Other Inhibitors

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

WAY-312491 is an active compound.

(R)-Butaprost (free acid) is a prostaglandin E2 (PGE2) analog exhibiting high EP2 receptor subtype selectivity, commonly used to delineate EP receptor

Ganoderic acid F inhibits the proliferation of HeLa human cervical carcinoma cells with IC(50) values of 19.5+/-0.6 microM.

corticotropin-releasing factor receptor 1 (CRF1) antagonist

CK 3197 is a selective positive inotropic agent for the treatment of congestive heart failure. It has hemodynamic and myocardial energetic effects.

Mivazerol hydrochloride is an alpha 2-adrenoceptor agonist.

TA-606 is an angiotensin type 1 receptor antagonist with antihypertensive activity.

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].

Leteprinim (AIT 082 acid) is an hypoxanthine derivative that stimulates in vitro neurite outgrowth and the production of adenosine and neurotrophins from

N8-Acetylspermidine dihydrochloride is a polyamine that regulates ischemic cardiac apoptosis and resultant cardiac dysfunction.

PF-06862309 is a PI3K inhibitor

SDB-006, a cannabimimetic indole, exhibits affinity for central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors, with EC50 values of 19 nM and 134 nM, respectively. This compound emerged from investigations into JWH 018 adamantyl carboxamide, a related substance known for its illicit sale in herbal mixes. SDB-006 is designated exclusively for research and forensic applications.

AGN-201904Z is a slow-release, acid-resistant pro-PPI that turns into omeprazole, offering extended acid suppression.

ICI-185282 is a potent thromboxane receptor antagonist.

TSR011-isomer, a TrKA/ALK inhibitor, is used potentially for the treatment of solid tumours and lymphoma.

HDM-201 succinate is an orally bioavailable human double minute 2 homolog (HDM2) inhibitor with potential antineoplastic activity.

JNJ-3790339, a Ritanserin analogue, is a potent DGKα inhibitor with 9.6 μM IC50, enhancing T-cell activation and toxic to cancer cells.

1,3-Diarachidoyl glycerol, a diacylglycerol featuring arachidic acid at the sn-1 and sn-3 positions, is identified within enzymatically randomized pig lard.

Antiparasitic agent-8 (Compound 9) exhibits potent antiparasitic activity against Hymenolepis nana, while demonstrating low levels of cytotoxicity [1].

Spermine (N3BBB), a click chemistry reagent with an azide group, facilitates diverse biochemical studies [1].

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.

ICMT-IN-4 (compound 28) serves as an inhibitor of ICMT, exhibiting an IC50 value of 0.27 μM [1].

3'-Ethoxy spinosyn L, a minor component in the insecticide spinetoram, is utilized in certain formulations for its insecticidal properties. Marketed solely for research and analytical purposes, it is designed for controlled laboratory use with no option for bulk purchase.

B 581 is an inhibitor that specifically blocks farnesylated.

D-Carnitine, an orally available isomer of the essential nutrient L-carnitine, facilitates the transport of long-chain fatty acids into the mitochondrial matrix for beta-oxidation. Additionally, D-Carnitine exhibits antiparasitic activity [1] [2] [3].

β-Catenin-IN-4 is a β-catenin inhibitor characterized by a K_i value of 0.64 μM.

Prostaglandin F2α (PGF2α) 1,9-lactone, a lipid-soluble internal ester of PGF2α, demonstrates resistance to hydrolysis by human plasma esterases, maintaining its structure even after 20 hours of incubation under physiological conditions. Unlike PGF2α, this compound exhibits minimal antifertility and vasoactivity.

Bioethanomethrin is a biochemical.

EC18 is a bioactive chemical.

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

Urocortin II, a neuropeptide hormone within the corticotropin-releasing factor (CRF) family—which comprises mammalian CRF, urocortin I, urocortin III, frog sauvagine, and piscine urotensin I—displays 34, 43, and 37-40% sequence homology with rat and human CRF, human urocortin I, and human urocortin III, respectively. This compound enhances rabbit ventricular myocyte shortening and relaxation in both a time- and concentration-dependent manner. In vivo studies reveal that urocortin II lowers arterial blood pressure in both normotensive and spontaneously hypertensive rats through peripheral CRF2 receptor agonism, inducing dose-dependent tachycardia and hypotension at doses of 3 and 30 pmol/kg. Additionally, it mitigates the visceral pain response to colorectal distension at 10 and 20 μg/kg in conscious rats and delays gastric emptying in mice.

ICMT-IN-28 (compound 65) serves as an inhibitor of ICMT, exhibiting significant potency with an IC50 value of 0.008 μM [1].

Rel-HDMP-28 hydrochloride (Compound 2g) is an analogue of methylphenidate, exhibiting selective affinity for the serotonin transporter (SERT) with a binding constant (Ki) of 105 nM [1].

17-Phenyl-18,19,20-trinor-PGD2 (17-Phenyl-PGD2), an analogue of prostaglandin D2 (PGD2), acts as a potent inhibitor of platelet aggregation induced by adenosine diphosphate (ADP), exhibiting an IC50 value of 8.4 μM, compared to PGD2's IC50 of 18.6 nM. Additionally, it serves as a weak agonist for cyclic AMP accumulation [1].

