Tri-GalNAc(OAc)3 Cbz is a ligand for asialoglycoprotein receptor (ASGPR) where the sugars are protected by acetylation and the tris tertiary amine is protected by benzyloxycarbonyloxy (Cbz). This peracetylated tri-GalNAc(OAc)3 Cbz can be serve as a valuable building block for ASGPR-targeted therapies. Its three branches or arms, each ending in a GalNAc sugar, ensure strong binding to hepatocyte ASGPR. However, the key feature lies in its protective groups: acetylated sugars allow for controlled removal to expose reactive sites for conjugation, while the Cbz-protected amine provides stability and can be selectively cleaved to introduce a reactive amine group for further biomolecule attachment, ultimately enabling researchers to tailor tri-GalNAc(OAc)3 Cbz into customized conjugates for specific therapeutic applications.

Tri-GalNAc(OAc)3 TFA is a tri-GalNAc ligand that can be used for the synthesis of GalNAc-LYTAC. GalNAc-LYTAC engages the asialoglycoprotein receptor for targeted protein degradation. tri-GalNAc: triantenerrary N-acetylgalactosamine; LYTAC: lysosome-targeting chimera.

tri-GalNAc-COOH is an asialoglycoprotein receptor (ASGPR) ligand that can be used for LYsosome TArgeting Chimera (LYTAC) research.

tri-GalNAc-COOH acetylation is the acetylated and modified form of tri-GalNAc-COOH. tri-GalNAc-COOH acetylation can be used for the synthesis of LYTAC.

ASGPR ligand-1 is a compound that targets the asialoglycoprotein receptor (ASGPR) and is utilized in various disease research contexts .

Triantennary GalNAc Acid is an asialoglycoprotein receptor (ASGPR) ligand for lysosomal targeting chimera (LYTAC) research and development.

Tri-GalNAc-NHS ester is a LYsosome TArgeting Chimera (LYTAC) and a ligand of asialoglycoprotein receptor (ASGPR). ASGPR is a lysosomal targeting receptor specifically expressed on liver cells, for the degradation of extracellular proteins including membrane proteins. Tri-GalNAc-NHS ester can be used as a protein degrader and it can be used for the research of LYTAC.

MS8815 is a selective enhancer of zeste homolog 2 (EZH2) PROTAC degrader. MS8815 has inhibition activity for EZH2 with an IC50 value of 8.6 nM. MS8815 can be used for the research of triple-negative breast cancer (TNBC).

Tri-b-GalNAc-b-Ala-PEG3-MAL contains three terminal beta-N-acetylgalactosamine (GalNAc) sugars arranged in a trivalent configuration, facilitating high-affinity binding to the asialoglycoprotein receptor (ASGPR) expressed on hepatocyte surfaces. The crucial functional group is a terminal maleimide (MAL) moiety, enabling chemoselective bioconjugation with biomolecules harboring thiol (-SH) groups. This strategy allows for site-specific conjugation under mild conditions, valuable for developing targeted conjugates in disciplines like targeted drug delivery and antibody-drug conjugate (ADC) development for hepatocellular carcinoma.

BSJ-05-037 is a potent and selective heterobifunctional degrader of ITK with DC50 of 17.6-41.8 nM in TCL lines DERL-2 and Hut78. BSJ-05-037 induces potent degradation of ITK dependent on CRBN, neddylation, and the proteasome. BSJ-05-037 induces GATA-3 loss and decreases chemotherapy resistance in vitro. BSJ-05-037 disrupts TCR signaling, downregulates the Th2-associated transcription factor GATA-3, and can overcome chemotherapy resistance in TCL models in vivo.

(±)-U-50488 ((±)-trans-(1R,2R)-U-50488) is a selective kappa opioid receptor agonist. (±)-U-50488 can improve symptoms related to status epilepticus, but has no significant effect on spontaneous seizure episodes. (±)-U-50488 can be used for research of epilepsy.

WX-02-23 is a small-molecule probe that stereoselectively and site-specifically binds to C258 of FOXA1 and C1111 of SF3B1. WX-02-23 remodels FOXA1's chromatin binding and pioneer activity in a DNA-dependent manner, disrupts spliceosome assembly, and enhances the thermal stability of SF3B1. WX-02-23 inhibits tumor cell proliferation and induces apoptosis. WX-02-23 can be used for research on cancers such as prostate cancer.

S-enantiomer of ARV-102. ARV-102 is a highly potent, orally bioavailable PROTAC that targets LRRK2 with a of 0.14 nM, designed to cross the blood-brain barrier to address neurodegenerative diseases. By hijacking the body’s ubiquitin-proteasome system, it achieves deep and sustained degradation of LRRK2 protein in both peripheral tissues and the central nervous system, offering a potentially superior therapeutic approach over traditional kinase inhibitors.

dBET6 is a highly potent, selective and cell-permeable degrader of BET with an IC50 of 14 nM, and has antitumor activity.

PROTAC BCL6 Degrader-3 (compound 92) is a BCL6 PROTAC degrader. PROTAC BCL6 Degrader-3 can be used for the study of cancer or an autoimmune disease.

β-Catenin modulator-9 (Compound IIa-2075) is a β-Catenin modulator. β-Catenin modulator-9 specifically targets the activity of the stable β-catenin pool and inhibits the Wnt signaling pathway. β-Catenin modulator-9 can be used in cancer-related research.

