Otros inhibidores

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

1-Palmitoyl-2-oleoyl-3-linolenoyl-rac-glycerol is a triacylglycerol comprising palmitic acid, oleic acid, and α-linolenic acid esterified at the sn-1, sn-2, and sn-3 positions, respectively.

PU-48 is a potent inhibitor of urea transporters A (UT-A) with an IC50 value of 0.32 μM, exhibiting a significant diuretic effect in mouse models without

ICMT-IN-9 (compound 47) is a potent ICMT inhibitor with an IC50 value of 0.16 μM [1].

Nicotinoyl azide (N-Az) is a probe of light-activated chemical. It has been used to measure the solvent accessibility of purine nucleobases.

AZD1386: oral TRPV1 receptor antagonist. Info from NIH/NCATS and DrugBank.

CAY10455, an analog of arachidonoyl ethanolamide (anandamide; AEA), is non-fluorescent extracellularly but exhibits bright fluorescence at 530 nm inside cells due to esterase-mediated cleavage. Its uptake by C6 glioma cells is competitively inhibited by AEA and its analogs, suggesting that CAY10455 and AEA utilize the same transporter. Conversely, CAY10455 also inhibits the uptake of tritiated AEA, further indicating competition for the AEA transporter.

A1AT Modulator 1 potently inhibits Z α1-antitrypsin (A1AT) polymerization, exhibiting a pIC50 of 8.3 [1].

<p>AM-461 is a DP2 receptor antagonist.</p>

9(E),11(E)-Conjugated Linoleic Acid Methyl Ester, identified in thermally stressed cooking oils, can serve as an indicator for the adulteration of olive oils with lower quality oils. [Matreya, LLC. Catalog No. 1257]

R 93274 is a radioiodinated 5-HT2A receptor antagonist.

RAF mutant-IN-1 is an inhibitor of RAF kinase(IC50 values of 21 nM, 30 nM and 392 nM for C-RAF 340D/Y341D, B-RAFV600E and B-RAFWT, respectively).

NC1 is a potent allosteric inhibitor of lymphoid-specific PTPN22, a protein tyrosine phosphatase.

Fomocaine (P 652), an orally active local anesthetic, also exhibits antiarrhythmic activity [1] [2].

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。

MK-287 is a PAF antagonist blocking [3H]C18-PAF binding to platelets, PMNs, and lungs; may treat asthma.

Fecosterol, a metabolite derived from Saccharomyces cerevisiae, is utilized in phytosterolemia research.

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

Dinonadecanoin is a diacylglycerol characterized by the presence of the saturated fatty acid, nonadecanoic acid (nonadecanoic acid), at two positions.

SB-682330A is a Raf kinase inhibitor.

Phosphazide is a zidovudine prodrug.

<p>SOS1 agonist-1 (compound 79) serves as an agonist for the Son of sevenless homologue 1 (SOS1), a crucial guanine nucleotide exchange factor involved in catalyzing the GDP to GTP exchange on RAS proteins, thus regulating RAS activation. By increasing nucleotide exchange on RAS, SOS1 agonists enhance cellular RAS-GTP levels and induce biphasic signaling alterations in ERK1/2 phosphorylation, playing a pivotal role in anti-cancer activity [1].</p>

Compound 4, known as GALK1-IN-1, is a potent inhibitor of galactokinase, exhibiting an IC50 value of 4.2129 μM [1].

YUN90389 (CAS#1673590-38-9) is the first pparα/δ dual antagonist, as reported in 2019.

RP-52770 is a bioactive chemical.

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

(–)-IHCH7041 is a optical rotation negative isomer of IHCH7041.

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

α,β-Methylene ATP，一种ATP的膦酸酯类似物，充当P2X3和P2X7受体的配体。该化合物对P2X1和P2X3表现出高选择性激动剂活性，而在P2X2, 4, 7受体上无活性。

AP-C4 is a selective inhibitor targeting guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII), exhibiting a pIC50 value of 5.2.

<p>STAT3-IN-14 is a STAT3 inhibitor and has STAT3 phosphorylation inhibitory activity. STAT3-IN-14 can directly bind to the hinge region of STAT3 .</p>

Orexin Receptor Modulator-1 is a compound utilized in the study of various conditions including substance addiction, panic disorder, anxiety, post-traumatic

<p>SB 203580 sulfone, an analog of the p38 MAP kinase inhibitor SB 203580, inhibits IL-1 production in monocytes and binds competitively with CSAID binding proteins (CSBP), inhibiting stress response signaling. It exhibits an IC50 of 0.2 μM for IL-1 inhibition and 0.03 μM for CSBP-mediated signaling inhibition [1].</p>

