C199 is a PROTAC degrader targeting PRMT4 (DC50 = 106 nM). C199 shows high selectivity for PRMT4 over other protein arginile methyltransferases. C199 exhibits strong cell degradation ability. C199 induces apoptosis in MM cell lines. C199 efficiently clears PRMT4 protein via the VHL-proteasome pathway. C199 has a relatively long half-life and shows strong anti-multiple myeloma (MM) tumor activity.

AM12814 is a potent and partial CB1 and CB2 agonist with Ki values of 0.7 nM and 3.4 nM. AM12814 can inhibit cAMP accumulation and recruitse β-arrestin 2. AM12814 exhibits cannabimimetic effects. AM12814 can be used for the research of neurological disease, suah as catalepsy.

RSL3-NH2-Ala-Val-DBCO-PEG4-Maleimide is a drug-linker conjugate for ADC. RSL3-NH2-Ala-Val-DBCO-PEG4-Maleimide consists of a GPX4 inhibitor and ferroptosis inducer (RSL3-NH2) and a linker (H-Ala-Val-OH). RSL3-NH2-Ala-Val-DBCO-PEG4-Maleimide can be used for synthesis of ADCs.

PD-161182 is a non-peptide NK-3 antagonist. PD-161182 can be studied in NK-3-related central nervous system disturbances, pain, inflammation, pulmonary and skin diseases.

PFI-7-O-C4-piperazin is a E3 ligase ligand-linker conjugate that can be used for synthesis of PROTACs, such as NEP162. The E3 ligase ligand (PFI-7) of NEP162 is a highly selective antagonist of GID4 (KD = 0.22 μM). NEP162 is a BRD4 PROTAC degrader with anti-tumor activity[1].

NEP162 is a BRD4 PROTAC degrader with DC50s of 1.2 and 1.6 μM in SW480 and U2OS cells. NEP162 exhibits antiproliferative activity, effectively inhibits tumor growth and induces apoptosis. NEP162 can be used for the study of osteosarcoma, colorectal cancer and non-small cell lung cancer, etc.

tri(GalNAc-PEG2)-PEG4-cyclo(Ac-DCAW-{Arg(3F-Ph)-PEG2}-LGELVWCT) (Cys2-Cys12) is an asialoglycoprotein receptor (ASGPR) ligand that can be used for LYsosome TArgeting Chimera (LYTAC) research.

AZD3409 is a prenyl inhibitor that exhibits inhibitory activity against both farnesyl transferase and geranylgeranyl transferase I. AZD3409 inhibits the growth of breast cancer cells, with IC50s of 220 nM (MDA-MB-468), 180 nM (MDA-MB-361), and 290 nM (SK-Br-3). AZD3409 significantly reduces the activation level of AKT in breast cancer cell lines. AZD3409 induces G0/G1 phase arrest in MDA-MB-468 cells, causes G2/M phase arrest in MDA-MB-361 cells. AZD3409 can be used for the study of breast cancer.

FE101120 is a non-peptide agonist CCK2 receptor agonist. FE101120 can be used for the study of diabetes.

MC-Gly-Gly-Phe-OSu is an ADC linker. MC-Gly-Gly-Phe-OSu can be used for the research of cancer.

WP-1034 is a JAK-STAT inhibitor with proapoptotic and antileukemic activity in acute myeloid leukemia (AML). WP-1034 blocks activation of Stat 3 and 5. WP-1034 induces cell cycle arrest and triggers apoptosis. WP-1034 can be used for AML research.

SB 414240 is a selective neurokinin-2 receptor (NK-2R) antagonist with Kis of 1 nM and 193 nM for human NK-3R and human NK-2R, respectively. SB 414240 does not bind the human μ-opioid receptor (hMOR). SB 414240 can be used for the study of neurological disease.

Boc-4-(3-oxobutyl)piperidine-(S,R,S)-AHPC is an E3 ligase ligand-linker conjugatecan be used in the synthesis of PROTAC BRD2 BD1 Degrader-1.

SK2220691 is a potent TRPV4 inhibitor. SK2220691 inhibits pulmonary edema induced by GSK1016790. SK2220691 inhibits HCl-induced increases in key factors such as VEGF, keratinocyte-derived chemokine (KC; CXCL1), and granulocyte colony-stimulating factor (GCSF).

HDZI 2,4OH exerts significant anti anxiety activity through GABA receptors. HDZI 2,4OH can penetrate the blood-brain barrier. HDZI 2,4OH exhibits low toxicity in zebrafish. HDZI 2,4OH can be used for research on neurological disorders such as anxiety disorders.

HI042 is a FMS-like Tyrosine Kinase 3 (FLT3) inhibitor. HI042 shows IC50 values of 0.62 μM for MOLM-13, 0.33 μM for MV4-11, and 0.89 μM for OCI-AML3 cells. HI042 selectively reduces the viability of FLT3-internal tandem duplication (FLT3/TD) mutations-positive cell lines, induces apoptosis, disrupts cell cycle progression, and diminishes the clonogenic potential. HI042 can be used for the research of acute myeloid leukemia (AML).

