shows antitumor effects.</p>

<p>Flucythrinate is an insecticide.</p>

<p>(+)-Carbovir is a nucleoside analog with increased chemical stability and increased metabolic stability.</p>

<p>Atherospermidine is a smooth muscle relaxant aporphines from Artabotrys maingayi.</p>

<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</p>

<p>Cindunistat, a potent oral iNOS inhibitor for symptomatic knee osteoarthritis.</p>

<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>

<p>9-Keto Fluprostenol Isopropyl Ester, an ester derivative of the FP receptor agonist fluprostenol, undergoes oxidation at carbon 9. This compound serves as a potential prodrug for 9-keto fluprostenol, which may function as an agonist at EP receptors. Additionally, it is considered a possible metabolite of fluprostenol isopropyl ester (travoprost), drawing parallels to the metabolism of latanoprost by 15-hydroxyprostaglandin dehydrogenase observed in monkey cornea. Furthermore, certain F-series prostaglandins, such as 6-keto prostaglandin F1α (PGF1α), undergo conversion to their E-series counterparts in isolated human platelets, highlighting a metabolic pathway of relevance.</p>

<p>CS640 is a selective calmodulin-dependent kinase inhibitor, targeting multiple isoforms, namely CaMK1D, CaMK1B, CaMK1A, CaMK1G, PIP5K1C, MEK5, RIPK4, and MLK3,</p>

<p>Anticancer agent 162 (compound 1d) serves as a potent theranostic agent, selectively inducing oncosis in Hela cells with pronounced lipophilicity and</p>

<p>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>

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

<p>4'-Azidothymidine exhibits potent and selective activity against the human immunodeficiency virus.</p>

<p>TIE-2/VEGFR-2 kinase-IN-3, a benzimidazole derivative, serves as a potent inhibitor of the tyrosine kinase receptors TIE-2 and VEGFR-2, exhibiting IC50 values</p>

<p>1,2-Diarachidoyl-rac-glycerol is a diacylglycerol featuring arachidic acid at both the sn-1 and sn-2 positions.</p>

<p>SOMG-833 HCl is a selective inhibitor of c-MET. It acts by blocking c-MET dependent neoplastic effects and exerting antitumor activity.</p>

<p>ML 298 hydrochloride is a phospholipase D2 (PLD2) inhibitor.</p>

<p>(R)-Avanafil ((R)-TA1790) is a selective phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.2 nM, utilized for the research of erectile dysfunction [1</p>

<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.</p>