PZ-2891 (PZ2891) is an orally bioavailable, and brain penetrant allosteric activator of Pantothenate kinase (PANK) with neuroprotective activity. It acts as both an orthosteric inhibitor with IC50 of 1.3 nM and an allosteric activator of PANK3 in the presence of acetyl-CoA in biochemical assays. Pantothenate kinase (PANK) is a metabolic enzyme that regulates cellular coenzyme […]

Cebranopadol hemicitrate, the hemicitrate salt of Cebranopadol (also known as GRT-6005), is a novel, first in class compound with potent agonist activity on ORL-1 (opioid receptor like -1) and the well established mu opioid receptor. Cebranopadol is an analgesic nociceptin/orphanin FQ peptide (NOP) that exhibits high potency and efficacy in several rat models of acute […]

HUHS015 is a novel and potent inhibitor of PCA-1/ALKBH3 (prostate cancer antigen-1/AlkB Homolog 3) both in vitro and in vivo that was discovered from the optimization of a hit compound identified during random screening using a recombinant PCA-1/ALKBH3. The bioavailability (BA) of HUHS015 was 7.2% in rats after oral administration. Continuously administering HUHS015 significantly suppressed […]

NSC23005 is a novel and potent p18 inhibitor with ED50 of 5.21 nM in promoting Hematopoietic stem cells (HSCs) expansion in both murine and human models. Hematopoietic stem cells have emerged as promising therapeutic cell sources for high-risk hematological malignancies and immune disorders. However, their clinical use is limited by the inability to expand these […]

UNC1079, the piperidine analog of UNC1021, is a structurally similar but significantly less potent inhibitor for use as a negative control in cellular studies. It is used as a chemical probe for the methyllysine (Kme) reading function of L3MBTL3, a member of the malignant brain tumor (MBT) family of chromatin-interacting transcriptional repressors. The low anticipated […]

ARRY-797 (also known as ARRY 371797) is a novel, potent and selective inhibitor of p38α (p38 mitogen-activated protein kinase). ARRY-371797 Inhibits LPS-Induced IL-6 and In Vivo Growth of RPMI-8226 Human Multiple Myeloma Cells. Treatment of Lmna(H222P/H222P) mice with the p38α inhibitor ARRY-371797 prevented left ventricular dilatation and deterioration of fractional shortening compared with placebo-treated mice […]

JWH-133 is a synthetic cannabinoid and a potent & selective agonist of the CB2 receptor with a Ki of 3.4nM and selectivity of ~ 200x for CB2 over CB1 receptors. It was discovered by and named after, John W. Huffman. JWH-133 is responsible for preventing the inflammation caused by Amyloid beta proteins involved in Alzheimer’s […]

Cligosiban (formerly known as PF-3274167) is a novel, potent, selective and high-affinity nonpeptide antagonist of oxytocin receptor (OTR) with Ki of 9.5 nM. PF-3274167 displayed promising in vivo pharmacokinetics and significantly improved aqueous solubility over related compounds containing a biaryl substituent. Oxytocin receptor is a G protein-coupled receptor/protein which functions as receptor for the hormone […]

Decoyinine (also known as Angustmycin A) is a potent and selective inhibitor of GMP synthetase (GMPS, guanosine monophosphate synthase). Decoyinine allows sporulation in Bacillus subtilis to initiate and proceed under otherwise catabolite-repressing conditions. Decoyinine did not overcome catabolite repression of alpha-amylase synthesis in a wild-type strain of B. subtilis but did cause premature and enhanced […]

Ro 48-8071 fumarate is an orally bioavailable inhibitor of OSC (Oxidosqualene cyclase) with IC50 of ~6.5 nM. OSC represents a new and unique target for cholesterol-lowering drugs. In addition, Ro 48-8071 has shown anticancer activity, at 10 μM, it significantly reduces the viability of PC-3 prostate cancer cells, but not normal prostate cells. Ro 48-8071 […]