Ionizable Lipid Products

WP-1122(WP 1122) is a candidate drug to treat SARS-COV-2(COVID-19) .2-DG completely prevented SARS-CoV–2 replication in Caco–2 cells. Glycolysis is a process by which cells convert glucose into energy and infected (host) cells are induced by viruses to dramatically increase their dependence on glycolysis. WP1122 is a prodrug of 2-DG whereby chemical elements are added to 2-DG to improve its delivery in vivo.

AFN-1252(Debio 1452) is a potent inhibitor of enoyl-acyl carrier protein reductase (FabI), inhibited all clinical isolates of Staphylococcus aureus and Staphylococcus epidermidis at concentrations of ≤0.12 μg/ml. IC50 value:Target: Antibiotic agentAFN-1252 was inactive (MIC90, >4 μg/ml) against clinical isolates of Streptococcus pneumoniae, beta-hemolytic streptococci, Enterococcus spp., Enterobacteriaceae, nonfermentative gram-negative bacilli, and Moraxella catarrhalis. These data support the continued development of AFN-1252 for the treatment of patients with resistant staphylococcal infections.

BRD7586 is a cell-permeable small molecule inhibitor of SpCas9 with EC50 of 6.2  µM and 5.7  µM in the eGFP-disruption and HiBiT-knock-in assays, respectively. BRD7586 specifically engages SpCas9 but not Cas12a in cells and enhances SpCas9 specificity at multiple loci.

Sebetralstat is a plasma kallikrein inhibitor (WO2016083820). Sebetralstat can be used for the research of metabolic diseases.

2OH-BNPP1 is an inhibitor of BUB1 kinase, a Ser/Thr kinase, used for the treatment of cancer.

AnCoA4 (AnCoA-4, AnCoA 4) is a potent Orai1 channel inhibitor that inhibits store-operated calcium (SOC) with EC50 of 0.88 uM; binds to the C terminus of Orai1, directly inhibits calcium influx through the channel and also reduces binding of STIM1; decreased gene expression involved in T cell activation, including IL2, CD27, NFATC1, TNF, TBX21, CSF, ICOS, and CXCR3; effectively blocks T cell activation in vitro and in vivo.

Anamorelin is a novel ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay.

FX-909（FX 909） is a first-in-class inverse agonist of the peroxisome proliferator-activated receptor gamma (PPARG) lineage transcription factor with EC50 of 1 nM and shows >2000-fold selectivity for PPARG over PPARA/PPARD - acting through a mechanism that promotes a repressive conformation of PPARG.

GPR65 agonist (BTB09089) is a novel GPR65 agonist.

SB02024 is a novel highly potent, selective, ATP competitive, orally active inhibitor of vacuolar protein sorting 34 (Vps34) with Kd of 1 nM, >1000 times selective towards other PI3K isoenzymes; SB02024 is also highly selective at 1 uM in the DiscoveRx ScanMax panel of 468 kinases; reduces the number of GFP-2xFYVE puncta with IC50 of 14 nM, induces a dose-dependent increase in levels of NCOA4 and p62; blocks autophagy in vitro and reduces xenograft growth of two breast cancer cell lines, MDA-MB-231 and MCF-7; also significantly potentiates cytotoxicity of Sunitinib and Erlotinib in MCF-7 and MDA-MB-231 in vitro.

LDC203974(IMT1B) is a highly specific inhibitor of human mitochondrial RNA polymerase (POLRMT) with improved pharmacokinetic profiles than LDC195943(IMT1).

AZD-5069 is a potent CXCR2 chemokine receptor antagonist, used for caner treatment.

CC-90010 (compound 1) is a reversible and orally active BET inhibitor. CC-90010 is applied in the study for advanced solid tumors

Nalfurafine (TRK-820) is a potent selective and orally active G protein-biased kappa opioid receptor (KOR)-agonist with high translational potential[1]. Nalfurafine (TRK-820) enhances the therapeutic potential of MOR-targeting analgesics, has the potential for uremic pruritis treatment[2].

Palmitoyl hexapeptide-12 is a bioactive peptide with anti-aging effect and has been reported used as a cosmetic ingredient.

NMS-1286937 is a potent, selective and orally available PLK1 inhibitor, with an IC50 of 2 nM.

A non-selective agonist of the dopamine D3 receptor (Ki=0.71 nM); has 10-fold selectivity for the D3 receptor over the D2, D4, and D5 receptors and 100-fold selectivity for the D3 receptor over the D1 receptor; behaves as a full agonist of D1, D2, and D3 with similar potencies (EC50) in functional assay; also demonstrates significant affinity at α-adrenergic (α2B, Ki=27 nM) and serotonin receptors (5-HT1A Ki=30 nM); significantly attenuates MPTP-induced acute cell degeneration in mouse model.Parkinson's DiseaseApproved

AMG-548 is a potent, oral and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γand p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) [1]. AMG-548 inhibits Wnt signaling by direcly inhibing Casein kinase 1 isoforms δ and ε[2].

ARV-766 is an orally active and potent proteolysis targeting chimera (PROTAC) protein degrader. ARV-766 degrades wild-type androgen receptor (AR) but also relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations[1].

BAY1125976 is a selective allosteric Akt1/Akt2 inhibitor; inhibits Akt1 and Akt2 activity with IC50 values of 5.2 nM and 18 nM at 10 μM ATP, respectively.