AZ-23 is an ATP-competitive and orally bioavailable Trk kinase A/B/C inhibitor with IC50s of 2 nM (TrkA), 8 nM (TrkB), 24 nM (FGFR1), 52 nM (Flt3), 55 nM (Ret), 84 nM (MuSk), 99 nM (Lck), respectively.
9-Phenanthrol (9-Hydroxyphenanthrene) is a potent and selective human TRPM4 inhibitor, with an IC50 of 20 μM. 9-Phenanthrol can be used for the research of ischemia-reperfusion injury[1][2].
Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
Falcipain-2/3-IN-2 (Compound 12) is a dual falcipain-2 and falcipain-3 inhibitor[1].
SN-011 is a potent and selective mouse and human STING inhibitor, with an IC50 of 76 nM for STING signaling. SN-011 competes with cyclic dinucleotide (CDN) for the binding pocket of the STING dimer, blocking CDN binding and STING activation. SN-011 can be used for the research of STING-driven autoimmune and inflammatory disease[1].
Mal-PFP ester is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Kainic acid hydrate is a potent excitotoxic agent. Kainic acid hydrate also is an agonist for a subtype of ionotropic glutamate receptor. Kainic acid hydrate induces seizures[1][2].
CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, Kds are 1.1 nM (BRD2 BD1), 0.6 nM (BRD2 BD2), 0.52 nM (BRD3 BD1), 0.49 nM (BRD3 BD2), 0.8 nM (BRD4 BD2), 2 nM (BRDT BD1), 2.1 nM (BRDT BD2), 47 nM (CREBBP), 570 nM (CECR2), 110 nM (EP300), respectively, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo[1].
Pheniprazine is a potent and long acting inhibitor of monoamine oxidase. Pheniprazine has the potential for the research of depression[1].
(4S)-10-Nor-calamenen-10-one (Compound 15) enhances LPS-induced NO production by microglia. (4S)-10-Nor-calamenen-10-one is an eudesmane sesquiterpene that can be isolated from Alpinia oxyphylla[1].
m-PEG9-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
p38 MAPK-IN-2 is an inhibitor of p38 kinase.
Fmoc-NH-PEG10-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Colistin is a polypeptide antibiotic which inhibits gram-negative bacteria by binding to lipopolysaccharides and phospholipids in the outer cell membrane of gram-negative bacteria.
Diacetolol D7 is a deuterium labeled Diacetolol. Diacetolol is the major metabolite of Acebutolol. Diacetolol is a β-adrenoceptor blocking and anti-arrhythmic agent[1].
Triflumezopyrim, a mesoionic insecticide, has high efficiency at a low dosage, and is mainly used to control hopper species. Triflumezopyrim mainly acts on the nicotinic acetylcholine receptor (nAChR) inhibition, which is very highly 44 efficient, rapidly effective, and nearly nontoxic to nontarget arthropods[1].
Abemaciclib Metabolites M2 is a metabolite of abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s in the range of 1-3 nM. Anti-cancer activity[1].
Br-PEG4-C2-Boc is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
GNF-7 inhibits Bcr-Abl WT and Bcr-Abl T315I with IC50 of 133 nM and 61 nM, respectively. IC50 value: 133 nM (Bcr-Abl WT), 61 nM (Bcr-Abl T315I)Target: Bcr-Ablin vitro: GNF-7 is amongst the first type II inhibitors capable of inhibiting T315I to be described and will serve as a valuable lead to design next generation Bcr-Abl kinase inhibitors. GNF-7 exhibits some selectivity (4 to 100-fold) for T315I Bcr-Abl (IC50 = 11 nM, in Ba/F3 cell line) relative to kinases such as TPR-Met, NPM-ALK, JAK-3, Flt-3. in vivo: GNF-7 displays significant efficacy against T315I-Bcr-Abl without appreciable toxicity in a bioluminescent xenograft mouse model using a transformed T315I-Bcr-Abl-Ba/F3 cell line that has a stable luciferase expression. GNF-7 exhibits excellent pharmacokinetic parameters in mice, with good systemic exposure (AUC = 26656 hrs*nM, Cmax = 3.6 uM) along with reasonable half life (t1/2=3.2 hrs) and favorable oral bioavailability (BAV=36%) being observed following oral administration of a single dose of 20 mg/kg.
Rhamnose monohydrate (L-Rhamnose monohydrate) is a monosaccharide found in plants and bacteria. Rhamnose monohydrate-conjugated immunogens is used in immunotherapies[1]. Rhamnose monohydrate crosses the epithelia via the transcellular pathway and acts as a marker of intestinal absorption[2].
Aloisine RP106 (compound 38) is a potent inhibitor of Cdk1/cyclin B, Cdk5/p25, and GSK3 with IC50s of 0.70µM, 1.5µM, 0.92 µM, respectively[1].
Amino-PEG5-amine is a PEG-based (5 units) PROTAC linker can be used in the synthesis of PROTACs.
IMP-1088 is a potent, selective human N-myristoyltransferase with IC50 of less than 1 nM for both HsNMT1 and HsNMT2, inhibits Rhinoviruses (RVs) capsid myristoylation in cells; pharmacological and rapidly inhibits host-cell N-myristoylation, potently and efficiently block RV replication (IC50=17 nM) without cytotoxicity; potently blocks a key step in viral capsid assembly, to deliver a low nanomolar antiviral activity against multiple RV strains, poliovirus and foot and-mouth disease virus, and protection of cells against virus-induced killing.
(S)-3-Aminopiperidine-2,6-dione-d hydrochloride is the deuterium labeled (S)-3-Aminopiperidine-2,6-dione hydrochloride[1].
Bobcat339 (Bobcat 339) is a novel cytosine-based TET enzyme inhibitor with IC50 of 33 uM (TET1) and 73 uM (TET2), but not DNMT3a, does not inhibit the DNA methyltransferase DNMT3a; Bobcat339 is a useful tool for investigation of epigenetics and serve as a starting point for new therapeutics that target DNA methylation and gene transcription.
SKF96067 is a reversible inhibitor of the gastric H+/K+-ATPase.
I-SAP is a radioiodinated TXA2/PGH2 receptor antagonist. The bind between I-SAP and the receptors, is inhibited by the histidine modifying reagent diethyl-pyrocarbonate (DEPC)[1][2].
Lorundrostat is a aldosterone synthase inhibitor[1].
c-Kit-IN-5 is potent inhibitor of c-Kit, with IC50s of 22 nM and 16 nM in kinase assay and cell assay, respectively. c-Kit-IN-5 shows more than 200-fold selectivity for c-Kit over KDR, p38, Lck, and Src. c-Kit-IN-5 also exhibits desirable pharmacokinetic properties[1].
THP-SS-PEG1-Tos is a cleavable 1 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].