probes

Probestin is an aminopeptidase M inhibitor, isolated from Streptomyces azureus MH663-2F6.

DAGLβ-IN-1 is a universal intermediate for designing DAGL tailored activity-based probes, and is an inhibitor of diacylglycerol lipase-β (DAGLβ).

TCIP 1 is a small molecule in the category of transcriptional epigenetic covalent inhibitor probes (TCIPs) that forms covalent bonds with molecules targeting BCL6 and BRD4. This compound facilitates cell death gene expression by directing endogenous cancer drivers or transcription factors to the promoters of these genes. Additionally, TCIP 1 exhibits a gain-of-function mechanism, displaying both cell and tissue specificity, and it establishes a ternary complex with BCL6 and BRD4. It counteracts BCL6's inhibitory effect on apoptosis gene expression, leading to the activation of apoptosis. Furthermore, TCIP 1 markedly suppresses MYC oncogene expression and curtails the proliferation of diffuse large B-cell lymphoma (DLBCL) [1].

(-)-Epicatechin gallate ((-)-Epicatechin 3-O-gallate) is one of the catechin isomers and a potent antioxidant that can modulate a wide range of membrane proteins. Its bilayer-modifying potency was tested using gramicidin A (gA) channels as probes. All the catechins alter gA channel function and modify bilayer properties, with a 500-fold range in potency. The gallate group causes current block, as evident by brief downward current transitions.

Benzofuroxan is used as a starting material for the synthesis of other compounds, such as drugs and other chemicals; it is also used in the synthesis of polymers; it is also used in the synthesis of fluorescent dyes and as fluorescent probes for the detection of certain molecules.

DOTA-NHS-ester is a linker for affibody molecules with applications in small animal PET, SPECT, and CT. It can be used to label radiotherapeutic agents or imaging probes for tumor detection.

DOTA-NHS-ester (TFA) serves as a linker for affibody molecules, and it is applicable in small animal imaging techniques such as positron emission tomography (PET), single-photon emission computed tomography (SPECT), and CT scans. It can also be used to label radiopharmaceuticals or imaging probes for tumor detection.

4-Chloropyridine acts as an inhibitor of Nicotinamide N-methyltransferase (NNMT). Serving as a substrate for NNMT, this compound enhances the electrophilicity at the C4 position through methylation of the pyridine nitrogen. This modification facilitates an aromatic nucleophilic substitution reaction with the non-catalytic cysteine (C159) in NNMT, ultimately leading to suicidal activity inhibition of the enzyme. 4-Chloropyridine is a promising candidate for the development of activity-based probes targeting NNMT functions.

GAPDH-IN-1 (Compound F8) is a GAPDH inhibitor, with an IC50 value of 39.31 μM for GAPDH enzyme activity. It forms a covalent adduct with the aspartic acid in the active site, displacing the enzyme's cofactor NAD+, and simultaneously enhances the reactivity of cysteine-reactive probes with the catalytic cysteine.

MU1920 is an ATP-competitive, selective inhibitor of haspin with an IC50 of 6 nM. In mouse plasma and microsomes, it demonstrates favorable pharmacokinetic properties and metabolic stability. Although it lacks significant anticancer activity, MU1920 is suitable for developing chemical probes.

DOTA-NI-FAPI-04 is an FAP inhibitor (IC50 = 7.44 nM). By integrating FAP targeting with hypoxia-sensitive groups (nitroimidazole), DOTA-NI-FAPI-04 significantly enhances tumor uptake and retention. Through DOTA chelation with metal isotopes (such as 68Ga and 177Lu), it forms radioactive probes ([68Ga]Ga DOTA-NI-FAPI-04 and [177Lu]Lu DOTA-NI-FAPI-04) useful for research in tumor diagnosis and therapeutics. This compound exhibits dual-targeting potential in cancer imaging, tumor microenvironment analysis, and radionuclide therapy, particularly in scenarios involving the interaction between tumor stroma and hypoxic regions.

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

DBHDA is a reagent to convert a Cys into a Dha moiety by reacting with a C-terminal Cys residue and thus allowing the use of recombinant Ubl G76C mutants to prepare probes.

m-PEG12-aldehyde is a PEG derivative containing an aldehyde group. Aldehyde is reactive to hydrazide and aminooxy groups which are commonly used in biomolecular probes for labeling and crosslinking carbonyls (oxidized carbohydrates). The hydrophilic PEG s

2,6-Dichloropurine-9-β-D-riboside is a building block.1,2It has been used in the synthesis of photoaffinity probes for nucleotide binding sites in proteins. 1.Wower, J., Hixson, S.S., Sylvers, L.A., et al.Synthesis of 2,6-diazido-9-(β-D-ribofuranosyl)purine 3',5'-bisphosphate: Incorporation into transfer RNA and photochemical labeling of Escherichia coli ribosomesBioconjug. Chem.5(2)158-161(1994) 2.Seiter, M.S., Bauer, M.P., Bogel, P.D., et al.Synthesis of novel spin-labeled photoaffinity derivatives of NAD+ and ATP and their characterization as coenzymes and substrates of several enzymesSynthesis2269-273(1996)

