Cancer Targeted Therapy

CDK2-IN-23 (Compound 17) is a kinase selective and highly potent CDK2 inhibitor (IC₅₀ = 0.29 nM). CDK2-IN-23 shows the pharmacodynamic inhibition of CDK2 in CCNE1-amplified mouse models. CDK2-IN-23 can be used for the research of cancer.

ZLDI-8 is a Notch activating/cleaving enzyme ADAM-17 inhibitor and inhibits the cleavage of Notch protein. ZLDI-8 decreases the expression of pro-survival/anti-apoptosis and epithelial-mesenchymal transition (EMT) related proteins. ZLDI-8 is also a competitive and irreversible tyrosine phosphatase (Lyp) inhibitor with an IC₅₀ of 31.6 μM and a K_i of 26.22 μM. ZLDI-8 inhibits the growth of MHCC97-H cells with an IC₅₀ of 5.32 μM.

p53 Activator 7 is a p53 mutation Y220C (MDM-2/p53) activator with an EC₅₀ of 104 nM. p53 Activator 7 can bind to p53 mutant and restore its ability to bind DNA (WO2022213975A1; Example B-1). p53 Activator 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Diclofenac (Standard) is the analytical standard of Diclofenac. This product is intended for research and analytical applications. Diclofenac is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.

Mc-Gly-Gly-Phe-Gly-PAB-OH (Mc-GGFG-PAB-OH) is a cleavable ADC linker used for antibody-drug conjugates (ADCs).

Bersanlimab (BI-505) is a fully human monoclonal antibody that targets intercellular adhesion molecule-1 (ICAM-1 or CD54). Bersanlimab has anticancer effects.

m-PEG4-Br is a cleavable ADC linker used in the synthesis of antibody-drug conjugate (ADC) for Trastuzumab (HY-P9907). m-PEG4-Br is placed distally from the monomethyl auristatin E (MMAE) payload to yield an ADC with altered hydrophilicity, antigen binding, and in vitro potency. m-PEG4-Br also can be used as a PROTAC linker that can be used in the synthesis of PROTACs.

NRX-103094 is a Molecular glue and β-catenin/β-TrCP interaction enhancer, with an EC₅₀ of 62 nM for the binding of pSer33/S37A β-catenin peptide to recombinant β-TrCP/Skp1 complex. NRX-103094 shows selectivity for Ser37 phosphorylation-deficient β-catenin, and has no effect on wild-type doubly phosphorylated β-catenin or other β-TrCP substrates. NRX-103094 can be used in research related to colorectal cancer and ovarian endometrioid adenocarcinoma.

1-Boc-azetidine-3-carboxylic acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). 1-Boc-azetidine-3-carboxylic acid is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[2]

Grape seed extract is a natural product, with anti-inflammatory and anti-proliferative effects. Grape seed extract shows inhibitory activity on the fat-metabolizing enzymes pancreatic lipase and lipoprotein lipase. Grape seed extract induces apoptotic in human colorectal cancer cells.

ZXH-1-161 is a potent CRBN modulator that selectively induces the degradation of GSPT1 in a CRBN-dependent manner. ZXH-1-161 can inhibit the proliferation of multiple myeloma cells and exhibits antitumor activity.

CDK9 inhibitor HH1 is a potent and selectively CDK9 inhibitor. CDK9 inhibitor HH1 inhibits the transcription of CDK. CDK9 inhibitor HH1 can be used in research of cancer.

(3S,4S)-A2-32-01 (compound 24 (S,S)) is the low/inactive (S,S)-enantiomer of A2-32-01. A2-32-01 is a potent caseinolytic protease (ClpP) inhibitor. (3S,4S)-A2-32-01 is applicable for oncology and microbiology research.

FANCM-BTR PPI-IN-1 (Compound 32) is a FANCM/BTR interaction inhibitor that blocks the localization of FANCM to telomeres. FANCM-BTR PPI-IN-1 exhibits anticancer activity against osteosarcoma.

DiR (solution) is a long-chain carbocyanine dye. Carbocyanine dyes are widely used as Di to label cells, organelles, liposomes, viruses and lipoproteins.
Solvent and concentration: DMSO: 5 mM

Mangafodipir trisodium (MnDPDP), hepatocellular-specific contrast agent, is an efficacious inhibitor of CIPN (chemotherapy-induced peripheral neuropath) and other conditions caused by cellular oxidative stress. Mangafodipir trisodium shows no negative interference with the tumoricidal activity of chemotherapy.

HDAC9-IN-1 is a selective class IIa HDAC inhibitor that binds to HDAC9 with an IC₅₀ of 40 nM. HDAC9-IN-1 potently inhibits HDACs 4 and 7 while showing weak activity against HDAC6 (IC₅₀ values: 180 nM (HDAC4), 190 nM (HDAC7), 970 nM (HDAC6)). HDAC9-IN-1 significantly inhibits several human cancer cells, induces apoptosis and DNA damage in human cancer cells, and modulates caspase-related proteins and p38 in human cancer cells. HDAC9-IN-1 can be used for the research of oral cancer, breast cancer, gastric cancer.

(R)-9b is an ATP-competitive kinase inhibitor. (R)-9b binds to the ATP-binding site of ACK1/TNK2, inhibiting their kinase activity and autophosphorylation, with a human IC₅₀ of 56 nM. (R)-9b also inhibits JAK2, Tyk2, ALK, c-Src, ABL1, CHK1, FGFR1, LCK, and ROS/ROS1. (R)-9b can be used for research on prostate cancer.

NS3694, a diarylurea compound, is an apoptosome inhibitor. NS3694 inhibits apoptosome formation and caspase activation.

PY159 is a humanized antibody targeting TREM1/CD354. PY159 reprograms immunosuppressive intratumoral myeloid cells towards an inflammatory, anti-tumor phenotype, promotes anti-tumor immune responses, upregulates monocyte activation markers, and induces proinflammatory cytokines. PY159 can be used for the research of platinum-resistant ovarian cancer, advanced solid tumors, and advanced refractory solid tumors.