Carbuterol (SKF 40383-A) is a selective β2-adrenergic receptor agonist that primarily targets bronchial smooth muscle, exhibiting significant bronchodilatory and anti-allergic activity. Carbuterol can directly inhibit the immunologically induced release of histamine and slow-reacting substance of anaphylaxis (SRS-A), thereby alleviating allergic responses. Carbuterol exerts mild β1-mediated cardiac stimulation and is applicable to studies related to respiratory and immune-related diseases such as asthma and allergic disorders.

XIAP ligand-Linker Conjugate 1 is an E3 ligase ligand-linker conjugate that incorporates the XIAP BIR2 ligand XB2M54 and linker. XIAP ligand-Linker Conjugate 1 can be used for synthesis of PROTAC ERα Degrader-1.

HPK1 ligand 4 is a PROTAC target protein ligand that can be used for synthesis of PROTACs, such as PROTAC HPK1 Degrader-5. PROTAC HPK1 Degrader-5 is a potent and orally active HPK1 PROTAC degrader with anti-tumor activity.

diABZI-Mal is a STING agonist. diABZI-Mal activates cGAS-STING pathway to induce cytokine production such as interferon-type I. diABZI-Mal promotes maturation of DC cells and efficiently induces CD8+ T immune reaction. diABZI-Mal inhibits tumor growth.

MI891 is a highly selective PXR antagonist (IC50 = 3.76 μM, Kd = 1.7 μM) and inverse agonist (IC50 = 6.1 μM). MI891 selectively disrupts the interaction between PXR and its coactivator SRC1. MI891 effectively inhibits Rifampicin-induced PXR activation. MI891 is useful for the study of metabolic diseases and other diseases.

TM471-1 is an orally active and covalent Bruton's tyrosine kinase (BTK) inhibitor with IC50 values of 1.3 nM (BTKWT), >40,000 nM (BTKC481S), 7.9 nM (TEC) and 12.4 nM (TXK). TM471-1 inhibits cell growth in vivo and in vitro, arrests cell cycle at G0/G1 phase and induces cell apoptosis.

KW-2478 (hydrochloride) is an HSP90 inhibitor (IC50 = 3.8 nM). KW-2478 inhibits the growth and induces apoptosis in chronic myeloid leukemia (CML) cells and liver cancer cells. KW-2478 weakens the BCR/ABL and MAPK signaling pathways, leading to increased p27 and p21 expression and decreased cyclin B1 expression. KW-2478 downregulates STAT3 expression. KW-2478 may be used in research on cancers such as CML and liver cancer.

F3-PEG8-RiboTAC is a RiboTAC that can specifically degrade the mRNA of the oncogene LGALS1. F3-PEG8-RiboTAC can induce tumor cell apoptosis and inhibit invasion. F3-PEG8-RiboTAC has anti-tumor activity and can be used in the research of tumors such as leukemia and triple-negative breast cancer.

BMS-344577 (Compound 22) is a potent and orally active factor Xa inhibitor (IC50 = 4 nM, EC2xPT = 7 μM). BMS-344577 shows potent CYP3A4 inhibition activity (IC50 = 0.3 μM). BMS-344577 can be used for the research of cardiovascular disease.

BT-O2C is a highly selective p300 PROTAC degrader. BT-O2C can significantly degrade the level of p300 in HAP1 cells. BT-O2C has significant cytotoxicity in CIC:DUX4 sarcoma (CDS) cell lines (IC50 ranges from 152 to 221 nM) and significantly reduces the expression of CDS target genes (ETV1, ETV4, ETV5). BT-O2C can be used for research on cancer.

GSK-3β inhibitor 27 (Compound 1c) is a reversible and competitive GSK-3β inhibitor with an IC50 value of 2.2 μM. GSK-3β inhibitor 27 inhibits tau hyperphosphorylation, reduces Aβ protein aggregation and possesses metal chelation and neuroprotective potential. GSK-3β inhibitor 27 is promising for research of neurodegenerative diseases (such as Alzheimer’s disease).

JW 618 is a selective ABHD6 inhibitor, with IC50s of 38 and 13 nM for mouse and rat ABHD6.

RPR 130737 is a selective, potent and competitive inhibitor for factor Xa with a Ki of 2.4 nM. RPR 130737 shows selectivity of more than 1000-fold over thrombin, activated protein C, plasmin, tissue-plasminogen activator and trypsin. RPR 130737 can prolong plasma activated partial thromboplastin time and prothrombin time. RPR 130737 shows no effect on platelet aggregation. RPR 130737 can be used for the research of cardiovascular disease, such as thrombosis.

WZH-17-002 is a WZH-15-125-based ALK PROTAC degrader with a DC50 of 25 nM. WZH-17-002 enhances activities against Lorlatinib-resistant ALK compound mutations. WZH-17-002 significantly reduces drug resistance in ALK-fusion non-small cell lung cancer (NSCLC) and inhibits tumor growth in EML4-ALK G1202R/L1196 M xenograft mice model.