NaPi2b-IN-2 (compound 5) serves as a potent inhibitor of the sodium-dependent transport protein 2b (SLC34A2, NaPi2b), exhibiting an IC50 of 38 nM against human

<p>Boc-Val-Dil-Dap-OH is a cleavable linker utilized in the synthesis of antibody-drug conjugates (ADCs), facilitating the connection between the antibody and the therapeutic drug [1].</p>

<p>17-Hydroxyheptadecanoic acid, a hydroxylated fatty acid identified in aeolian particles from the Frioul Islands and the outer bark of E. globulus, serves in the synthesis of diverse macrocyclic lactones. [Matreya, LLC. Catalog No. 1760]</p>

<p>HA-14-1, a small molecule, binds the surface pocket of Bcl-2 proteins (IC50= ~ 9 µM), including Bcl-xl and Bcl-W, and disrupts their interaction with the Bak peptide. This action induces apoptosis by activating Apaf-1 and caspase-9 and -3. Additionally, HA-14-1 effectively induces apoptosis in human acute myeloid leukemia (HL-60) cells, with a 50 µM concentration resulting in a 90% loss of cell viability.</p>

FK-352 is a pyrazolopyridine derivative and adenosine-1 receptor antagonist.

BMY-42393 is an oral prostacyclin agonist and platelet aggregation inhibitor with IC50 of 0.3-2μM and stimulates adenylate cyclase (EC50 = 25nM).

<p>Jak2-IN-7j is a selective Jak2 inhibitor which demonstrates a time-dependent knock-down of pSTAT5, which is a downstream target of Jak2.</p>

<p>UCPH-102: Selective EAAT1 inhibitor, IC50 0.43 μM, treats Alzheimer's, ALS, chronic pain, OCD; crosses blood-brain barrier, targets T-ALL cells.</p>

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

Esterbut-6 is a potent tumor cell proliferation inhibitor in vivo by stabilizes butyric acid.

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

Levuglandin E2 is a secoprostanoid from prostaglandin endoperoxide.

58-G3 is an agonist of methuselah (Mth)-specific that acts by inducing dose-dependent calcium elevation and membrane translocation of β-arrestin2.

<p>WAY-658675 is an active molecule.</p>

BMS-986122: IRAK4 inhibitor, reduces symptoms in mouse lupus models, may benefit human lupus therapy.

LC kinetic stabilizer-1: potent, selective for amyloid light chains, EC50: 140 nM (WIL-FL*), 74.1 nM (WIL-FL*T46L/F49Y).

Osivelotor is an allosteric modulator of hemoglobin S (HbS) [1].

<p>DNA-PK Inhibitor IV is an active molecule that can be used in life science related research. The CAS number of DNA-PK Inhibitor IV is 70362-07-1.</p>

Vinclozolin M2, an active metabolite of vinclozolin, is generated through successive esterase activity and decarboxylation in C. elegans, as well as decarboxylation in human liver microsomes. It functions as an antagonist to the mineralocorticoid (IC50= 1,400 nM) and androgen receptors (IC50= 0.17 nM), demonstrated in reporter assays with MCF-7 cells. This compound is exclusively sold for research and analytical purposes, tailored for controlled laboratory use, and is not available in bulk sizes.

CycLuc3 is a type of mutant firefly luciferase variant with enhanced light emission.

<p>TRAP-6-IN-1 inhibits collagen/TRAP-6, IC50: 17.12/11.88 μM, blocks platelet aggregation.</p>

<p>Compound CMC23, an FPR2 agonist, mitigates lactate dehydrogenase release in LPS-stimulated cultures and reduces pro-inflammatory IL-1β and IL-6 levels.</p>

Antiproliferative Agent-38 (COM 18), a tetracyclic compound, features a reactive ring nitrogen (likely the quinoline moiety) that resists N-alkylation.

SSAO/VAP-1 inhibitor 1 regulates glucose transport and may reduce inflammation, potential for diabetes and inflammatory disease research.

<p>Endosulfan II, an organochlorine insecticide and a stereoisomer of Endosulfan I, effectively targets various insects such as bollworms and tobacco budworms, with lethal doses (LD50s) of 4.14 and 4.95 mg/g, respectively. It interacts with GABA receptors in rat brain membranes, demonstrating an inhibition concentration (IC50) of 60 nM. Notably, Endosulfan II exhibits lower toxicity in rats compared to Endosulfan I, with LD50 values of 240 and 18 mg/kg, respectively.</p>

ATX inhibitor 15, an indole-based carbamate, has a 2.17 nM IC50 against ATX, suppresses pro-fibrotic genes, and protects against mouse lung fibrosis.

