Plazomicin (ACHN490; ACHN-490; Trade name: Zemdri) is a next-generation aminoglycoside antibacterial derived from sisomicin by appending a hydroxy-aminobutyric acid (HABA) substituent at position 1 and a hydroxyethyl substituent at position 6′. In June 2018, Plazomicin gained FDA approval to treat adults with complicated urinary tract infections. Plazomicin has been reported to demonstrate in vitro synergistic […]

Falnidamol (formerly known as BIBX 1382) is a potent and selective inhibitor EGFR inhibitor with IC50 of 3 nM and potential anticancer activities; it displays > 1000-fold lower potency against ErbB2 (IC50 = 3.4 μM) and a range of other related tyrosine kinases (IC50 > 10 μM). BIBX1382 and BIBU1361 are both potent and selective […]

Miridesap (formerly known as CPHPC; Ro63-8695; GSK-2315698) is a novel proline-derived small molecule ligand for serum amyloid P component (SAP). It is able to strip amyloid P from deposits by reducing levels of circulating serum amyloid P. It is an anticancer agent which depletes circulating serum amyloid P component (SAP) almost completely but leaves some […]

Resibufogenin (also known as Bufogenin; Recibufogenin; RBG), a component of huachansu, is a natural product with the potential for the treatment of pancreatic cancer. It has been shown to exhibit the anti-proliferative effect against cancer cells, and this may be attributed to the degradation of cyclin D1 caused by the activation of GSK-3β.

CEP-1347 (also known as KT7515), a derivative of the natural product K-252a found in broths of Narcodiopsis bacterium, is a novel, potent and mixed lineage kinase inhibitor (mainly JNK) with IC50 of 30 nM on JNK1. It demonstrates neuroprotective properties and has the potential for the treatment of neurodegenerative diseases such as PD. CEP-1347 promotes […]

Laduviglusib (CHIR-99021; CHIR99021) 2HCl, the dihydrochloride of CHIR-99021, is a potent and selective inhibitor of glycogen synthase kinase 3α/β (GSK-3α/β) with IC50s of 10 nM and 6.7 nM, respectively. Reference: PLoS One. 2013;8(3):e58501.

LGD-6972 soidum (LGD6972; MB-11262; MB11262) is a novel and orally bioavailable glucagon receptor antagonist with antidiabetic effects. It has linear plasma pharmacokinetics consistent with once daily dosing that is comparable in healthy and T2DM subjects. It also reduces plasma glucose in the postprandial state. Dose-dependent increases in fasting plasma glucagon are observed, but glucagon levels […]

PF-04929113 mesylate (also known as SNX-5422 mesylate) is a potent and selective inhibitor of heat shock protein 90 (HSP90) with Kd of 41 nM, it induces Her-2 degradation with IC50 of 37 nM. PF-04929113 is a synthetic prodrug of SNX-2112 with potential antineoplastic activity. PF-04929113 is rapidly converted to SNX-2112, which accumulates in tumors relative […]

BMS-711939, an analog of BMS-687453, is a novel potent and selective peroxisome proliferator activated receptor (PPAR) alpha agonist, with an EC50 and IC50 of 4 nM for human PPARα and >1000-fold selectivity vs human PPARγ (EC50 of 4.5 μM) and PPARδ (EC50 > 100 μM) in PPAR-GAL4 transactivation assays. BMS-711939 has an excellent pharmacological and […]

Q203 is an imidazopyridine amide (IAP) compound that block Mycobacterium tuberculosis growth by targeting the respiratory cytochrome bc1 complex. It has the potential for the treatment of tuberculosis. Q203 inhibited the growth of MDR and XDR M. tuberculosis clinical isolates in culture broth medium in the low nanomolar range and was efficacious in a mouse […]