α5β1 integrin-IN-1 (compound 65) is a potent and selective α5β1 integrin inhibitor with a pIC50 of 9.4. α5β1 integrin-IN-1 displays >10000-fold selectivity for α5β1 over αVβ3 (pIC50 = 5.5). α5β1 integrin-IN-1 reduces airway smooth muscle (ASM) tension through the disruption of cellular tethering. α5β1 integrin-IN-1 exhibits excellent inhalation pharmacokinetics in rodent. α5β1 integrin-IN-1 can be used for asthma research.

α4β7 Integrin-IN-1 (Example 356) is a potent inhibitor of α4β7 integrin (integrin). Its ability to block the interaction between α4β7 integrin and MadCAM-1 (EC50) is 0.05 nM. α4β7 Integrin-IN-1 can be used for the study of inflammatory bowel disease.

α1A/1D-Adrenoceptor antagonist-1 (Compound 15) is a selective α1A/1D-adrenoceptor dual antagonist with IC50 values of 20.26 and 164.9 nM. α1A/1D-Adrenoceptor antagonist-1 shows an IC50 of 1912 nM for α1B-adrenoceptor.α1A/1D-Adrenoceptor antagonist-1 can be used for research of benign prostatic hyperplasia.

α,δ-NAG is an orally active glutaminase-resistant less-hydrolyzable L-Glutamine derivative. α,δ-NAG is a G protein-coupled receptor (GPCR) allosteric modulator. α,δ-NAG suppresses neutrophilic airway inflammation by activating the GPCR/ERK/MKP-1 pathway. α,δ-NAG can be used for the researches of inflammation and immunology, such as asthma.

ZMC2 is a thiosemicarbazone-class metal ion chelator and zinc ionophore with a human mutant p53R175H binding Ka of 27.4 nM.ZMC2 binds Fe, Cu, Mn, Zn, and other transition metals.ZMC2 facilitates zinc transport across membranes.ZMC2 restores zinc binding to zinc-deficient p53 mutants, restoring wild-type structure and function, including site-specific DNA binding.ZMC2 generates reactive oxygen species (ROS).ZMC2 can be used for the research of cancer.

ZLY025 is a potent and orally active CCNK molecular glue degrader with an DC50 of 42.7 nM. ZLY025 exhibits broad-spectrum antiproliferative activity against various tumor cells with IC50 values ranging from 0.08 to 2.45 μM. ZLY025 can induce cells apoptosis and G1 phase arrest. ZLY025 can be used for the research of cancer, such as lung cancer.

ZLWH-67 is a β-Carboline derivative and Antibacterial agent. ZLWH-67 inhibits DNA synthesis, suppresses biofilm formation, and increases reactive oxygen species (ROS) levels. ZLWH-67 exhibits potent in vitro antibacterial activity against MRSA (MIC = 0.5-4 μg/mL), S. epidermidis (MIC = 4 μg/mL), E. faecalis (MIC = 4-8 μg/mL), and S. pneumoniae (MIC = 16 μg/mL). ZLWH-67 displays anti-MRSA effects in murine skin and pneumonia infection models.

ZK-Thiazolidinone is an ATP-competitive Polo-like kinase 1 (Plk1) inhibitor with an IC50 of 19 nM. ZK-Thiazolidinone inhibits tumor cell proliferation, induces cell cycle arrest and typical mitotic defects. ZK-Thiazolidinone impairs the recruitment of γ-tubulin and Aurora A kinase to centrosomes, resulting in failure of bipolar spindle maintenance and sister chromatid arm cohesion.\nZK-Thiazolidinone is applicable for cancer research.

ZAK-IN-2 (Compound 8) is a selective, covalent ZAK inhibitor with an IC50 of 11.5 nM. ZAK-IN-2 forms a covalent bond with Cys22 in the P-loop of ZAK to inhibit its kinase activity. ZAK-IN-2 inhibits the phosphorylation of the downstream target p38. ZAK-IN-2 blocks Doxorubicin-induced cleavage of Caspase 3. ZAK-IN-2 is applicable to research related to myocardial hypertrophy.

Z226407860 is a RING-box protein 1 (RBX1) inhibitor. Z226407860 reduces house dust mite-induced airway epithelial injury and ROS accumulation by inhibiting RBX1. Z226407860 can be used for the research of asthma.

YZ-836P is a Protein arginine methyltransferase 5 (PRMT5) targeting agent. YZ-836P promotes ubiquitination and proteasomal degradation of PRMT5 in a cereblon (CRBN)-dependent manner, which in turn reduces levels of its downstream target KLF5. YZ-836P induces G1 phase cell cycle arrest in triple-negative breast cancer cells. YZ-836P induces apoptosis in triple-negative breast cancer cells. YZ-836P exerts cytotoxic effects on triple-negative breast cancer cells. YZ-836P inhibits the growth of triple-negative breast cancer patient-derived organoids. YZ-836P inhibits the growth of triple-negative breast cancer xenografts in nude mice. YZ-836P can be used for the research of triple-negative breast cancer.

YM-1758735 is an orally active androgen receptor (AR) antagonist with an IC50 of 0.2 μM. YM-1758735 inhibits AR-mediated transcriptional activation. YM-1758735 can be used for the research of prostate.

YCH3292, a derivative of YCH189 is a potent, selective and orally active PARP1/2 inhibitor with IC50 both <0.001 nM. YCH3292 can increase the stability of PARP-DNA complexes. YCH3292 exhibits robust antiproliferative activity. YCH3292 can induce double-strand breaks in DNA, increase the protein levels of γH2AX, P-RPA32, and P-Chk1 and induce tumor cells S or G2/M phase arrest and apoptosis. YCH3292 can inhibit tumor growth in MC38 xenograft model.