GSK-962 (also known as GSK’962 or GSK962) is a negative control for GSK’963 (also known as GSK’963 or GSK963). GSK-963 is a potent and selective RIP1 kinase inhibitor. GSK’963 is significantly more potent than Nec-1 (a known RIP1 kinase inhibitor ) in both biochemical and cellular assays, inhibiting RIP1-dependent cell death with an IC50 of […]

ML239 was originally identified as a potent and selective inhibitor of breast cancer stem cells with an IC50 of 1.16 μM, but recent studies (2016 Nature 12(2):109-16.) suggested that it most likely acts through activation of fatty acid desaturase 2 (FADS2). ML239 was discovered from high-throughput screen (HTS) with the National Institute of Health–Molecular Libraries […]

MCOPPB 3HCl is a novel and potent nonpeptide agonist of nociceptin receptor with pKi of 10.07 and may be used as an anxiolytic agent. MCOPPB has a high affinity for the human NOP [N/OFQ (nociceptin/orphanin FQ) peptide] receptor (pKi = 10.07 +/- 0.01) and selectivity for the NOP receptor over other members of the opioid […]

FIPI HCl, the hydrochloride salt of FIPI which is formerly known as 5-Fluoro-2-indolyl deschlorohalopemide, is a derivative of halopemide which potently and selectively inhibits both PLD1 (phospholipase D) and PLD2 with IC50 values of 25 nM and 20 nM, respectively. FIPI is able to attenuate mercury-induced lipid signaling resulting in protection against cytotoxicity in aortic […]

NSC23005 sodium 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 […]

HDM201 R Enantiomer is the R enantiomer of HDM201 (also called NVP-HDM201, HDM stands for ‘human double minute 2 homolog’). HDM201 is an orally bioavailable, highly potent and selective inhibitor of the p53-Mdm2 protein-protein interaction. It has high affinity for Mdm2 in the picomolar range and a selectivity ratio of more than 10000-fold vs Mdm4. […]

This product is discontinued due to commercial reason. BT-11 is a first-in-class, potent, orally available and selective modulator of LANCL2 (Lanthionine synthetase C-like 2) which is a novel therapeutic target for inflammatory and autoimmune diseases and diabetes, exerts anti-inflammatory and insulin-sensitizing effects. BT-11 at high doses has an excellent safety profile up to 1000 mg/kg/day. […]

Netarsudil (formerly known as AR-13324; AR13324; trade name Rhopressa) is ROCK inhibitor approved in 2017 for the treatment of glaucoma and ocular hypertension. It inhibits ROCK with Ki of 0.2-10.3 nM. Netarsudil also inhibits norepinephrine transport activity which can reduce the production of aqueous humor. As of 2018, Netarsudil has been approved by FDA for […]

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 and chronic pain (tail-flick, rheumatoid arthritis, […]

HU-211 (Dexanabinol) is a novel, potent synthetic terpene-based cannabinoid devoid of central cannabinoid (CB1) and peripheral cannabinoid (CB2) agonist activity, thus lacking the psychomotor responses characteristic of Δ9-THC. HU-211 does exhibit the neuroprotective, antioxidant properties of other related compounds like cannabidiol. HU-211 also has anti-inflammatory properties derived through inhibition of NF-κB and the resulting decreases […]