tool

Fructooligosaccharides is a levorotatory monosaccharide and an isomer of glucose.

5-bromo-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione (5-bromo-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione) is a synthetic compound. It has been used as a catalyst and as a tool in enzyme kinetic studies; it has also been used in studies of enzyme inhibition, as well as in drug receptor interaction studies.

Carbachol (Carbamoylcholine chloride), an analog of acetylcholine, serves as a valuable tool in the investigation of various physiological responses mediated by nicotinic (nAChR) and muscarinic (mAChR) acetylcholine receptors. These responses include smooth muscle contraction, gut motility, and neuronal signaling. Known for its agonistic properties, Carbachol activates both nAChR and mAChR, with reported Ki values ranging from 10 to 10,000 nM for different receptor types and experimental preparations.

D-Mannitol (Mannitol) is a diuretic and renal diagnostic aid related to sorbitol. It has little significant energy value as it is largely eliminated from the body before any metabolism can take place. It can be used to treat oliguria associated with kidney failure or other manifestations of inadequate renal function and has been used for determination of glomerular filtration rate. D-Mannitol is also commonly used as a research tool in cell biological studies, usually to control osmolarity.

Reserpine (Serpalan) is an alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.

Meldrum's acid (Isopropylidene malonate) is an antimicrobial agent used in deodorant. Meldrum's acid-based multicomponent reaction is a potential tool to prepare novel polymers.

3F8 is a selective GSK-3β inhibitor that can be used as a new tool and potential therapeutic candidate compound for GSK3-related diseases, and can be used in the study of neurological disorders and cancer.

2,2'-Anhydrouridine (2,2'-Cyclouridine) is a research tool for antiviral and anticancer studies.

LKM38, a novel diazolidinyl cholesterol probe, is a promising cholesterol mimetic.LKM38 both maintains cholesterol-resistant cell growth and appropriately regulates key cholesterol homeostatic pathways.LKM38 can be a powerful tool for studying cholesterol protein interactions and trafficking.

5'-Fluoro-5'-deoxyadenosine (5'-Fluoro-5'-deoxy-adenosine) is utilized commonly as a tool for studying the Actinomycete bacterium Streptomyces cattleya.

CC214-1 is an mTOR inhibitor with potential anticancer activity, inhibits protein translation, and induces autophagy. CC214-1 is an in vitro tool compound for exploring the biology of mTOR kinases and can be used to study myeloma.

Phos-tag Acrylamide AAL-107 is an acrylamide-pendant that can be used as a tool to visualize phosphorylated proteins.

BRK inhibitor P21d hydrochloride is a highly potent inhibitor of breast tumor kinase (BRK PTK6), displaying an IC50 of 30 nM, and effectively suppresses p-SAM68 with an IC50 of 52 nM. This compound serves as a valuable tool for evaluating BRK inhibitors' efficacy in xenograft breast tumor models, enabling in vivo activity assessment.

GP-82996 (CINK4) is a pharmacological inhibitor specifically targeting CDK4 6, exhibiting IC50 values of 1.5 μM for CDK4 cyclin D1, 5.6 μM for CDK6 cyclin D1, and 25 μM for Cdk5 p35. It effectively induces apoptosis in U2OS cancer cells, positioning it as a potential investigational tool in cancer research [1] [2].

JAK3-IN-11 (Compound 12) exhibits potent, noncytotoxic, irreversible, orally active JAK3 inhibitory activity (IC50 = 1.7 nM) with an excellent selectivity profile (>588-fold compared to other JAK isoforms), covalently binds to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T-cell proliferation which is a promising tool for studying autoimmune diseases [1].

Ionomycin is an calcium ionophore and an antibiotic that binds calcium ions (Ca2+). It is produced by the bacterium Streptomyces conglobatus.It is used in research to raise the intracellular calcium level (Ca2+) and as a research tool to understand Ca2+ transport across biological membranes. Ionomycin promotes apoptosis and induces the activation of protein kinase C (PKC).

Chlorin E6 (CE6) is a second-generation photosensitizer with antitumor activity when used in combination with irradiation. In a mouse model of implanted fibrosarcoma, Chlorin E6 (2.5-10 mg/kg, i.v., 50-200 J/cm2 irradiation) resulted in complete tumor disappearance after varying degrees of irradiation. Agents including Chlorin E6 were tested in a Phase I clinical study in patients with early superficial squamous cell carcinoma of bronchial origin with favorable results (40 mg/m2, IV, 100 J/cm2 laser irradiation). In a Phase II clinical trial in patients with early stage lung cancer, the same mode of administration resulted in a complete response in 82.9% of patients. Chlorin E6 has been investigated as a nanotechnology drug delivery tool.

