Parsaclisib (INCB050465) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib can be used for the research of relapsed or refractory B-cell malignancies.

Potent Allosteric Agonist-Positive Allosteric Modulator of α7 Nicotinic Acetylcholine Receptors

preQ1 is a precursor in the biosynthesis of queuosine, a bacterial nucleoside incorporated into tRNA by tRNA transglycosylase. preQ1 binds to an aptamer domain on tRNA that acts as a riboswitch to repress gene expression.

Sacubitril, also known as AHU377, is angiotensin receptor neprilysin inhibitor being studied for use in combination with valsartan for heart failure. Sacubitril is a prodrug that is activated to LBQ657 by de-ethylation via esterases. LBQ657 inhibits the e

Zabedosertib (BAY 1834845) is a IRAK4 inhibitor with immunomodulatory potential. IRAK4 is a protein kinase involved in signaling innate immune responses from Toll-like receptors.

GO289 (GO-289, GO 289) is a potent and selective inhibitor of casein kinase 2 (CK2) with IC50 of 7 nM in in vitro kinase assays, shows minor effects on CKIδ and CKIα activity in vitro.

Cyclo(Gly-Gln) is a cyclic dipeptide.

ANR-94 is a potent and selective adenosine A2A receptor (AA2AR) antagonist with an Ki of 46 nM for hAA2AR. ANR 94 has the potential for the research of Parkinson's disease.

SP-8356, an anti-inflammatory synthetic verbenone derivative, is a potent, orally active cluster of differentiation 147 (CD147) inhibitor. SP-8356 inhibits CD147-cyclophilin A (CypA) interaction and reduces MMP-9 activity. SP-8356 exerts anti-breast cancer effects by inhibiting NF-κB signaling. Anti-atherosclerotic effects[1][2][3].

Aficamten (CK-274) is a novel cardiac myosin inhibitor with an IC50 of 1.4 μM. Aficamten can be used for the research of hypertrophic cardiomyopathy (HCM).

H-7 is a specific protein kinase C inhibitor, which inhibits superoxide release from human neutrophils (PMN) stimulated with phorbol myristate acetate or synthetic diacylglycerol.

STD-101-D1 is a novel brain permeable, G protein-biased beta-1 adrenergic receptor (ADRB1) partial agonist with EC50 of 16.9 nM.

FN1-8 is a novel, synthetic small molecule that efficiently interferes with Gli/TAF9 interaction and downregulate Gli/TAF9-dependent transcriptional activity (at 15 uM); inhibits non-canonical Gli activation and acts downstream of the canonical Hh pathway; suppresses cancer cell proliferation in vitro and inhibits tumor growth in vivo.

UDP-GalNAz disodium (UDP-N-azidoacetylgalactosamine disodium) is the analogue of UDP-GalNAc. UDP-GalNAc is the donor substrate of many N-acetylgalactosaminyltransferases, enzymes which transfer GalNAc from the nucleotide sugar to a saccharide or peptide acceptor.

KAR-5585 (Rodatristat) is the prodrug of the potent TPH1 inhibitor KAR5417, shows robust reduction of intestinal serotonin (5-HT) levels in mice.

MCUF-651 (MCUF651) is a small molecule guanylyl cyclase A receptor (GC-A) positive allosteric modulator (PAM), potentiate ANP-mediated cGMP with EC50 of 0.45 uM (Emax=82%) in HEK293 GC-A cells.MCUF-651 enhanced ANP-mediated cGMP generation in human cardiac, renal, and fat cells and inhibited cardiomyocyte hypertrophy in vitro.MCUF-651 binds to GC-A (Kd=397 nM) and selectively enhances the binding of ANP to GC-A ( MCUF-651+ANP, Kd=0.06 nM).MCUF-651 is orally bioavailable in mice and enhances the ability of endogenous ANP and BNP to generate GC-A-mediated cGMP ex vivo.

GPS167 is a specific small molecule splicing regulator SRSF10 inhibitor, modulates BCLAF1 splicing with IC50 of 2 uM in human colorectal HCT116 cells, directly inhibits CLK1, CLK2 and CLK4, but not SRPK1 and DYRK1A.GPS167 promotes the dephoshorylation of SRSF10 and changes its interaction with partner proteins.GPS167 treatment leads to a partial dephosphorylation of SRSF10 and increases the recovery of CLK1 and CLK4.GPS167 impairs the growth of cancer cell line, elicits p53-dependent cytotoxicity.GPS167 is cytotoxic for human colorectal cancer organoids but not normal organoids.

QC-01-175 is a hetero-bifunctional molecule designed to engage both tau and Cereblon (CRBN) to trigger tau ubiquitination and proteasomal degradation (tau PROTAC).QC-01–175 effected clearance of tau in frontotemporal dementia (FTD) patient-derived neuronal cell models, with minimal effect on tau from neurons of healthy controls.QC-01–175 also rescued stress vulnerability in FTD neurons, phenocopying CRISPR-mediated MAPT-knockout.

Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.

Epitalon is an anti-aging agent and a telomerase activator. Epitalon has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon can be used for cancer, old age and Retinitis Pigmentosa.

DS-9300 is a potent, orally active, selective EP300/CBP HAT inhibitor with an IC50 value of 28 nM. DS-9300 has anticancer activity and can be used in prostate cancer disease research.

AZD0095 is a selective and orally active MCT4 inhibitor (IC50: 1.3 nM). AZD0095 effectively inhibits the tumor growth in NCI-H358 xenograft in combination with Cediranib.

BAY-747 (BAY747) is a novel potent, selective, brain-penetrant soluble guanylate cyclase (sGC) stimulator.

BT173 is a small molecule allosteric inhibitor of HIPK2-Smad3 interaction, specifically inhibits the TGF-β1/Smad3 pathway.BT173 disrupts HIPK2-Smad3 protein-protein interaction (PPI) without significant inhibition of HIPK2 kinase activity or inhibition of p53 activation.BT173 inhibits Smad3 phosphorylation in human kidney cells in vitro.BT173 significantly attenuated renal fibrosis development in the UUO mice, significantly decreased Smad3 phosphorylation and α-SMA expression in the UUO kidneys.Treatment of BT173 ameliorated kidney fibrosis in Tg26 mice.

ADU-S100 (MIW815) is a synthetic cyclic dinucleotide agonist of STING, elicits potent and durable anti-tumor immunity when administered IT in pre-clinical syngeneic tumor models..

BMS-820132 (BMS 820132) is potent, selective, partial glucokinase (GK) activator with AC50 of 29 nM.

AZD4625 is a potent, selective, covalent allosteric inhibitor of mutant GTPase KRAS G12C with IC50 of 3 nM, inhibitor H358 cell proliferation with GI50 of 4 nM.AZD4625 is a clinical development candidate for the treatment of KRASG12C positive tumors.

JBJ-09-063 is a potent, mutant-selective allosteric EGFR inhibitor against EGFR L858R, T790M and C797S mutations, with IC50 of <0.1 nM for recombinant EGFR L858R/T790M kinase domain.

MIF-IN-1 (compound 14) is a potent macrophage migration inhibitory factor (MIF) inhibitor (pIC50=6.87).

BuChE-IN-1 (Compound 23) is a potent inhibitor of butyrylcholinesterase (BuChE). Butyrylcholinesterase (BuChE) is recently regarded as a biomarker in progressed Alzheimer’s disease (AD).