ZPL-5212372 (PF 5212372) is a cPLA2α inhibitor (IC50 = 7 nM). ZPL-5212372 inhibits the release of prostaglandin D2 (PGD2), cysteyl leukotrienes, leukotriene B4, thromboxane A2, and PGD2 from human lung cells. ZPL-5212372 inhibits delayed bronchoconstriction and airway hyperresponsiveness in a sheep allergic inflammation model. ZPL-5212372 may be used in asthma research.

tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate is a PROTAC linker that can be used in the synthesis of PROTACs.

Renin-IN-4 is a Renin inhibitor. Renin-IN-4 can be used for the research of cardiovascular disease.

PU-11 is a Hsp90α/Hsp90β inhibitor with IC50 values of 18.6 μM and 89.8 μM and Kd values of 2 and 4.2 μM. PU-11 binds to the ATP-binding pocket of Hsp90α and Hsp90β and displays selective binding preference for Hsp90α over Hsp90β, mediated by the nonconserved Hsp90α Ser52 residue. PU-11 can be used for the research of neurodegenerative disorders.

PD-1/PD-L1-IN-61 is a PD-1/PD-L1 interaction inhibitor with a human IC50 of 5.3 nM. PD-1/PD-L1-IN-61 embeds into the hydrophobic pocket at the PD-L1 dimer interface, stabilizing binding through hydrogen bonds and π-π stacking with PD-L1 residues. PD-1/PD-L1-IN-61 acts as an immune activator, enhances immune-killing activity of peripheral blood mononuclear cells against cancer cells, restores T-cell immune function, and promotes IFN-γ secretion. PD-1/PD-L1-IN-61 can be used for the research of triple-negative breast cancer.

Nivimedone (BRL 10833 free base) is an orally active antiallergic agent. Nivimedone inhibits IgE-mediated passive cutaneous anaphylaxis in rats. Nivimedone suppresses antigen-induced histamine release from lung tissues passively sensitized with atopic serum. Nivimedone can be used in research related to bronchial asthma.

LY-73497 is a Phenethylthiazolythioureas derivative. LY-73497 has anti-HIV-1 activity.

LY3295668 (AK-01) erbumine is a highly specific and orally active inhibitor of Aurora-A kinase with a Ki values for AurA and AurB of 0.8 nM and 1038 nM respectively. LY3295668 erbumine can effectively inhibit the autophosphorylation of AurA, induce mitotic arrest and apoptosis. LY3295668 erbumine avoids the formation of polyploids related to AurB inhibition. LY3295668 erbumine can be used for the study of small cell lung cancer.

L-Kynurenine-5-F (Compound 2h) is the 5-F derivative of L-Kynurenine.

Lerimazoline is a selective 5-HT1D receptor agonist with Ki values of 72 and 3480 nM for h5-HT1D and h5-HT1B. Lerimazoline inhibits Forskolin-stimulated cAMP production and induces contractions in rabbit saphenous vein preparations. Lerimazoline can be used for the research of migraine.

INCB059872 TFA is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor. INCB059872 TFA can be used for the research of myeloid leukemia.

IDO1-IN-32 (Compound 45) is a potent and orally effective IDO1 inhibitor with an IC50 of 10 pM. IDO1-IN-32 exhibits significant anti-proliferative activity against Hela cells. IDO1-IN-32 can significantly inhibit tumor growth in CT26 and LCC transplanted mouse models by activating anti-tumor immunity. IDO1-IN-32 can be used for research on colon cancer and breast cancer.

HIF-1α-IN-10 is a ligands for target protein for PROTAC (HIF-1α). HIF-1α-IN-10 can be used to synthesize PROTAC HIF-1α degrader-2.

HER2-IN-23 is a selective HER2 inhibitor. HER2-IN-23 reduces in total HER2 expression rather than in phosphorylated HER2 (p-HER2). HER2-IN-23 reduces cyclin D1 level and stimulates PARP cleavage. HER2-IN-23 can be used for the study of HER2-positive breast cancer.

FLT3-IN-39 (Compound W4) is a selective FLT3 inhibitor, with an IC50 value of 16.0 nM against FLT3-ITD and an IC50 value of 20.4 nM against FLT3-D835Y. FLT3-IN-39 inhibits FLT3-ITD and FLT3-D835Y mutant kinases. FLT3-IN-39 induces G0/G1 cell cycle arrest and Apoptosis in cancer cells, and reduces intracellular ROS levels. FLT3-IN-39 exhibits anti-tumor activity against acute myeloid leukemia.