<p>THB is a glucocorticoid with anti-inflammatory effects, acting on GC receptors; its isomers vary between male and female rat brains.</p>

ATIC-IN-1 (compound 14) serves as an inhibitor specifically aimed at the dimerization of Aminoimidazole carboxamide ribonucleotide transformylase/inosine

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

3-O-Acetylbufotalin is a derivate of bufadienolide with anti-cancer activity.

MK-1421 is a potent and selective sstr3 antagonist.

GSK1360707 is a selective triple reuptake inhibitor (TRI).

SB1-F-78 is an USP30 inhibitor.

<p>WAY-311474 is an investigational compound targeting amyloid-related diseases and synucleinopathies.</p>

CLR-131, a protein kinase B (PKB) inhibitor, is used potentially for the treatment of non small cell lung cancer, solid tumors.

Valsartan acid, a byproduct of the angiotensin II type 1 (AT1) receptor antagonist Valsartan, emerges through the activated sludge treatment process and has been identified as a contaminant in drinking water.

Tomicorat is an anti-inflammatory agent.

1,3-Dioctanoyl glycerol, a diacylglycerol, features octanoic acid at the sn-1 and sn-3 positions.

<p>HCT-116-IN-1, a γ-lactam-fused pyridone derivative, exhibits anticancer properties, demonstrating significant cytotoxicity towards HCT116 cells, with an IC50</p>

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

SMS1-IN-1 is a potent inhibitor of sphingomyelin synthase 1 (SMS1, IC50 = 2.1 μM), and can be used in the atherosclerosis studies.

"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)."

MK-386 is a potent and selective inhibitor of human type-1 5alpha-reductase.

GMC-1111 dihydrochloride is a dopamine partial agonist and stabilizer.

Sunepitron Free Base, a 5-HT1A agonist/α₂-antagonist, halted in Phase III for depression/anxiety.

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].

OY-201 is a promising anti-ischemic stroke agent capable of crossing the blood-brain barrier (BBB).

<p>OM-1700 inhibits tankyrase 1 (IC50=127 nM) and 2 (IC50=14 nM); hinders colon cancer cell growth, COLO 320DM (GI50=650 nM).</p>

<p>eIF4A i28, an inhibitor of the eukaryotic initiation factor-4A (eIF4A) with an IC50 of 8.60 μM in an eIF4A ATPase assay, effectively reduces the viability of</p>

D-threo-PDMP inhibits glucoceramide synthase, cutting cell surface glycosphingolipids and hindering neurite growth.

<p>SR2595 is an inverse agonist of nuclear receptor PPARγ with an IC 50 of 30 nM [1].</p>

STING agonist D61 is a compound that activates the stimulator of interferon genes (STING), leading to the induction of IFN3-inducible secreted alkaline

<p>8-Keto-berberine is a non-naturally occurring 11, 12-oxygenated protoberberine. It is a derivative from naturally occurring 9, 10-oxygenated protoberberine.</p>

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

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]

Crobenetine hydrochloride, a sodium channel antagonist, is used potentially for the treatment of stroke.

ES 8891 is an inhibitor of renin.

PF-06748962 is a potent and selective lactam-based prostaglandin EP3 receptor antagonist.

<p>M04 acts as a stimulator of interferon genes (STING) agonist, effectively inducing IFN reporter gene expression in HEK293T cells equipped with wild-type human STING. Its activity is specific, not affecting HEK293T cells with the R71H-G230A-R293Q (HAQ) human STING variant or mouse RAW 264.7 cells, showcasing allelic- and species-dependent effects at a concentration of 75 µM. This compound also stimulates the production of TNF-α, IL-10, IL-1β, and IL-12p70 in human peripheral blood mononuclear cells (PBMCs). At 50 µM, M04 enhances human monocyte-derived dendritic cells' expression of HLA-DR (MHC class II receptor) and co-stimulatory molecules CD40, CD80, and CD86, improving T cell cross-priming in an ex vivo assay.</p>

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.

1-Deaza-fad also known as Deazafad. 1-deazaFAD has comparable activity in the mutase reconstituted.

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.

LM985 is one of a series of compounds based on the flavone ring structure. It has anti-tumor activities.

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.

BODIPY-Palmitate, a fluorescent derivative of palmitic acid, exhibits excitation and emission maxima at 488 nm and 508 nm, respectively. It is employed in the monitoring of fatty acid uptake and metabolism within cultured cells.

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

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>ARQ 736 effectively targets and inhibits BRAF, crucial in MAPK pathway, beneficial for treating melanomas and certain colon cancers.</p>

RPR203494 is a pyrimidine analogue of the p38 inhibitor RPR200765A with an improved in vitro potency.

KUNG38 is a purine-based inhibitor of Grp94.

NIP-101 is a potent calcium antagonist.