Ionizable Lipid Products

JNK-IN-8 is a potent JNK inhibitor with IC50s of 4.7 nM, 18.7 nM, and 1 nM for JNK1, JNK2, and JNK3, respectively.

GW2580 is an orally bioavailable inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM.

MI-2 is a Menin-MLL interaction inhibitor with IC50 of 446±28 nM.

Camostat Mesylate(FOY305; FOY-S980) is a trypsin-like protease inhibitor.Camostat mesilate (500 mM) inhibits generation of TGF-beta by suppressing plasmin activity and reduces the activity of TGF-beta, which blocks in vitro activation of HSCs [1]. Camostat mesilate (20 mM) combined with insulin results a significant hypoglycemic effect following large intestinal administration. Camostat mesilate (20 mM) is effective in reducing insulin degradation in both small and large intestinal homogenates of rats [2]. Camostat mesilate (2 mM) inhibits MCP-1 and TNF- production in activated rat monocytes. Camostat mesilate (2 mM) inhibits proliferation and MCP-1 production of cultured rat PSCs. Camostat mesilate (1 mg/g) prevents pancreatic atrophy and improves pancreatic exocrine function of rat chronic pancreatitis induced by DBTC. Camostat mesilate (1 mg/g) inhibits chronic inflammation and pancreatic fibrosis induced by DBTC. Camostat mesilate (1 mg/g) inhibits the development of pancreatic fibrosis and PSCs activation in the pancreas induced by DBTC. Camostat mesilate (1 mg/g) suppresses monocytes infiltration and inhibits MCP-1 expression both in serum and in pancreatic tissue [3].

SBP1(spike-binding peptide 1) is a first-in-class peptide binder to the SARS-CoV-2 spike protein. SBP1 specifically binds SARS-CoV-2-RBD with low nanomolar affinity. SBP1 to the RBD was determined to be 47 nM with the average Kon = 4.69*104M-1S-1 and Koff

Arbidol (Umifenovir) hydrochloride is an broad-spectrum antiviral chemical agent which can inhibit cell entry of enveloped viruses by blocking viral fusion with host cell membrane

Neratinib is an orally available, irreversible tyrosine kinase inhibitor with IC50s of 59 nM and 92 nM for HER2 and EGFR, respectively.

MYF-03-176 is an orally active and potent anticancer agent. MYF-03-176 shows strong antitumor efficacy in MPM mouse xenograft model via oral administration[1].

NAB-14 is a potent, selective negative allosteric modulator of GluN2C/2D-containing NMDA receptors with IC50 of 580 nM, >800-fold selective over GluN2A/GluN2 receptors; inhibits triheteromeric (GluN1/GluN2A/GluN2C) NMDARs with modestly reduced potency and efficacy compared to diheteromeric (GluN1/GluN2C/GluN2C) receptors; inhibits GluN2D-mediated synaptic currents in rat subthalamic neurons and mouse hippocampal interneurons, but has no effect on synaptic transmission in hippocampal pyramidal neurons.

Tianeptine sodium salt is a selective facilitator of 5-HT uptake in vitro and in vivo.Tianeptine has no affinity for a wide range of receptors, including 5-HT and dopamine (IC50 > 10 μM) and has no effect on noradrenalin or dopamine uptake. Antidepressant, analgesic and neuroprotective following systemic administration in vivo.

ML 086 is a potent, specific inhibitor of phosphatase PHOSPHO1 with IC50 of 139 nM, with no activity against TNAP (IC50>100 uM); a useful chemical tool to examine the functional role of this enzyme in skeletal mineralization and soft tissue ossification abnormalities.

A potent, specific, competitive inhibitor of choline kinase-α (Chok-α) by targeting the choline binding site; significantly increases LC3II expression in MCF-7 and MCF-7/TAM cells, increases the size and number of autophagosome, causes MCF-7 and MCF-7/TAM cells to a slight increase in p62; suppresses MAPK and PI3K/AKT signaling, disrupts actin cytoskeletal organization, and reduces plasma membrane ruffling; significantly decreases tumor growth in a lung tumor xenograft mouse model, suppresses tumor phosphocholine, and diminishes activating phosphorylations of ERK and AKT in vivo.

MsbA inhibitor 1 is a novel small molecule lipopolysaccharide biogenesis inhibitor, inhibits MsbA, an ATP-dependent flippase that translocates LPS across the inner membrane; causes mislocalization of LPS to the cell interior, inhibits Δ5 strain with MIC of 0.2 ug/ml.

NUC-3373 is a phosphoramidate-based prodrug of the monophosphate form of 5-fluoro-2'-deoxyuridine, the active metabolite of fluorouracil,an antimetabolite fluoropyrimidine analog of the pyrimidine nucleoside, with potential antineoplastic activity.

Thiacetazone (Thioacetazone) is a thiourea-containing antitubercular agent and is an orally active antibiotic. Thiacetazone has antibacterial action, which inhibits growth of Mycobacterium tuberculosis H37Rv with a MIC value of 0.1 μg/mL[1].

Ciprofloxacin is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.

UU-T03 is the ethyl ester derivative of UU-T02, which is a potent, selective inhibitor of β-catenin/Tcf4 interaction with Ki of 1.36 uM; exhibits growth inhibition of SW480 cells with IC50 of 10.77 uM; downregulates the transcription of AXIN2, LGR5, cyclin D1, and c-Myc in dose-dependent manners in SW480 cells.

PSI-6130 is a potent and selective inhibitor of HCV NS5B polymerase, and inhibits HCV replication with a mean IC50 of 0.6 μM.

LDC195943(IMT1) is a highly specific inhibitor of human mitochondrial RNA polymerase (POLRMT).

BC1618 is a novel Fbxo48 inhibitor and prevent pAmpkα degradation with MEC (minimal efficacious concentration) of 0.6 μM.