Fenaminstrobin (SYP-1620) is a strobilurin Fungicide. Fenaminstrobin binds to cytochrome bc1 in the mitochondrial respiratory chain, thereby inhibiting ATP production. Fenaminstrobin exhibits acute toxicity to Daphnia magna. Fenaminstrobin effectively controls diseases such as Fusarium ear rot, downy mildew, rice blast and pear scab.

CRBN ligand-895 (Compound 14) is an E3 ubiquitin ligase ligand for cereblon (CRBN), which is used to recruit the cereblon protein. CRBN ligand-895 can be used for the synthesis of PROTACs, such as PROTAC HDAC8 Degrader-4.

1-Olein-2-butyrin-3-palmitin is an acylglycerol.

(rel)-PRT062607 ((rel)-P505-15) is the relative configuration of PRT062607. PRT062607 is a highly selective inhibitor of Syk kinase, with an IC50 value of 1-2 nM, and is more than 80 times less potent against Fgr, Lyn, FAK, Pyk2, and Zap70.

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.

Vilanterol (GW642444) acetate is a long-acting β2 adrenergic receptor agonist. Vilanterol acetate has pEC50 values for β2-AR, β1-AR, and β3-AR of 9.4, 6.4, and 6.1, respectively. Vilanterol acetate selectively activates airway β2 adrenergic receptors, increases cAMP and thus relaxes bronchial smooth muscle. Vilanterol acetate can be used in asthma research[1][2].

LM-189, a G protein alpha subunit I (Gαi)-biased agonist, is a Gαi-biased ligand of β2-adrenergic receptor (β2AR). LM-189 stabilizes a distinct conformation in TM6 and increases the dynamics of ICL2. LM-189 can be used to develop the Gαi-biased β2AR agonists.

LM-189 free base, a G protein alpha subunit I (Gαi)-biased agonist, is a Gαi-biased ligand of β2-adrenergic receptor (β2AR). LM-189 free base stabilizes a distinct conformation in TM6 and increases the dynamics of ICL2. LM-189 free base can be used to develop the Gαi-biased β2AR agonists.

VUF26034 (Compound 12b) is a photoresponsive ligand for the human β2-adrenergic receptor (β2-AR.

ABT-866 is an α1A-adrenoceptor agonist and an antagonist at the α1B- and α1D-adrenoceptor subtypes. ABT-866 has an EC50 of 0.60 μM for the α1A in the rabbit urethra. ABT-866 has a pA2 value of 5.4 for the α1B in the rat spleen. ABT-866 has a pA2 value of 6.2 for the α1D in the rat aorta. ABT-866 exhibits good urethral selectivity and lower cardiovascular side effects in stress urinary incontinence models. ABT-866 can be used for the research of diseases such as stress urinary incontinence.

L742791 is a β3-AR agonist. L742791 elicits lipolytic response in isolated nonhuman primate adipocytes.

GG-818 is a potent and selective α1 adrenoceptor antagonist, with pKi values of 9.7 for α1a, 7.8 for α1b, and 7.6 for α1d. GG-818 can be used for benign prostatic hyperplasia research.

CGP 12177 ((±)-CGP 12177) is a β-Adrenergic receptor (β-AR) ligand. CGP 12177 is a β3-AR (Ki = 88 nM) agonist with β1/β2-AR (Ki = 0.9 nM for β1; Ki = 4 nM for β2) antagonist action. CGP 12177 exhibits partial agonist properties for α1-AR in rat pulmonary artery. CGP 12177 regulates the expression of ucp and leptin genes in NMRI mice adipose tissues. CGP 12177 can be used for cardiovascular and metabolic disease research[1][2][3][4].

DC-015 is a selective and orally active alpha 1-adrenoceptor antagonist on plasma lipid and vascular reactivity in hyperlipidaemic rodent model. DC-015 is a synthesized quinazoline derivative. DC-015 decreases mean arterial pressure in rats. DC-015 has antihypertensive activity.

L-657743 is a highly potent, highly selective, and orally active α2-adrenoceptor antagonist. L-657743 can be used in the research of neurological diseases such as depression.