HOIPIN-8 is a potent inhibitor of the linear ubiquitin chain assembly complex (LUBAC) with an IC50 of 11 nM. As a derivative of HOIPIN-1, it exhibits 255-fold greater inhibition of both petit-LUBAC and TNF-α-mediated NF-κB activation compared to HOIPIN-1. HOIPIN-8 is a promising tool to explore cellular functions of LUBAC.

Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) serves as a potent inhibitor related to Pentamidine, targeting the calcium-binding protein S100B with a dissociation constant (Kd) of 6.9 µM. It demonstrates specificity by preferentially killing melanoma cells overexpressing S100B compared to cells lacking this protein. Additionally, Heptamidine is employed as a valuable research tool in the study of Myotonic dystrophy (DM).

ELOVL1-IN-3 is a potent and orally active inhibitor of elongation of very long chain fatty acid 1 (ELOVL1) enzyme. ELOVL1-IN-3 serves as a useful tool for researching adrenoleukodystrophy (ALD).

CK-869, an Actin-Related Protein 2 3 (ARP2 3) complex inhibitor with an IC50 of 7 μM, is a valuable tool for investigating the Arp2 3 complex.

VUF10460, a non-imidazole histamine H4 receptor agonist, [58C8-51-20-3] is structurally classified under the chlorobenzylpiperazine ethers with the IUPAC designation (2-[(2-chlorophenyl)methyl]-1-piperazinyl)(1H-indol-3-yl)methanone. It is typically utilized in pharmacological research and exhibits specificity for the H4 subtype, making it a valuable tool in immunological studies.

GAT100 is a potent and covalent negative allosteric modulator (NAM). GAT-100 behaved as a robust positive allosteric modulator of binding of orthosteric agonist CP55,940. This novel covalent probe can serve as a useful tool for characterizing CB1R allosteric ligand-binding motifs.

Thalidomide 5'-amine-alkylC6-amine serves as a specialized cereblon ligand for PROTAC research and development, combining an E3 ligase ligand and an alkylC6 linker with a terminal amine for target protein ligand conjugation. It is among a series of functionalized tool molecules designed for PROTAC R&D.

Hexamethonium Free Base is a nicotinic cholinergic antagonist often referred to as the prototypical ganglionic blocker. It is poorly absorbed from the gastrointestinal tract and does not cross the blood-brain barrier. It has been used for a variety of therapeutic purposes including hypertension but, like the other ganglionic blockers, it has been replaced by more specific drugs for most purposes, although it is widely used a research tool.

CDy9 is a highly selective fluorescent probe for the detection and isolation of mESC using fluorescence microscopy and flow cytometry. CDy9 allows the detection and isolation of intact stem cells with marginal impact on their function and capabilities. CD

Functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC research and development; incorporates an E3 ligase ligand plus a PEG linker ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules for PROTAC R&D. This product has been recently renamed. The previous name for this product was VH 032 - linker 2 PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.

EPZ020411 is a potent and selective PRMT6 inhibitor tool compound. EPZ020411 shows good bioavailability following subcutaneous dosing in rats making it a suitable tool for in vivo studies. EPZ020411 suppresses RCC1 arginine methylation and improves the cytotoxic activity of radiotherapy against GSC brain tumor xenografts.

Antibacterial agent 37 is an effective antimicrobial compound. It holds potential as a valuable tool for researching bacterial infections.

JAK3-IN-9 is a potent and orally active inhibitor of the Janus kinase 3 (JAK3) enzyme, displaying an impressive IC50 value of 1.7 nM. It exhibits high selectivity towards the JAK3 signaling pathway, making it a valuable tool for studying autoimmune diseases. Additionally, JAK3-IN-9 possesses desirable characteristics such as low toxicity and excellent oral bioavailability. It also demonstrates promising anti-arthritis activity, thus enhancing its potential as a therapeutic agent [1].

Functionalized von-Hippel-Lindau (VHL) protein ligand for PROTAC research and development; incorporates an E3 ligase ligand plus a PEG1 linker with terminal carboxylic acid ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules for PROTAC R&D. PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.

Nurr1 Inverse Agonist-1 is an inverse agonist for the neuroprotective transcription factor Nurr1, serving as a research tool.

Biotin-labeled ODN TTAGGG (sodium) is an inhibitory oligonucleotide (ODN) that antagonizes TLR9, AIM2, and cGAS, serving as a tool for assessing cellular uptake and localization of CpG ODN using biotin detection systems and light microscopy.

BLT2 antagonist-1 (compound 15b) is a selective inhibitor of the BLT2 receptor, impeding the chemotaxis of CHO-BLT2 cells at an IC50 of 224 nM without affecting CHO-BLT1 cell chemotaxis. It blocks the interaction between LTB4 and the BLT2 receptor with a K_i of 132 nM and may serve as a research tool for inflammatory airway diseases, including asthma and chronic obstructive pulmonary disease [1].

