probe

ML346 is a novel activator of Hsp70.

Itaconate-alkyne (ITalk) is a bioorthogonal probe for quantitative, site-specific chemoproteomic profiling of itaconate in inflammatory macrophages, facilitating biochemical evaluation and proteomic analysis of its direct targets.

Antipyrine (Phenazone), an antipyretic and analgesic, has been given as ear drops and by mouth. Antipyrine is frequently used to test the effects of other diseases or drugs on drug-metabolizing enzymes in the liver.

Phenacetin (Acetophenetidin) is a phenylacetamide that was formerly used in ANALGESICS but nephropathy and METHEMOGLOBINEMIA led to its withdrawal from the market.

Maleimide (2,5-Pyrroledione) (2,5-Pyrroledone) is a new nanoparticle surface functional group which favors easy conjugation with cell penetration peptides. The conjugation is enabled via click chemistry to preserve its biofunctions.

BAY-474 is an inhibitor of tyrosine-protein kinase c-Met. It acts as an epigenetics probe

Biotin-PEG3-azide is a PEG-based PROTAC linker utilized in the synthesis of PROTACs.

LP99 is an epigenetic probe. LP99 disrupts the binding of BRD7 and BRD9 to chromatin in cells. LP99 is an effective and selective inhibitor of the BRD7 and BRD9 bromodomains (Kd: 99 nM against BRD9).

UNC1215, an effective and specific MBT (malignant brain tumor) antagonist, binds L3MBTL3 (IC50/Kd: 40/120 nM). The selectivity of UNC1215 for L3MBTL3 is 50-fold higher versus other members of the human MBT family.

GSK4112 (SR6452) is a Rev-erbα agonist with an EC50 of 0.4 μM and serves as a small molecule chemical probe for studying the cell biology of the nuclear heme receptor Rev-erbα.

I-BRD9 (GSK602) is the first selective cellular inhibitor for BRD9 with pIC50 of 7.3.

ML188 is a selective noncovalent SARS-CoV 3CLpro inhibitor(IC50 : 1.5 μM), with moderate MW and good enzyme and antiviral inhibitory activity.

Nitrobenzylthioinosine (NBMPR) is an inhibitor of ENT1 transporter that binds to ENT1 transporter with high affinity.

Cysteine thiol probe (Methyl (4-bromobenzoyl)-L-cysteinate) is a chemoselective thiol probe for detection of electrophilic metabolites

NFC nitro probe 1 (compound 18) is a chemical probe designed for the detection of Mtb, exhibiting high potency against both R-Mtb and NR-Mtb.

Progesterone-3-biotinyl Photoaffinity Probe is a compound containing the active substance progesterone. It is utilized in studies related to sperm activation mechanisms.

Melanin probe-1, an 18F-picolinamide-based PET probe, is utilized for PET imaging of malignant melanoma. It demonstrates remarkable tumor targeting efficacy, superior tumor imaging contrasts, favorable biodistribution profiles, and robust in vivo stability.

CXCR4 probe 1 (compound 5) is a potent and specific CXCR4-targeted PET tracer that acts on the CXCR4-specific antagonist TN14003 (IC50: 6.9 nM). It has potential as a CXCR4-specific imaging probe for the diagnosis and prognostic monitoring of inflammatory diseases, CXCR4-positive tumors, and metastatic tumors.

Melanoma is a lethal skin cancer. The early detection of melanoma using positron emission tomography (PET) probes is critical for improving the survival of melanoma patients. Melanin probe-2 is a non-radioactive bromo-picolinamide precursor that has been used for the synthesis of18F-picolinamides based PET probe (melanin probe-1). The tumor-targeting efficacy and imaging property of three melanin probes were evaluated in B16F10 tumor-bearing mice.18F-1 and18F-3 had much lower tumor uptake compared with18F-2 (Melanin probe-2), which were 12.74 ± 1.70, 16.61 ± 2.60, and 16.87 ± 1.23 %ID/g at 0.5, 1, and 2 h, respectively[1].

Cyclopropenone probe 1 can specifically and efficiently modify a triple-negative breast cancer driver, glutathione S-transferase pi-1 (GSTP1) , by covalently binding at the catalytic active site.

BLT2 Probe 1 (Compound 13), a fluorescent probe derived from the synthetic BLT2 agonist CAY10583, offers a robust tool for exploring BLT2 receptor ligand pharmacology across various assay systems [1]. As BLT2 is a valuable target for treatments in diabetic wound healing and gastrointestinal lesions, this probe facilitates relevant biomedical research.

Compound 39, also known as Y1R probe-1, is a high-affinity fluorescent probe targeting the Neuropeptide Y Y1 Receptor, with potential applications in cancer research [1].

CB2R Probe 1, a cannabinoid 2 receptor (CB2R) fluorescent probe, exhibits both safety and environmental friendliness, boasting a dissociation constant (K i) of 130 nM. Notably, it demonstrates low cytotoxicity within cancer cells [1].

Compound E1, also known as G-quadruplex DNA fluorescence probe 1, is a selective fluorescent probe targeting G-quadruplex DNA. It possesses the ability to penetrate membranes and enter living cells, demonstrating low cytotoxicity [1].