KD025m1 is a novel selective ROCK2 inhibitor. KD025m1 has good anti obesity, improved insulin sensitivity, and blood glucose control effects. KD025m1 can be used to study metabolic diseases such as diabetes and obesity.

PD 172760 is a selective D4 receptor antagonist. PD 172760 along with the action of other neurotransmitter receptors may be important in treating psychosis.

DD-04-038 is a molecular glue degrader. DD-04-038 induces proteins (such as IKZF1/3, ZBED3 and PATZ1) to bind to CRBN, promoting their ubiquitination and degradation.

ALK ligand-Linker Conjugate 1 is a ALK ligand-linker conjugate that can be used for synthesis of PROTAC ALK degrader-4.

NSC 850745 is a selective and potent c-Met/STAT3 inhibitor with IC50 values of 210 and 670 nM. NSC 850745 can inhibit cell proliferation, induce G2/M phase arrest and induce apoptosis. NSC 850745 can downregulate AKT-1, VEGF and Bcl-2 expression and upregulate p53, Bax and caspase expression. NSC 850745 can be used for the research of cancer, such as leukemia and colon cancer.

SMARCA2/4 Ligand-Linker Conjugate 2 is a target protein ligand-linker conjugate that can be used to synthesize PROTAC AU-15330.

A2073 is a flavagline derivative that potently inhibits the proliferation of erythroleukemia cells by causing cell cycle arrest and suppressing the MAPK, NF-κB, and PI3K signaling pathways. A2073 formes stable interactions with cell cycle-related proteins (CDK1, CCNA2, PRIM1). A2073 exhibits significant anti-proliferative activity against tumor cells while maintaining a favorable toxicity profile in a zebrafish xenograft tumor model. A2073 can be used for the study of acute erythroleukemia.

AD-5467 is a potent and selective aldose reductase inhibitor. AD-5467 exhibits antidiabetic effect. AD-5467 can be used for the research of metabolic disease, such as diabetes.

Osunprotafib (ABBV-CLS-484) hydrochloride is an orally active and selective active site PTPN1 (IC50: 2.5 nM) and PTPN2(IC50: 1.8 nM) inhibitor. Osunprotafib hydrochloride has 6-8-fold weaker activity on PTPN9 and no detectable activity on SHP-1 or SHP-2. Osunprotafib hydrochloride increases the sensitivity of human cancer cell lines to IFNγ. Osunprotafib hydrochloride generates robust anti-tumor immunity by enhancing JAK-STAT signalling and reducing T cell dysfunction.

CCC-0975 is a hepatitis B virus (HBV) inhibitor (EC50=10 μM). CCC-0975 interferes with the conversion of relaxed circular DNA (rcDNA) to cccDNA, synchronously reducing cccDNA and its precursor deproteinized rcDNA (DP-rcDNA) without promoting their intracellular degradation. CCC-0975 is promising for research of chronic hepatitis B.

PNU-142586 is the major metabolite of Linezolid. PNU-142586 can inhibit the activity of DNA topoisomerase 2-α (TOP2A) and DNA topoisomerase 2-β (TOP2B). PNU-142586 interferes with DNA replication and transcription by blocking the binding of DNA to TOP2 and inhibiting ATP hydrolysis. PNU-142586 can be used to study Linezolid-induced hematotoxicity and its molecular mechanism.

FAPI-JNU is a molecule targeting fibroblast activation protein (FAP). FAPI-JNU specifically binds to FAP highly expressed in the tumor microenvironment, and uses radionuclides [68Ga]Ga or [177Lu]Lu to achieve tumor imaging diagnosis. [177Lu]Lu−FAPI−JNU can effectively target and inhibit tumor growth in tumor-bearing mice. FAPI-JNU is promising for research of FAP-positive tumors (such as various solid tumors).

Dacemazine (Ahistan) is a phenothiazine derivative that acts as a histamine H1 receptor antagonist. Dacemazine exhibits local anesthetic activity and can alleviate spasms induced by acetylcholine and histamine.

PXR ligand-Linker Conjugate 1 is a conjugate of PXR ligand and linker, which can be used to synthesize PROTAC MI1013.

KRAS G12C Ligand-Linker Conjugates 1 is a conjugate of KRASG12C ligand and linker, which can be used in the synthesis of PROTAC YF135.

