α-Synuclein-IN-17 (Compound 10) is an α-Synuclein inhibitor, with an IC50 value of 9 μM. α-Synuclein-IN-17 exhibits potent inhibitory activity against both in-vitro assembled asyn fibrils and LBD brain tissue-amplified asyn fibrils. α-Synuclein-IN-17 can be used for the study of Parkinson's disease (PD) and Lewy Body Disease (LBD).

ZSTK3744 is an aryl hydrocarbon receptor (AhR) agonist. ZSTK3744 directly binds to AhR, upregulates the expression of AhR target genes including CYP1A1, CYP1B1 and TIPARP, and mediates cell growth inhibitory activity in triple-negative breast cancer cells. ZSTK3744 induces apoptosis in triple-negative breast cancer cells. ZSTK3744 exhibits anti-tumor activity and can be used in the research of chemoresistant triple-negative breast cancer.

WWZ-11-098 is a selective CDK6 PROTAC degrader with DC50 of 2.6 nM. WWZ-11-098 induces degradation of CDK6 in a CRBN-dependent manner, while sparing CDK1, CDK2, CDK4, and CDK9. WWZ-11-098 induces apoptosis, G1-S cell cycle arrest and shows anti-proliferative activity in cancer cells. WWZ-11-098 exhibits antitumor efficacy in a xenograft model without signs of toxicity. WWZ-11-098 can be used for the research of leukemia. (Pink: CDK6 ligand ; Blue: Cereblon E3 ligase ligand; Black: linker).

VUF 4904 is an impentamine analog and a neutral antagonist of the histamine H3 receptor. VUF 4904 can be used in the research of diseases related to the function of the H3 receptor, such as Alzheimer's disease.

UDP-N-acetylmuramoyl-L-alanyl-D-glutamyl-6-carboxy-L-lysyl-D-alanyl-D-alanine is a nucleoside metabolite.

UDP-2-alkyne-GlcNAc (Compound 3) is a UDP-GlcNAc derivative. UDP-2-alkyne-GlcNAc can be used for the remodeling of cell surface glycans.

Tyrosine kinase-IN-11 (Compound 4b) is a tyrosine kinase inhibitor. Tyrosine kinase-IN-11 decreases general tyrosine kinase activity, selectively inhibits PDGFR-β, SRC, and c-MET kinases. Tyrosine kinase-IN-11 induces apoptosis, accompanied by reduced ERK signalings. Tyrosine kinase-IN-11 exhibits selective anticancer activity against pancreatic cancer and renal cancer.

Triptolide-6-succinate-β-D-glucose (Compound 2) is a glucose-conjugated derivative of Triptolide. Triptolide-6-succinate-β-D-glucose is a tumor-selective prodrug targeting glucose transporters ( GLUT). Triptolide-6-succinate-β-D-glucose can induce the degradation of the RPB subunit of RNA polymerase II. Triptolide-6-succinate-β-D-glucose inhibits the proliferation of HEK293T cells with an IC50 value of 268 nM. Triptolide-6-succinate-β-D-glucose can be used for the research of cancer, such as prostatic cancer.

TLD-1433 is the fourth-generation ruthenium (II) based photodynamic compound (PDC). TLD-1433 is activated by green light (525 ± 25 nm) and efficiently generates ROS to achieve pathogen inactivation. After photoinactivation, TLD-1433 significantly induces lipid peroxidation of the cell membrane, which can directly damage the integrity of the viral envelope. TLD-1433 has ID50 for enveloped viruses (such as H1N1 influenza virus, coronavirus OC43, HSV-1, Zika virus) is as low as nanomolar level; for non-enveloped viruses (such as adenovirus Ad5, mammalian rotavirus MRV), a concentration of micro-molar level is required for inactivation. TLD-1433 has antigen retention property and can be used for the preparation of inactivated vaccines.

Ticagrelor acetonide (Isopropylidene ticagrelor) (Compound 7) is a drug intermediate that can be used for the synthesis of lysine-specific demethylase (LSD1) inhibitors.

