Conophyllidine, a bisindole alkaloid, is a selective M2 polarization inhibitor. Conophyllidine inhibits histone acetylation by targeting the histone acetyltransferase domain of the P300/CBP proteins. Conophyllidine inhibits IL-4-induced arginase with an IC50 of 0.31 μM. Conophyllidine effectively induces a phenotypic switch in tumor-associated macrophages (TAMs) from an anti-inflammatory to an inflammatory type, thereby enhancing cytotoxic CD8+ T cell recruitment and functionality within the tumor microenvironment. Conophyllidine can be used for the study of TAMs.

FIP22 is a potent and selective IRAK4 PROTAC degrader (HEK293T cells: DC50 = 3.2 nM; THP-1 cells: DC50 = 10.6 nM). FIP22 induces the ubiquitin-proteasome system by forming an IRAK4-FIP22-CRBN ternary complex (EC50 = 12.63 nM), thereby potently blocking IRAK4-mediated NF-κB and MAPK signaling pathways. FIP22 can be used for the study of atopic dermatitis.

Allotrap 07 is a synthetic peptide composed of residues 75-84 of HLA-B7, a class I MHC molecule. Allotrap 07 combined with Cyclosporin A induces donor-specific tolerance in rat cardiac allografts, significantly prolonging graft survival.

MEN 10207 (acetate) is a selective antagonist of the NK-2 tachykinin receptor. MEN 10207 (acetate) induces tachykinin-induced contractions in rat bladder and guinea pig airways in vivo. MEN 10207 (acetate) inhibits [β-Ala 8 ]-NKA (4-10)-induced enhancement of bladder motility in anesthetized rats and [β-Ala 8 ]-NKA (4-10)-induced enhancement of bronchoconstriction in anesthetized guinea pigs.

XEN-2174 is a noradrenaline transporter (NET) inhibitor. XEN-2174 inhibits the reuptake of noradrenaline through non-competitive inhibition, increasing the concentration of noradrenaline in the synaptic cleft, thereby activating α2-adrenergic receptor at the spinal level and exerting analgesic effects. XEN-2174 exhibits long-lasting analgesic effects in models of neuropathic pain and postoperative pain in rats. XEN-2174 can be used in pain research.

FAP6-19 is a fibroblast activation protein (FAP) targeting radioligand with a Kd of 18.2 nM. FAP6-19 selectively delivers therapeutic radioactive nuclides (such as 177Lu) to the tumor site by targeting the overexpressed FAP protein in the tumor microenvironment, achieving precise killing of cancer cells while minimizing radiation damage to healthy tissues. FAP6-19 exhibits extremely high total cellular uptake and good intracellular retention ability in HT1080 cells. After being labeled with 111In, FAP6-19 produced extremely high tumor/kidney and tumor/liver dose ratios in the mouse model with 4T1 tumors. FAP6-19 can be used in the research of solid tumors expressing FAP.

TL033 is a drug-Linker conjugates for ADC. TL033 contains a linker and bioactive small molecule toxins. TL033 can conjugate with Sacituzumab antibody (anti Trop-2) for synthesizing BT001021. BT001021 has anti-cancer activities against various cancers, such as breast cancer, non-small cell lung cancer (NSCLC), gastric cancer.

TL033 TFA is a drug-Linker conjugates for ADC. TL033 TFA contains a linker and bioactive small molecule toxins. TL033 TFA can conjugate with Sacituzumab antibody (anti Trop-2) for synthesizing BT001021. BT001021 has anti-cancer activities against various cancers, such as breast cancer, non-small cell lung cancer (NSCLC), gastric cancer.

BPR-890 is a potent agonist of CB1. BPR-890 exhibits excellent CB2/1 selectivity and has in vivo efficacy in diet-induced obese mouse model.

1,3-Bis(isothiocyanatomethyl)benzene is a plant regulator. prevents the invasion of pathogens by inducing stomatal closure. 1,3-Bis(isothiocyanatomethyl)benzene significantly increases the levels of ROS and NO in guard cells. 1,3-Bis(isothiocyanatomethyl)benzene has shown significant control effects on grape downy mildew, cucumber downy mildew, and wheat leaf rust.

JLJ648 is a Gag-Pol dimerizer with antiviral activity. JLJ648 can inhibit HIV replication and induce infected cell pyroptosis. JLJ648 can be used for the research of infection, such as HIV (human immunodeficiency virus).

ORG-20241 is a PDE3/PDE4 dual inhibitor. ORG-20241 has a significant bronchodilator effect and completely prevents allergen induced airway hyperresponsiveness. ORG-20241 can significantly inhibit eosinophil infiltration at high concentrations. ORG-20241 can be used for research on asthma.

Org 30029 (hydrochloride) is a Ca2+ sensitizer with positive inotropic effect. Org 30029 (hydrochloride) can be used for the research of cardiovascular disease.