DCP-Rho1 is a fluorescent probe for the detection of sulfenic acid-containing proteins.1,2 It displays excitation/emission maxima of 560/581 nm, respectively, and has been used to visualize protein oxidation sites in situ. |1. Klomsiri, C., Rogers, L.C., Soito, L., et al. Endosomal H2O2 production leads to localized cysteine sulfenic acid formation on proteins during lysophosphatidic acid-mediated cell signaling. Free Rad. Biol. Med. 71, 49-60 (2014).|2. Holmila, R.J., Vance, S.A., Chen, X., et al. Mitochondria-targeted probes for imaging protein sulfenylation. Sci. Rep. 8(1), 6635 (2018).

ICAAc is a solvatochromic fluorescent pH probe.1 As the polarity of the solvent increases, the emission wavelength of ICAAc increases. It displays excitation/emission maxima of 466/553, 431/515, and 418/503 nm in water, dioxane, and hexane, respectively. The absorption maximum of ICAAc decreases with increasing pH. It displays absorption/emission maxima of 470/554 and 428/553 nm at pH 3 and 11, respectively, in aqueous Britton-Robinson buffer, and the fluorescence intensity increases as pH decreases. ICAAc can be used for live cell applications. |1. Nagy, M., Racz, D., Nagy, Z.L., et al. Amino-isocyanoacridines: Novel, tunable solvatochromic fluorophores as phystiological pH probes. Sci. Rep. 9, 8250 (2019).

1,3,4,6-Tetra-O-acetyl-2-azido-2-deoxy-α-D-mannopyranose is an analog of N-acetylmannosamine (ManNAc) and a building block. It has been used as a precursor in the synthesis of differently substituted trimers of the group A [N. meningitidis] capsular polysaccharide repeating unit for immunological experiments. It has also been used in the synthesis of fluorescent probes for lysosomal labeling.

monoMICAAc is a solvatochromic fluorescent pH probe.1 As the polarity of the solvent increases, the emission wavelength of monoMICAAc increases. It displays excitation/emission maxima of 425/491, 437/515, and 472/554 nm in hexane, dioxane, and water, respectively. The absorption maximum of monoMICAAc decreases with increasing pH. It displays absorbance/emission maxima of 475/553 and 446/553 nm at pH 3 and 11, respectively, in aqueous Britton-Robinson buffer, and the fluorescence intensity increases as pH decreases. monoMICAAc can be used for live cell fluorescent applications. |1. Nagy, M., Racz, D., Nagy, Z.L., et al. Amino-isocyanoacridines: Novel, tunable solvatochromic fluorophores as phystiological pH probes. Sci. Rep. 9, 8250 (2019).

SNOB 1 Reagent is a biotinylated probe for detecting S-nitrosylated proteins in a single step. S-Nitrosylated binding (SNOB) proceeds rapidly on surface proteins or cell lysates under normal physiological conditions. Proteins tagged with SNOB 1 Reagent can be analyzed using avidin-linked probes (e.g., by immunoblot) or by mass spectrometry.

Mild oxidation can convert the sulfhydryl group of cysteine residues on proteins to cysteine-sulfenic acid derivatives (Cys-SOH). Protein sulfenylation, then, is a post-translational modification that is relevant to redox signaling. DYn-2 is a chemoselective probe for detecting sulfenylated proteins in intact cells. DYn-2 consists of 1,3-cyclohexanedione coupled to an alkyne moiety by a 3-carbon spacer. The cyclohexanedione group selectively reacts with protein sulfenic acid modifications. The alkyne group of DYn-2 can then be detected using azide-bearing tags by standard click chemistry. This approach offers superior sensitivity relative to using azide-modified probes with alkynyl detection tags.

8Br-HA is an inhibitor of fragile histidine triad diadenosine triphosphatase (FHIT; IC50= 0.12 μM).1It inhibits the growth of HCC827 and H460 lung cancer cells (GI50s = 0.87 and 5.9 μM, respectively). 1.Kawaguchi, M., Sekimoto, E., Ohta, Y., et al.Synthesis of fluorescent probes targeting tumor-suppressor protein FHIT and Identification of apoptosis-inducing FHIT inhibitorsJ. Med. Chem.64(13)9567-9576(2021)

N-ε-propargyloxycarbonyl-L-lysine (H-L-Lys(Poc)-OH) is an unnatural amino acid (UAA) derived from lysine, used for bio-conjugation, particularly to attach fluorescent probes in organisms from E. coli to mammalian cells, including animals.

1-(Anilinocarbonyl)proline is a compound utilized for identifying dual-action probes within a cell model of Huntington's disease.