BCPT02 is a ADC linker, used in the synthesis of antibody-drug conjugates (ADCs).

STG-001 is a retinol binding protein 4 (RBP4) antagonist. STG-001 inhibits RBP4 to reduce the synthesis of retinal and diretinol, thereby preventing photoreceptor degeneration. STG-001 can be used in the study of sexually precocious nephropathy (STGD).

Kynuramine is an endogenous amine that serves as a fluorescent substrate and probe for plasma amine oxidase.

SC-57461 is a potent, selective, and orally effective LTA4 hydrolase (Ki = 23 nM and 27 nM) inhibitor. SC-57461 can significantly inhibit edema. SC-57461 is commonly used in the study of inflammatory skin conditions.

SP-141 (hydrochloride) is a specific inhibitor of MDM2. SP-141 (hydrochloride) promotes MDM2 auto-ubiquitination and degradation. SP-141 (hydrochloride) might be used for the research of pancreatic cancer and breast cancer cells.

VUBI1-octanoic acid is a conjugate of SOS1 ligand and linker, which can be used in the synthesis of (4S)-PROTAC SOS1 degrader-1.

Thalidomide-C1-O-CO-C2 is a ligand for E3 ubiquitin ligase. Thalidomide-C1-O-CO-C2 can be connected to Aurora-A ligand 1 by a linker to form PROTAC CDK4/6/9 degrader 2

AM11638 is an endocannabinoid analog targeting cannabinoid receptors (CB1 and CB2 receptors) with analgesic effects. AM11638 is promising for research of neurological diseases and inflammation-related diseases.

Luvesilocin (Example 6) is a tryptamine prodrug. Luvesilocin can convert into an active form, acting as a 5HT2A agonist in vivo upon administration. Luvesilocin can be studied in research for mental diorders.

BMS-229724 is an orally active and tight-binding cytosolic phospholipase A2 (cPLA2) inhibitor with an IC50 of 2.8 μM. BMS-229724 can inhibit the production of arachidonic acid and eicosanoids in U937 cells, neutrophils, platelets, and other cells. BMS-229724 has anti-inflammatory activity and can be used in the research of diseases such as skin inflammation.

LXT34 (Example 2) is a GPR120 agonist. LXT34 has an anti-inflammatory activity. LXT34 promotes GLP-1 formation in the gastrointestinal tract and improves insulin resistance in macrophages and pancreas cells. LXT34 can be used for inflammatory diseases, such as type 2 diabetes, obesity and non-alcoholic fatty liver research.

Dopamine D4 receptor ligand 3 (Compound 16) is a dopamine D4 receptor (D4R) antagonist (pKi: 8.86). Dopamine D4 receptor ligand 3 has pIC50 values of 5.78, 5.55, and 6.17 for Go, Gi, and βArr2 sensors in HEK-293T cells, respectively. Dopamine D4 receptor ligand 3 inhibits the viability of three human glioma cell lines, U87 MG, T98G, and U251 MG. Dopamine D4 receptor ligand 3 induces ROS production and mitochondrial dysfunction in glioma cells.

SAR216471 is a P2Y12 receptor antagonist. SAR216471 reversibly blocks the binding of 2MeSADP to P2Y12 receptors in vitro with an IC50 of 17 nM. SAR216471 can result in the inhibition of platelet aggregation. SAR216471 exhibits anti-thrombotic activity in rat model. SAR216471 can be studied in research on thrombosis.

TriOncoFAP-GlyPro-MMAE is a small molecule drug conjugate (SMDC) targeting fibroblast activation protein (FAP) with an IC50 of 13 pmol/L. TriOncoFAP-GlyPro-MMAE combines a FAP-targeting ligand (TriOnco), a cleavable glycine-proline linker, and a cytotoxic payload (MMAE).

YZ-35 is a STAT3 inhibitor, with a Ki value of 0.38 μM. YZ-35 binds directly to STAT3 with high affinity, exhibiting a dissociation constant (Kd) of 190 nM. YZ-35 directly attenuates the dual phosphorylation of STAT3 (Tyr705 and Ser727). YZ-35 suppresses colony formation, cellular migration, and induces apoptosis in breast cancer cell lines (BCSC). YZ-35 selectively suppresses BCSC self-renewal. YZ-35 inhibits tumor growth in the BCSC xenograft models. YZ-35 can be used for the study of breast cancer.