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.

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.

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.

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.

E913 is a CCR5 antagonist that competes with the binding of antibodies to CCR5 which recognize the C-terminal half of the second extracellular loop (ECL2B) of CCR5. E913 can specifically block the binding of macrophage inflammatory protein-1alpha (MIP-1alpha) to CCR5 (IC50 = 0.002 μM) and MIP-1alpha-elicited cellular Ca2+ mobilization (IC50 = 0.02 μM). E913 inhibits the replication of laboratory and primary R5 HIV-1 strains as well as various multidrug-resistant monocyte/macrophage tropic (R5) HIV-1 (IC50 = 0.03-0.06 μM). E913 can be used for the research of infection, such as HIV-1 infection.

FE100726 (Compound 39) is a Cholecystokinin 2 (CCK2) receptor agonist. FE100726 has a superior binding capacity on CCK2 receptor. FE100726 can induce gastric acid secretion in anaesthetized rat models. FE100726 can be used for diabetes research.

ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC50 = 15.2 nM, Ki =1.5 nM) and potent GSK-3β inhibitor activity (IC50 = 19.3 nM). ARN25657 exhibits excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. ARN25657 inhibits P-glycoprotein (P-gP)-mediated acetoxymethyl calcein efflux and improves in vitro ADME properties while maintaining a balanced dual-target profile. ARN25657 is useful for studying bipolar disorder and related neuropsychiatric disorders.

Aurora kinase inhibitor-14 (Compound 79) is an orally active and highly selective inhibitor of Aurora kinases with IC50 values of 0.5 nM and 1.2 nM for Aurora A and Aurora B, respectively. Aurora kinase inhibitor-14 binds to the ATP-binding site of Aurora kinases to block chromosome segregation during mitosis and induce apoptosis in tumor cells. Aurora kinase inhibitor-14 is promising for research of various solid tumors and hematological malignancies, such as non-small cell lung cancer, breast cancer, and acute myeloid leukemia.

MNFA is a derivative of Monofluoroacetic acid. MNFA is an effective pesticide.

KD-027 (SLx-2101) is a Phosphodiesterase 5 (PDE5) inhibitor. KD-027 can be used for endothelial dysfunction, and hypertension research.

AHN 070 is an irreversible peripheral benzodiazepine receptor (PBR) ligand. AHN 070 can bind to PBR with nanomolar affinity and is pH-dependent. AHN 070 can be used for studying the structure and function of PBR.

MK-8389 is an orally active LMW allosteric FSH receptor agonist. MK-8389 affects thyroid function.

DNK-333 is a potent and balanced dual NK1 and NK2 receptor antagonist with IC50 values of 4.8 nM and 5.5 nM, respectively. DNK-333 blocks the Neurokinin A (NKA)-induced bronchoconstriction in asthma.

TKA-731 is an NK1 receptor antagonist. TKA-731 can reverse mechanical hyperalgesia. TKA-731 can be used for research on neuropathic pain.

FKBP12 ligand-3 (compound dj) is a high-affinity ligand targeting FKBP12. FKBP12 ligand-3 can be used to selectively enhance the binding of heterobifunctional molecules to BRD4, enriching the drug intracellularly through the "CellTrap" effect to form a ternary complex of FKBP12-ligand-BRD4. This ternary complex has inhibitory activity against BRD4, thereby inhibiting the expression of BRD4 target genes (such as MYC) and inducing tumor cell death. FKBP12 ligand-3 can be used for selective cancer research based on differences in intracellular presenter protein levels.

EGFR ligand-14-PEG3-Boc contains EGFR ligand and linker. EGFR ligand-14-PEG3-Boc can be used for the synthesis of SJF-1521.

4-DTM-phenoxy-PEG4-CH2COOH (Formula 3) is a cleavable PEG-based ADC linker that can be used in the synthesis of antibody-drug conjugates (ADCs).

Di(4-morpholine-amide)-4-DTM-phenoxy(3,5-F)-PEG4-CH2COOH (compound BL) is a cleavable PEG-based ADC linker that can be used in the synthesis of antibody-drug conjugates (ADCs).

TBK1 ligand 2-C-O-C4-O-C3-O-C-amide is a conjugate of TBK1 ligand and linker, which can be used in the synthesis of PROTAC TBK1 degrader-2.

PROTAC BRD4 ligand-1-NH-PEG-phenol-PEG-COOtBu is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for BRD4 and a PROTAC linker. PROTAC BRD4 ligand-1-NH-PEG-phenol-PEG-COOtBu can be used for synthesis of PROTAC BRD4 Degrader-14.