ZINC08792229 is a novel inhibitor of SIRT1.

EP2 receptor agonist 4 selectively activates the EP2 receptor with an efficacy concentration (EC50) of 43 nM [1].

1-Palmitoyl-2-Arachidonoyl-sn-glycero-3-PC is a phospholipid found in biological membranes and contains palmitic acid and arachidonic acid in its structure.

ONO-8539 is a prostanoid EP1 receptor antagonist.

GJH-166 is an analog of dopamine that has been shown to inhibit adrenergic transmission in canines.

RGB-1 is a small molecule that stabilizes the RNA G-quadruplex structure and enhances G-quadruplex-mediated RNA translation inhibition.

PF-06260414 is a selective androgen receptor modulator or SARM used to treat muscle weakness.

ICMT-IN-21 (compound 6ag) is an ICMT inhibitor with an IC50 value of 8.8 µM, featuring sulfonamide-modified farnesyl cysteine (SMFC).

JYL-1511 is the TRPV1 channel partial agonist.

(+)-Chloroquine, an aminoquinoline drug, inhibits the in vitro terminal glycosylation of angiotensin-converting enzyme 2 (ACE-2) [1].

1,3-Dilinoleoyl glycerol, an unsaturated diacylglycerol featuring linoleic acid (18:2) side-chains at the C-1 and C-3 positions, is valuable for lipid research.

JWH 080 is a synthetic cannabinoid that exhibits affinity for both central CB1 receptors (Ki = 5.6 nM) and peripheral CB2 receptors (Ki = 2.2 nM) in vitro. The in vivo physiological and toxicological characteristics of this compound remain uncharacterized. It is designed for forensic and research purposes.

Metesind, a thymidylate synthase inhibitor, is used potentially for the treatment of brain cancer and solid tumours.

Oxilorphan is a μ-opioid blocker and a weak κ-opioid activator; similar to naloxone in strength; can cause hallucinations and dysphoria.

AH-9700 fumarate, salt of AH-9700, treats frequent urination from cystitis, unlike oxybutynin.

JNJ-42259152 is a phosphodiesterase 10A PET tracer.

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

Ledazerol is a vasodilator.

WAY-649123 is an active molecule that exhibits (in vitro) antagonistic properties against (alpha-1A adrenergic receptors), with a (pKi) of 8.9.

FK788 is a diphenylcarbamate derivative that functions as a highly potent and selective IP agonist.

ICMT-IN-42 (compound 21) serves as an ICMT inhibitor, demonstrating potency with an IC50 of 0.054 μM [1].

VU0155069 hydrochloride (CAY10593 hydrochloride) is a potent and selective inhibitor of phospholipase D (PLD), exhibiting IC50 values of 46 nM for PLD1 and 933 nM for PLD2. It effectively inhibits the migration of both human and mouse breast cancer cell lines [1] [2].

UDM-001651: oral PAR4 antagonist, IC50=4 nM, Kd=1.4 nM, antiplatelet IC50=25 nM in γ-thrombin assay.

Cintirorgon (LYC-55716) is an oral RORgamma agonist with immunomodulatory and anticancer effects.

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

C-6 NBD-dihydro-Ceramide, a biologically active, fluorescent analog of short-chain ceramides, features membrane permeability.

<p>RO116-9132/238 is a bioactive chemical.</p>

Compound 1 (Anti-inflammatory agent 44) is a 6-methoxyflavonol glycoside exhibiting anti-inflammatory properties, and it can be extracted from the aerial parts

FTY720, an immune modulator, down-regulates sphingosine-1-phosphate (S1P) receptors, enhances the activity of sphingosine transporter Abcb1 and leukotriene C4 transporter Abcc1, and inhibits cytosolic phospholipase A2 activity. Its efficacy relies on in vivo phosphorylation by sphingosine kinases, resulting in FTY720-phosphate which also down-regulates S1P receptors. NBD-FTY720, a fluorescently-labeled analog of FTY720, retains the hydroxy methyl side chain targeted for phosphorylation, suggesting potential phosphorylation in vivo.

HA-2a inhibits the JAK2/STAT3 pathway by downregulating circDcbld2 expression in RAW264.7 cells [1].

GLF (H-Gly-Leu-Phe-OH), a tripeptide isolated from α-lactalbumin with immunostimulatory properties, prevents alopecia, epidermal thickening, and adipocyte layer

17-Phenyl trinor Prostaglandin E2 (17-phenyl trinor PGE2) is a synthetic analog of PGE2, functioning as an agonist at the EP1 and EP3 receptors. It induces contraction of the guinea pig ileum at a 11 µM concentration and displays slightly less potency than PGE2 in stimulating the gerbil colon and rat uterus. Notably, with an ED50 value of 350 µg/kg, 17-phenyl trinor PGE2 exhibits 4.4 times greater antifertility efficacy in hamsters compared to PGE2.

Tomicorat is an anti-inflammatory agent.

