targeting

5(6)-Carboxyfluorescein (5-(and-6)-Carboxyfluorescein mixed isomers) contains a carboxylic acid that can be used to react with primary amines via carbodiimide activation of the carboxylic acid.

HOE-S 785026 trihydrochloride is a live cell labeling dye that binds to nucleic acids by targeting the minor groove in DNA double strands, with a preference for A T-rich regions (fluorescence is significantly enhanced by A T-rich double-stranded DNA). It crosses cell membranes and binds to living or immobilized cells, with its fluorescence intensity increasing as the solution pH rises.

7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for [14C]-lactate influx; new antitumor treatment targeting lactate transport in Y cells.

NucPE1, a nuclear-localized fluorescent hydrogen peroxide, is specifically localized to cellular nuclei without appended targeting moieties.

GD433 is a chemical probe specifically designed for use in vivo targeting NTMT1.

VZMC013 is a potent chemical probe targeting the MOR-CCR5 heterodimer, effectively inhibiting HIV-1 entry exacerbated by opioid compounds. It exhibits nanomolar binding affinity to both MOR and CCR5, inhibits CCL5-activated calcium mobilization, and significantly enhances anti-HIV-1BaL activity compared to previously reported bivalent ligands. In TZM-bl cells co-expressing CCR5 and MOR, VZMC013 demonstrates greater inhibition of viral infection than in cells expressing only CCR5. Additionally, VZMC013 blocks HIV-1 entry into peripheral blood mononuclear cells (PBMC) in a concentration-dependent manner and more effectively inhibits opioid-accelerated HIV-1 entry in phytohemagglutinin-activated PBMC than in opioid-free environments.

Cy3-PEG-FA (MW 2000) is a fluorescent folate-PEG derivative with excitation emission wavelengths of approximately 550 nm 570 nm. The compound can be easily tracked due to its intense red fluorescence signal. It is applicable in cell imaging, folate receptor targeting, and detection.

Complex 3 is a fluorescent dithiocarbamate-copper complex exhibiting anticancer properties, specifically targeting mitochondria. It has excitation emission maxima at 455-495 535 nm. Complex 3 inhibits the growth of pancreatic cancer cells BxPC-3, AsPC-1, PANC-1, and WI38, with IC50 values of 0.74, 0.41, 0.62, and 2.06 µM, respectively. In AsPC-1 cells, it induces lipid peroxidation, mitochondrial fragmentation and constriction, apoptosis, and cytokine-cytokine receptor interaction dysfunction. Furthermore, Complex 3 reduces tumor volume and induces apoptosis within tumors in AsPC-1 mouse xenograft models.

Cyanine3 carboxylic acid is a non-toxic red fluorescent dye that serves as a non-reactive fluorophore for experimental controls and calibration. It can also be conjugated with targeting active molecules to create fluorescent probes for rapid detection of molecular reactions. [Ex Em(nm)=550 570nm]

DOTA-XYIMSR-01 is a molecular probe targeting CAIX, capable of being labeled with 177Lu for the treatment and localization of malignant gliomas. The uptake of [177Lu]Lu-XYIMSR-01 in U87MG tumors is 6.19% injected dose per gram (% ID/g), with a tumor-to-muscle uptake ratio of 20.14. In an orthotopic glioma model, co-administration with temozolomide significantly enhances survival rates and inhibits tumor growth in mice. DOTA-XYIMSR-01 shows potential for research in the field of cancer treatment.

BI 2852 FL is a cell-permeable bioluminescence resonance energy transfer (BRET) fluorescent probe targeting the pan-RAS type. It is synthesized by conjugating a fluorophore with a derivative of the reversible SI/II-P KRAS inhibitor, BI 2852. BI 2852 FL is employed in a competitive BRET format to quantify the binding of SII-P to multimeric RAS complexes within living cells.

HKSOX-1m (5 6-mixture) is a mitochondria-targeting O2 fluorescent probe with excitation emission wavelengths of 509 534 nm (green), offering exceptional selectivity and sensitivity for O2 across a wide pH range and in the presence of strong oxidants and prevalent reductants within cells.

HKOCl-4m is a rhodol-based fluorescent probe designed for the specific and deliberate targeting of mitochondria, enabling the monitoring of mitochondrial hypochlorous acid (HOCl).