ZMF-23, a PAK1/HDAC6 dual inhibitor, suppresses PAK1 and HDAC6-mediated aerobic glycolysis and cellular migration while inducing TNF-α-regulated necroptosis and augmenting apoptosis. The compound effectively hampers the Warburg effect and cell motility, positioning it as a potential research tool for triple-negative breast cancer (TNBC) [1].

HBV-IN-38 (Example 193), an HBV DNA inhibitor with an EC50 value of ≤100 nM, serves as a research tool for investigating viral infections [1].

ML365 is a novel selective small molecule inhibitor of TASK1(KCNK3).

Pomalidomide 4'-PEG5-amine, a cereblon ligand designed for PROTAC research and development, features an integrated E3 ligase ligand and a PEG5 linker ending in an amine for easy conjugation to target protein ligands. It is among a series of functionalized tool molecules specifically crafted for PROTAC R&D.

RR-11a is a synthetic enzyme legumain inhibitor. This compound specifically targets and inhibits the activity of legumain, an enzyme implicated in various biological processes. RR-11a's synthetic nature allows for precise modulation of legumain activity, making it a valuable tool in biochemical research and potential therapeutic applications.

Antitumor agent-66 (Compound 4) is a derivative of (-)-cleistenolide, exhibiting potential as a research tool for cancer diseases [1].

AMPC, a powerful and efficient inhibitor of TFF3, demonstrates inhibitory effects on cell proliferation, survival, oncogenicity, and CSC-like behavior in TFF3-positive CMS4 CRC cells. It acts as a promising standalone anti-cancer agent and also enhances the effects of 5-FU when used in combination, making it a valuable tool for cancer research.

Functionalized von-Hippel-Lindau (VHL) protein ligand for PROTAC research and development; incorporates an E3 ligase ligand plus a PEG linker ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules for PROTAC R&D. This product has been recently renamed. The previous name for this product was VH 032 - linker 9 PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.

(Rac)-Zevaquenabant ((Rac)-MRI-1867, compound 6b) is a potent and selective antagonist of cannabinoid receptor type 1 (CB1R) and inducible nitric oxide synthase (iNOS), with a binding affinity (Ki) of 5.7 nM for CB1R. It holds promise as an investigative tool in liver fibrosis research due to these characteristics.

LYP-IN-1 is a powerful LYP inhibitor that demonstrates high potency, selectivity, and specificity, with a Ki of 110 nM and an IC 50 of 0.259 μM. Beyond its primary target, LYP-IN-1 also exhibits selectivity towards a wide range of PTPs, including SHP1 (IC 50 = 5 μM) and SHP2 (IC 50 = 2.5 μM). Additionally, LYP-IN-1 demonstrates remarkable efficacy in T- and mast cells, making it a valuable tool for investigating autoimmune disorders.

TRK II-IN-1 is a potent type II inhibitor of tropomyosin receptor kinases (TRK), with IC50 values of 3.3, 6.4, 4.3, and 9.4 nM against TRKA, TRKB, TRKC, and the mutant TRKA G667C, respectively. It also exhibits IC50 values of 1.3 nM against FLT3, 9.9 nM against RET, and 71.1 nM against VEGFR2. TRK II-IN-1 primarily serves as a research tool for studying TRK-driven cancers [1].

NSC 295642, a phosphatase inhibitor, significantly enhances phospho-Erk cytonuclear differences in intact cells, making it a valuable tool for cancer research.

MRS4719, a potent P2X4 receptor antagonist, exhibits a half-maximal inhibitory concentration (IC50) of 0.503 μM for the human P2X4 receptor. Demonstrating both neuroprotective and neuro-rehabilitative effects, it can decrease infarct volume and brain atrophy in an ischemic stroke model. Additionally, MRS4719 mitigates ATP-induced calcium influx in primary human monocyte-derived macrophages, making it a valuable tool for researching ischemic stroke.

HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt exhibits inhibitory activity towards pre-miR-21 RNA, indicating its potential as a research tool for studying neoplastic diseases, including various cancers that express miR-21 [1].

TRIM24 BRPF1-IN-2 (compound 20l) is an effective dual inhibitor of TRIM24 BRPF1 with IC50 values of 0.98 μM for TRIM24 and 1.16 μM for BRPF1, exhibiting strong binding affinity to the bromodomains of TRIM24 BRPF1, making it a valuable tool for prostate cancer research [1].

DNA Crosslinker 3 (dihydrochloride) (Compound 1) is a potent minor groove binder, exhibiting a DNA binding affinity (ΔTm) of 1.4°C, and serves as a valuable tool in anticancer research [1].