Iberin (NSC 321801), a sulfoxide analog of sulforaphane, is a naturally occurring antioxidant that is a member of isothiocyanate family. It inhibits cell survival with an IC50 of 2.3 μM in HL60 cell. It induces phase II enzyme activity and suppresses CDK expression, inducing apoptosis in cancer cells.

SB-772077B dihydrochloride (also known as SB-772077-B; SB-772077) is a novel and potent aminofurazan-based Rho kinase( ROCK) inhibitor with IC50s of 5.6 nM and 6 nM toward ROCK1 and ROCK2, respevtively. Oral administration of either SB-772077-B produced a profound dose-dependent reduction of systemic blood pressure in spontaneously hypertensive rats. At doses of 1, 3, and 30 […]

Bruceantin (also known as NSC165563), a novel anticancer quassinoid compound extracted from Brucea antidysenterica, is first isolated from Brucea antidysenterica which is a tree found and used in Ethiopia for the treatment of cancer such as leukemia, and the activity was observed against B16 melanoma, colon 38, and L1210 and P388 leukemia in mice.

PI3K/mTOR Inhibitor-1, a Sulfonyl-Substituted Morpholinopyrimidines based analog, is a novel, potent, orally bioavailable dual PI3K/mTOR inhibitor with potential antitumor activity. and with IC50s of 20/376/204/46 nM and 186 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ and mTOR, respectively. PI3K/mTOR Inhibitor-1 was identified as a potent dual PI3K/mTOR inhibitor whithc exhibited high inhibitory activity against PI3Kα/β/γ/δ (IC50 = 20/376/204/46 nM) […]

Amrubicin HCl (also known as SM-5887 hydrochloride), a third-generation synthetic 9-amino-anthracycline, is a potent DNA topoisomerase II inhibitor with antineoplastic activity. It can be used for the research of cancer. Amrubicin intercalates into DNA and inhibits the activity of topoisomerase II, resulting in inhibition of DNA replication, and RNA and protein synthesis, followed by cell […]

PRX933 HCl, the hydrochloride salt form of PRX933 which is extracted from patent WO 2014140631 A1, is a novel and potent 5-HT2c receptor agonist

GNE-955 is a novel, potent and orally bioavailable pan Pim kinase inhibitor with Kis of 0.018, 0.11, 0.08 nM for Pim1, Pim2, Pim3, respectively. Pim kinases have been identified as promising therapeutic targets for hematologic-oncology indications, including multiple myeloma and certain leukemia. GNE-955 was discovered bearing 5-azaindazole core with noncanonical hydrogen bonding to the hinge.

A-437203 is a novel, potent and selective D3 receptor antagonist with Ki of 71, 1.6, and 6220 nM for D2, D3, and D4 receptors, respectively.

Solabegron (formerly also known as GW 427353; GW-427353; GW-427,353) is a novel, potent and selective agonist for the β3 adrenergic receptor, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β3-AR, with an EC50 value of 22 nM. It is being investigated for the treatment of overactive bladder and irritable bowel syndrome. It […]

NVP-QAV-572 is a novel and potent PI3K inhibitor (extracted from patent US7998990B2, Compound Example 8) with an IC50 of 10 nM. NVP-QAV-572 is potentially useful in the treatment of conditions which are mediated by the activation of the Pi3 kinase enzymes, particularly inflammatory or allergic conditions