MHI-148 is a tumor-targeting near-infrared heptamethylenecarbocyanine dye for the detection, diagnosis, and study of cancer.MHI-148 is taken up and accumulates in the lysosomes and mitochondria of tumor cells but is not taken up in the lysosomes and mitochondria of normal cells.MHI-148 is a tumor-targeting near-infrared heptamethylenecarbocyanine dye for the detection and diagnosis of cancer.

Biotin-NH-PSMA-617 is a biotinylated derivative of the small molecule PSMA-617, designed to target prostate-specific membrane antigen (PSMA), which is prominently expressed on prostate tumor cells. The biotinylation of PSMA-617 enhances its ability to bind PSMA, making it a valuable tool in the targeting of prostate cancer cells for diagnostic and therapeutic applications.

IR-251 is a mitochondrion-targeting near-infrared (NIR) fluorescent probe that selectively accumulates in tumor cell mitochondria through organic anion transporting polypeptides (OATPs), leading to mitochondrial dysfunction. By impeding peroxisome proliferator-activated receptor gamma (PPARγ), IR-251 promotes reactive oxygen species (ROS) overproduction, consequently inhibiting the β-catenin signaling pathway as well as associated cell cycle and metastasis proteins. This mechanism contributes to the compound's ability to suppress tumor growth and metastasis [1].

BTCy, a near-infrared (NIR) fluorescence probe, exhibits polarity-sensitive and cell plasma membrane-targeting characteristics. It is applicable for in vivo tumor tissue imaging (λ ex = 561 nm, λ em = 600-700 nm) [1].

BODIPY 630/650X is a fluorescently labeled conjugate of the adenosine receptor ligand N-ethylcarboxamido-adenosine (NECA), which exhibits distinct excitation and emission maxima at approximately 630 nanometers and 650 nanometers, respectively, making it a valuable tool for fluorescence-based assays and imaging studies targeting adenosine receptor activity and distribution.

Biotin-PEG-Alk (MW 10000) is a biotinylated polyethylene glycol (PEG) derivative with an alkyne group designed for click chemistry applications. Combining biotin, an enzyme co-factor used in protein labeling, with PEG, a hydrophilic, water-soluble, and low-toxicity polymer, the alkyne moiety enables copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azido-containing molecules, enhancing the efficiency of targeting biotin-binding entities.

Biotin-PEG-Alk (MW 1000) is a biotinylated polyethylene glycol (PEG) derivative featuring alkyne functionality for click chemistry applications. Biotin acts as an enzyme co-factor for protein labeling, while PEG imparts hydrophilic, water-soluble, low-toxicity properties. The alkyne group (Alk) enables copper-catalyzed azide-alkyne cycloaddition (CuAAC) reactions with azido-modified molecules, enhancing targeting and binding with biotin receptors.

Sulfane Sulfur Probe 4 (SSP4) serves as a fluorescent probe targeting sulfane sulfur species, encompassing hydrogen sulfide-derived polysulfides, hydropersulfides, and persulfides generated endogenously. Upon interacting with these species, SSP4 undergoes a nucleophilic attack, leading to fluorescein production, characterized by 494 515 nm excitation emission peaks, along with the generation of two 1,2-benzodithiol-3-one molecules. This compound has been instrumental in localizing H2S3 within primary mouse neurons and identifying polysulfides in L. japonicus seedling roots.

TNP-ATP, a derivative of ATP, acts as an antagonist to the purinergic P2Y1, P2X3, and P2X2 3 receptors, demonstrating selectivity by showing lower inhibitory concentrations (IC50 = 6, 0.9, 7 nM, respectively) compared to the P2X2, P2X4, and P2X7 receptors (IC50 = 2, 15.2, >30 µM, respectively) in HEK293 cells expressing these human receptors. It effectively diminishes acetic acid-induced calcium influx in 1321N1 cells targeting P2X3 and P2X2 3 receptors (IC50 = 100 and 62 nM, respectively) and alleviates pain in a mouse model of visceral pain (ED50 = 6.35 µmol kg). Moreover, TNP-ATP exhibits a notable fluorescence characteristic, with an emission peak at 547 nm after excitation at 403 nm, which enhances four-fold and shifts to 538 nm when bound to the insulin-degrading enzyme (IDE).

CQ-Lyso is a chromenoquinoline compound specifically targeting lysosomes. It acts as a fluorescent probe designed to monitor lysosomal pH in live cells through single-wavelength excitation, enabling visualization of dynamic pH alterations in these organelles [1].

CTB Probe-1 (probe 1) serves as a small-molecule, lysosome-targeting fluorogenic probe designed for fluorescence imaging within living cells [1].