2-Ethynyl Adenosine, Adenosine derivative, tracks novel polyadenylated transcription, non-radioactive AMPylation reporter.

p-NH2-CHX-A"-DTPA is a bifunctional chelating agent [1].

CCPG is an agonist of excitatory Amino Acid.

1,2,3-Trimyristoleoyl glycerol, a triacylglycerol featuring myristoleic acid at the sn-1, sn-2, and sn-3 positions, is detected in Idiazabal cheese.

Benzamide, N,N-bis(5-(p-aminophenoxy)pentyl)- is a bioactive chemical.

MMT-Hexylaminolinker Phosphoramidite, a cleavable linker, facilitates the synthesis of oligonucleotide gapmers and other nucleic acid molecules [1] [2].

Phosphazide is a zidovudine prodrug.

ICMT-IN-43 (compound 22) acts as a potent inhibitor of the enzyme ICMT, exhibiting an inhibitory concentration (IC50) value of 0.04 μM [1].

DG046 is a potent ERAP1 inhibitor, a phosphinic pseudopeptide with unique π-stacking stabilization in the active site.

A-849519 is a reversible MetAP2 inhibitor with anti-angiogenic and anticancer properties, tested against prostate cancer and compared to TNP-470.

Nicotinamide, N-(5-(p-aminophenoxy)pentyl)- is a bioactive chemical.

1,2-Diheptadecanoyl-rac-glycerol is a diacylglycerol featuring heptadecanoic acid at both the sn-1 and sn-2 positions.

17-Phenyl trinor Prostaglandin F2α isopropyl amide is a derivative of 17-phenyl trinor prostaglandin F2α ethyl amide.

BMS-189664 HCl is a selective and orally active thrombin active site inhibitor.

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

Linear-benzoadenosine diphosphate is a nucleotide analog.

UU-T01 inhibits β-catenin/Tcf4 with Ki of 3.14 µM, binds β-catenin directly with KD of 0.531 µM.

VU661, a redox-active phenazine carboxamide, modulates circadian rhythms by inducing period lengthening.

TLR8 Agonist 5, exhibiting potent efficacy as a TLR8 agonist, demonstrates an EC50 of 20 nM in HEK-Blue hTLR8, effectively activating the immune response.

CP94, an iron chelator, enhances protoporphyrin IX photobleaching and reduces the viability of A431 squamous epithelial carcinoma cells at a 150 µM concentration with photodynamic therapy (PDT) using protoporphyrin IX precursors such as aminolevulinic acid (ALA), methyl aminolevulinate (MAL), or hexylaminolevulinate (HAL). Additionally, CP94 (2 mg/ml in drinking water) lowers hepatic non-heme and ferritin-bound iron levels while increasing hepatic protoporphyrin levels in mice. It also counteracts ferrocene-induced rises in rat brain iron levels at a dosage of 100 mg/kg.

Kynurenic acid, an active metabolite of tryptophan, is synthesized through a kynurenine intermediate by kynurenine aminotransferases (KATs). It acts as an antagonist of both NMDA and AMPA receptors, as well as α7 nicotinic acetylcholine receptors (nAChRs; EC50s = 235, 101, and 7 µM, respectively), and functions as an agonist for the aryl hydrocarbon receptor (AhR) and G protein-coupled receptor 35 (GPR35; EC50s = 1.4 and 39 µM, respectively). In a neonatal rat model of cerebral hypoxic-ischemia, induced by carotid artery ligation, administration of kynurenic acid at 300 mg/kg prevents weight loss in the lesioned hemisphere. Additionally, at concentrations of 1 and 5 mg/ml, it protects against neurodegeneration in the rhabdomere of the eye in an Htt93QtransgenicDrosophila model of Huntington's disease. Elevated levels of kynurenic acid in the cerebrospinal fluid have been observed in patients with schizophrenia.

C12 1-Deoxyceramide (m18:1/12:0) is a lipid molecule that can be used in life science related research. The CAS number of C12 1-Deoxyceramide (m18:1/12:0) is 1246298-54-3.

EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM. EMD638683 S-Form is the S-form of EMD638683.

Alpertine HCl is a small molecule compound with anti-neuropathic properties.

K-8986 is a novel h1-receptor antagonist

Clibucaine, a piperidine derivative, exhibits local anesthetic properties and is employed as a local anesthetic agent [1].

WAY 316606 hydrochloride is a chemical compound that serves as an inhibitor of sFRP-1 (secreted protein), which functions as an endogenous antagonist of the Wnt (secreted glycoprotein). Its affinity for sFRP-1 is measured through the FP (fluorescence polarization) binding assay, revealing an IC50 (half maximal inhibitory concentration) of 0.5 μM [1].

1-Arachidoyl-rac-glycerol, a monoacylglycerol, features arachidic acid at the sn-1 position and has been detected in pork muscle.

PDE7-IN-3 (Example 2) serves as an inhibitor of phosphodiesterase PDE7 and exhibits potential analgesic properties.

E7974, a hemiasterlin analog, targets the Vinca domain on tubulin, disrupts microtubules, and inhibits cell division and proliferation.

L 670548 is an agonist of muscarinic receptor.