TGF-β/Smad-IN-3 (Compound 4w) is an effective TGF-β/Smad inhibitor. TGF-β/Smad-IN-3 exerts anti-pulmonary fibrosis activity by simultaneously inhibiting the TGF-β/Smad and MAPK signaling pathways. TGF-β/Smad-IN-3 significantly inhibits collagen deposition induced by TGF-β1, with its IC50 value being 3.21 μM. TGF-β/Smad-IN-3 has an IC₅₀ of 46.77 nM for the autocrine motility factor (ATX). TGF-β/Smad-IN-3 significantly reduces the expression levels of α-SMA, COL1A1 and FN in TGF-β1-induced CCC-HPF-1 cells, and effectively inhibited TGF-β1-induced cell migration. TGF-β/Smad-IN-3 can be used for the study of pulmonary fibrosis.

Terfenadine N-oxide, an N-oxide derivative of Terfenadine, is a histamine H1 receptor antagonist (IC50 = 2.73 μM) and an hERG potassium channel inhibitor (IC50 = 0.698 μM). Terfenadine N-oxide is can be used for the research of histamine-related allergic diseases and hERG channel-associated arrhythmias.

Tafuramycin A, a Duocarmycin derivative, is a potent anticancer and parasite attenuating agent. Tafuramycin A can be used for triple-negative breast cancer (TNBC) and malaria infection research.

SUVN-507 is a 5-HT6 receptor antagonist. SUVN-507 can reverse cognitive impairments and enhance excitatory neural transmission while weakening inhibitory neural transmission. SUVN-507 can be used for the research of neurological disease, such as Alzheimer's disease.

SIRT2-IN-18 (Compound 8) is a SIRT2 inhibitor with IC50s of 5.3  and 12.3 μM for SmSIRT2 and hSIRT2, respectively. SIRT2-IN-18 shows potent antischistosomal activities against both Liberian and Puerto Rican strains of Schistosoma mansoni and reduces schistosomula and adult worm pair viability, pairing, and egg production, with low cytotoxicity in mammalian cells. SIRT2-IN-18 increases histone H3 hyperacetylation and induces cytochrome c-mediated apoptosis.

Simeton is a methoxy-5-triazine herbicide used for weed control in agricultural crops including corn, wheat, maize, and barley. Simeton is a methoxy-5-triazine herbicide widely used for weed control in agricultural crops including corn, wheat, maize, and barley.

Satranidazole is an orally effective insecticide and antimicrobial agent with high electron affinity. Satranidazole forms reduced nitro intermediates, which interact with DNA, causing helix instability, strand breakage and release of thymidine derivatives. Satranidazole exhibits antitrichomonal activity against Trichomonas vaginalis and Trichomonas foetus, and antiamoebic activity in rodent models of hepatic amoebiasis and caecal amoebiasis. Satranidazole inhibits the replication of bacteriophage φX174 DNA. Satranidazole can be used in research related to caecal amoebiasis, trichomoniasis and anaerobic bacterial infections.

RU 56279 is an androgen receptor (AR) antagonist with strong and systemic anti-androgenic activity. RU 56279 is also a common, potent and long-lasting anti-androgen metabolite of RU 56187 and RU 58841 in vivo. RU 56279 can be used as an AR ligand to construct an AR-targeted prodrug system for the study of AR-positive tumor cells.

Ro-65-3479 is a selective metabotropic glutamate receptor (mGlu2/3) antagonist. Ro-65-3479 blocks glutamate-induced signaling and modulates calcium channel activity. Ro-65-3479 is promising for research of disorders involving glutamatergic dysregulation, such as anxiety, schizophrenia, and neurodegenerative diseases.

RM-046 is an orally active, selective ternary complex inhibitor of KRASQ61H (active form). RM-046 forms a ternary complex with cyclophilin A, binds to active KRASQ61H in a non-covalent manner, blocks effector binding via steric hindrance and inhibits downstream signal transduction. RM-046 inhibits ERK phosphorylation and cancer cell proliferation, and induces sustained RAS pathway signal inhibition, anti-tumor activity and tumor regression in preclinical xenograft models. RM-046 can be used for the research of KRASQ61H mutant cancers.

RAFKBP12 is a FKBP12 PROTAC degrader. RAFKBP12 demonstrates the feasibility of the CAP-TAC strategy, which enables proteasome-dependent degradation of FKBP12 that is independent of E3 ubiquitin ligases and protein ubiquitination. (Pink: FKBP12 ligand ; Blue: RPN13 ligand ; Black: linker).