Hydroxylamine is a selective Monoamine oxidase (MAO) inhibitor used for inhibiting of platelet aggregation. Hydroxylamine is a intermediate of nitrogen cycle in aerobic ammonium oxidizers microorganisms, such as ammonium oxidizing bacteria (AOB), ammonium oxidizing archaea (AOA) and complete ammonium oxidizing bacteria (comammox). Hydroxylamine impacts NO and N2O emissions by aerobic ammonium oxidizers microorganisms and inhibits nitrite oxidizing bacteria (NOB) activity.

Trimelamol (CB10-375; NSC283162) is a highly efficient acid-catalyzed DNA interstrand crosslinker with low neurotoxicity due to its limited BBB penetration. Trimelamol exhibits anti-tumor activity and overcomes platinum resistance. Trimelamol is investigated for lung and ovarian cancer research[1][2][3][4][5].

PEG3-amide-C2-COOH is a PROTAC linker that can be used in the synthesis of PROTACs, such as BCL6 PROTAC 1.

Aurora kinase ligand-1 (Compound I-4) is an Aurora kinase B (AURKB) PROTAC ligand. Aurora kinase ligand-1 can be conjugated with E3 ligase Ligand and linker to synthesize AURKB PROTAC degrader MS44. MS44 can be used for cancer research.

YTK-1305 is a p62 ligand compound that promotes cellular autophagy.

DBM-819 is a reversible inhibitor of H⁺/K⁺-ATPase (H+/K+-ATPase), with an IC50 value of 5 μM. DBM-819 can reversibly block gastric acid secretion by inhibiting the proton pump in the gastric mucosa. It shows significant protective effects against duodenal ulcers induced by Cysteamine, gastric ulcers induced by Indomethacin, and gastric ulcers induced by Aspirin, with EC50 values of 6, 3.1, and 4 mg/kg respectively. DBM-819 can be used in ulcer prevention research.

4-Piperidineethanol-piperidine-Boc is a PROTAC linker can be used in the synthesis of PROTAC BRD4 Degrader-31.

IRAK4 ligand-14 is a ligand for IRAK4. IRAK4 ligand-14 can be used for synthesizing PROTACs such as APH02174.

APH02174 is a highly selective and orally active IRAK4 PROTAC degrader with the DC50 of 4.01 nM in THP-1 cells. APH02174 blocks inflammatory signals by inhibiting IL-6 release. APH02174 can be used for research on inflammatory conditions such as psoriasis vulgaris and rheumatoid arthritis.

BJH-60 is a mitochondrial complex 1 inhibitor. BJH-60 can inhibit mitochondrial oxygen consumption rate with an IC50 of 1.9 μM in A549 cells. BJH-60 shows no PDE inhibitory effect. BJH-60 can be used for the research of cancer, such as breast cancer.

KI-TOX-A3 is a selective protein-protein interaction (PPI) inhibitor targeting TOX protein (with an IC50 value of 0.51 μM for TOX-KAT7 interaction). KI-TOX-A3 induces proteasomal degradation of TOX, restores KAT7-mediated H3K14 acetylation, reversing CD8+ T cell exhaustion and inhibiting T-cell acute lymphoblastic leukemia (T-ALL) cell proliferation. KI-TOX-A3 is promising for research of hematological tumors (e.g., T-ALL).

PAB-(PEG4-Me)-Cit-Val-PEG2-amide-C2-MC is an ADC linker that can be combined with the TLR7/8 agonist for the synthesis of a linker-payload conjugate.

E3 Ligase Ligand-linker Conjugate 193 is an E3 ligase ligand-linker conjugate that incorporates the VHL Ligase Ligand and linker. E3 Ligase Ligand-linker Conjugate 193 can be used for synthesis of PROTAC pan-KRAS degrader-1

Alkyne-pyrazine-O-piperidine-(1-methylcyclopropyl) methanol is a PROTAC linker that can be used in the synthesis of PROTACs, such as PROTAC pan-KRAS degrader-1.

(Rac)-EBET-1055 is the racemate of EBET-1055. EBET-1055 is a bromodomain and extra-terminal (BET) PROTAC degrader. EBET-1055 effectively inhibits the growth of pancreatic ductal adenocarcinoma (PDAC). EBET-1055 also simultaneously modulates cancer-associated fibroblast (CAF) activity, upregulating all reporter gene activities in organoid co-cultures.

pro-FTY, a FTY720 anticancer prodrug, is a sphingosine-1-phosphate (S1P) inhibitor. pro-FTY specifically inhibits S1P signaling in cancer cells using a drug delivery system (DDS) that reacts with acrolein. pro-FTY significantly inhibits the survival of breast cancer cells, including multidrug-resistant cells and its organoids resistant to Paclitaxel or Doxorubicin. pro-FTY potently suppresses tumor growth in 4T1 cells or organoids xenograft tumors mice model while avoiding lymphocytopenia.

(R)-thioxo-Dxd is a Camptothecin derivative. (R)-thioxo-Dxd can be connected to monoclonal antibodies via linkers to form antibody-drug conjugate (ADC) molecules. (R)-thioxo-Dxd can be used for research on tumors with high HER2 or TROP2 expression.