Cancer Targeted Therapy

C3TD879 is a Type I kinase inhibitor that potently inhibits CITK catalytic activity (IC₅₀ = 12 nM). C3TD879 binds directly to full-length human CITK in cells (NanoBRET K_d < 10 nM). C3TD879 is a chemical probe suitable for interrogating the complex biology of CITK.

2-Fluorophenylboronic acid is an organic synthesis intermediate belonging to the fluorinated arylboronic acid class. The electron-withdrawing fluorine substituent in 2-Fluorophenylboronic acid reduces its pKa, thereby enhancing boronate bond formation with diols. 2-Fluorophenylboronic acid serves as a key synthetic intermediate for inhibitors of Plasmodium phosphatidylinositol 4-kinase IIIβ (PI4K). 2-Fluorophenylboronic acid can also be used to functionalize linear polyglycerols for constructing dual dynamic covalent cross-linked hydrogels that support 3D tumor spheroid culture of various cancer cells. 2-Fluorophenylboronic acid is applicable to research related to malaria and tumors.

Boc-Cystamine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Taraxerol is isolated from Taraxacum mongolicum, and has anti-inflammtory and anti-cancer effects. Taraxerol attenuates acute inlammation through inhibition of NF-κB signaling pathway. Taraxerol induces cell apoptosis.

TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity. TD52 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Tolterodine ((R)-(+)-Tolterodine) is a mAChR inhibitor and substrate for cytochrome P450 enzymes. Tolterodine competitively binds acetylcholine, reduces sympathetic excitation, and inhibits involuntary bladder muscle contraction. Tolterodine restores the Nrf2/NF-κB signaling pathway, mediates protection against inflammatory response and ferroptosis. Tolterodine ameliorates LPS (HY-D1056)-induced reactive oxygen species production and lipid oxidation. Tolterodine can be used for the research of urinary tract infections and overactive bladder.

Mal-PEG12-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Vanillylamine is an immediate precursor for capsaicinoids. Vanillylamine is a derivative of Vanillin (HY-N0098) is synthesized through a transaminase reaction in the phenylpropanoid pathway of capsaicinoid synthesis. Vanillylamine significantly alleviates myelosuppression caused by abdominal and pelvic tumor chemotherapy.

Arcotatug (IBI-343 antibody) is a CLDN18.2 targeting humanized monoclonal antibody. Arcotatug can be used for synthesis of ADCs.

Propargyl-PEG4-GGFG-DXd is a drug-linker conjugate for ADC. Propargyl-PEG4-GGFG-DXd contains a ADC linker and a DNA topoisomerase I inhibitor DXd (HY-13631D).

Dendrophenol (Moscatilin) is a NF-κB inhibitor that inhibits inflammation. Dendrophenol exerts potent cytotoxic effect against tumor cells and induces cell cycle arrest and apoptosis. Dendrophenol has antitumor activity. In addition, Dendrophenol can inhibit vascular calcification by inhibiting the activation of WNT3/β-catenin.

Pranoprofen is a non-steroidal anti-inflammatory agent (NSAID) for the research of keratitis or other ophthalmology diseases. Pranoprofen inhibit COX-1 and COX-2 enzymes, thus blocking arachidonic acid converted to eicosanoids and reducing prostaglandins synthesis.

2-(Piperidin-4-yl)ethan-1-ol (4-Piperidineethanol) is a PROTAC linker that can be used in the synthesis of PROTACs.

Benzamidine (Benzenecarboximidamide) hydrochloride hydrate is a competitive protease inhibitor that blocks the hydrolytic cleavage of glucagon by plasmin, trypsin and thrombin. Benzamidine hydrochloride hydrate effectively inhibits the degradation of glucagon by relevant proteases during the collection, storage and analysis of human plasma and blood samples. During in vivo metabolism, Benzamidine hydrochloride hydrate undergoes N-hydroxylation and produces multiple metabolites, exhibiting characteristics of delayed excretion or biphasic elimination. Benzamidine hydrochloride hydrate only induces slight single-strand DNA breaks at high concentrations and shows no significant genotoxic potential overall. Benzamidine hydrochloride hydrate may interfere with the detection of some glucagon antisera, but does not affect key antigen-antibody affinity at specific concentrations. Benzamidine hydrochloride hydrate can be used as a stabilizer in glucagon radioimmunoassays to ensure the accuracy and recovery rate of detection results.

Tetradecane-1,14-diol is a PROTAC linker that can be used in the synthesis of PROTACs.

3-(tert-Butoxycarbonyl)-3-azaspiro[5.5]undecane-9-carboxylic acid is a PROTAC linker that can be used in the synthesis of PROTACs.

(R)-(-)-Gossypol (AT-101) is the levorotatory isomer of a natural product Gossypol. AT-101 is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins with K_is of 260±30 nM, 170±10 nM, and 480±40 nM, respectively.

tert-Butyl trans-4-aminocyclohexanecarboxylate is a PROTAC linker that can be used in the synthesis of PROTACs.

NVP-CGM097 is a potent and selective MDM2 inhibitor with IC₅₀ of 1.7±0.1 nM for hMDM2.

EpoY (SD-142) acts as an irreversible inhibitor of the brain's primary tubulin tyrosine carboxypeptidase (TCP), a complex formed by vasohibin-1 (VASH1) and the small vasohibin binding protein (SVBP). By inhibiting TCP with an IC₅₀ value of approximately 500 nM, EpoY effectively decreases levels of detyrosinated alpha-tubulin, which is crucial for microtubule dynamics and neuronal differentiation. This inhibition leads to significant differentiation defects and has been linked to underlying issues associated with cancer and cardiomyopathies.