PXS 64, a mannose-6-phosphate (M6P) analogue. a lipophilic prodrug of PXS 25. PXS 64 is an effective anti-fibrotic agent by inhibiting the activation of latent TGF-β1. PXS64, inhibits fibrosis via TGF-β1 pathway in human lung fibroblasts. PXS 64 reduces TGFβ-mediated collagen IV, fibronectin, MCP-1, and phospho-smad2 expression in kidney cells. PXS 64 reduces collagen deposition in dermal scar fibroblasts. PXS 64 can be used for the research of chronic kidney disease, idiopathic pulmonary fibrosis, scarring.

PXS 25 is a cation-independent mannose 6-phosphate receptor (CI-M6PR) inhibitor that inhibits CI-M6PR-mediated activation of latent TGF-β1. PXS 25 inhibits conversion of high glucose-induced latent TGF-β1 to active TGF-β1 in proximal tubule cells under normoxic conditions. PXS 25 suppresses high glucose-induced fibronectin, collagen IV production, and phosphorylated Smad 2 in proximal tubule cells under normoxic conditions. PXS 25 has antifibrotic properties in skin fibroblasts. PXS 25 can be used for the research of diabetic nephropathy.

PROTAC TEAD degrader-2 (Compound 31) is an efficient TEAD1 PROTAC degrader with a DC50 of 0.6 nM. PROTAC TEAD degrader-2 inhibits the YAP/TAZ-TEAD interaction, with a IC50 of 1.8 nM. PROTAC TEAD degrader-2 exhibits significant selective inhibitory activity against YAP-dependent cancer cells and effectively suppresses the transcriptional activity mediated by YAP. PROTAC TEAD degrader-2 can be used for research on mesothelioma and glioma. (Pink: TEAD1 ligand ; Blue: Cereblon ligand ; Black: linker ).

PROTAC HMGCR Degrader-1 is an orally active HMGCR PROTAC degrader with IC50 of 1.32 μM. PROTAC HMGCR Degrader-1 is a lactone prodrug of PROTAC HMGCR Degrader-2. PROTAC HMGCR Degrader-1 achieves high plasma exposure of the active ingredient leading to robust HMGCR degradation and demonstrating promising cholesterol-lowering efficacy in vivo. PROTAC HMGCR Degrader-1 can be used for hyperlipidemia research.

PROTAC EGFR degrader 16 (Compound 98) a selective EGFR PROTAC degrader with DC50 values of < 50 nM in NCI-H1975 (EGFR L858R-T970M), NCI-H3225 (EGFR L858R) and NCI-H1976 + CS (EGFR L858R-T970M-L797S). PROTAC EGFR degrader 16 can be used for the study of EGFR-driven cancerssuch as non-small cell lung cancer (Pink: EGFR ligand; Blue: CRBN ligand; Black: Linker; EGFR ligand + Linker).

PROTAC c-Met Degrader-4 (compound D15) is a potent orally active PROTAC c-MET degrader. PROTAC c-Met Degrader-4 demonstrates excellent intracellular degradation potency with a DC50 < 0.5 nM. PROTAC c-Met Degrader-4 induces cell cycle arrest and apoptosis, inhibits cell invasion and migration, thereby suppressing cell proliferation. PROTAC c-Met Degrader-4 inhibits the growth of Hs746T xenograft tumors in nude mice. PROTAC c-Met Degrader-4 can be used for cancer research, such as non-small cell lung cancer and gastric cancer.

PRMT5-IN-55 is an inhibitor of PRMT5 with a pIC50 value of 9.6 at a 10 nM enzyme.

PI3K/PIKK-IN-2 (compound 2) is an inhibitor of PI3K/PIKK. PI3K/PIKK-IN-2 can be used in preparing antibody-drug conjugates (ADCs).

Phenylalanylphenylalanylamide (H-Phe-Phe-NH₂) is a ligand for the substance P 1–7 (SP1-7) binding site with a Ki value of 1.5 nM. Phenylalanylphenylalanylamide exerts significant anti-allodynic and anti-hyperalgesic effects in animal models of neuropathic pain following central administratio. Phenylalanylphenylalanylamide shows no distinct effect after peripheral (intraperitoneal) administration. Phenylalanylphenylalanylamide can be used for research on pain-related diseases.