Flashcards: Protein kinase inhibitors

Enzastaurin is a synthetic bisindolylmaleimide with potential antineoplastic activity.

Miltefosine (trade names Impavido and Miltex) is a broad-spectrum phospholipid antimicrobial drug.

Genistein is an angiogenesis inhibitor and a phytoestrogen and belongs to the category of isoflavones.

Piceatannol is a stilbenoid, a type of phenolic compound.

Alvocidib (INN; also known as Flavopiridol or HMR-1275) is a flavonoid alkaloid CDK9 kinase inhibitor under clinical development for the treatment of acute myeloid leukemia, by Tolero Pharmaceuticals, Inc.

Idelalisib (trade name Zydelig zye-DEL-ig, codenamed GS-1101 or CAL-101) is a drug used for the treatment of certain hematological malignancies.

Momelotinib (INN, formerly GS-0387, CYT-387) is an inhibitor of Janus kinases JAK1 and JAK2, acting as an ATP competitor with IC50 values of 11 and 18 nM, respectively.

Balanol is a fungal metabolite produced by the fungus Verticillium balanoides.

Lenvatinib (trade name Lenvima) is an anti-cancer drug for the treatment of certain kinds of thyroid cancer, and potentially for other cancers as well.

Y-27632 is a biochemical tool used in the study of the rho-associated protein kinase (ROCK) signaling pathways.

VX-680 is an aurora inhibitor.

U0126 is a highly selective inhibitor of both MEK1 and MEK2, a type of MAPK/ERK kinase.

Volasertib (also known as BI 6727) is a small molecule inhibitor of the PLK1 (polo-like kinase 1) protein being developed by Boehringer Ingelheim for use as an anti-cancer agent.

Tivantinib (ARQ197; by Arqule, Inc.) is an experimental anti-cancer drug.

Midostaurin (PKC412) is a multi-target protein kinase inhibitor being investigated for the treatment of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).

PP2 is a substance that has frequently been used in cancer research as a "selective" inhibitor for Src-family kinases.

Miyabenol C is a stilbenoid.

Alisertib (MLN8237) is an orally available selective aurora A kinase inhibitor developed by Takeda.

Fasudil hydrochloride (INN) is a potent Rho-kinase inhibitor and vasodilator.

H-89 is a Protein kinase A inhibitor that also inhibits several other kinases (IC50 values are 80, 120, 135, 270, 2600 and 2800 nM for S6K1, MSK1, PKA, ROCKII, PKBα and MAPKAP-K1b).

Linsitinib is an experimental drug candidate for the treatment of various types of cancer.

Masitinib is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs.

Binimetinib (MEK162, ARRY-162) is a MEK inhibitor being developed by Array Biopharma to treat various cancers.

Ripasudil (trade name Glanatec) is a drug used for the treatment of glaucoma and ocular hypertension.

Abemaciclib (previously known as LY2835219) is a CDK inhibitor selective for CDK4 and CDK6.

Seliciclib (roscovitine or CYC202) is an experimental drug candidate in the family of pharmacological cyclin-dependent kinase (CDK) inhibitors that preferentially inhibit multiple enzyme targets including CDK2, CDK7 and CDK9, which alter the growth phase or state within the cell cycle of treated cells.

Stauprimide is a semi-synthetic analog of the staurosporine family of indolocarbazoles.

Palbociclib (codenamed PD-0332991, trade name Ibrance) is a drug for the treatment of ER-positive and HER2-negative breast cancer developed by Pfizer.

Cobimetinib (trade name Cotellic) is a MEK inhibitor developed by Exelixis and Genentech.

Dinaciclib (SCH-727965) is an experimental drug that inhibits cyclin-dependent kinases (CDKs).

Ceritinib (trade name Zykadia) is a drug for the treatment of a specific type of lung cancer.

ZM447439 is an aurora inhibitor.

Hesperadin is an aurora kinase inhibitor.

Ro-318220 is a protein kinase C (PKC) inhibitor of the bisindolylmaleimide class.

BIM-1 and the related compounds BIM-2, BIM-3, and BIM-8 are bisindolylmaleimide-based protein kinase C (PKC) inhibitors.

Losmapimod (GW856553X) is a drug developed by GlaxoSmithKline which acts as a selective inhibitor of the enzyme family known as p38 mitogen-activated protein kinases.

SB-431542 is a drug candidate developed by GlaxoSmithKline (GSK) as an inhibitor of the activin receptor-like kinase (ALK) receptors, ALK5, ALK4 and ALK7.

SU6656 is a Src family kinase inhibitor developed by the biotechnology company SUGEN Inc (a subsidiary of Pharmacia) in 2000.

AEE788 is a multitargeted human epidermal receptor (HER) 1/2 and vascular endothelial growth factor receptor (VEGFR) 1/2 receptor family tyrosine kinases inhibitor with IC50 of 2, 6, 77, 59 nM for EGFR, ErbB2, KDR, and Flt-1.

Brigatinib (previously known as AP26113) is an investigational small-molecule targeted cancer therapy being developed by ARIAD Pharmaceuticals, Inc.

Calphostin C is a natural chemical compound.

K252a is an alkaloid isolated from Nocardiopisis sp.

KT5720 is a kinase inhibitor with specificity towards protein kinase A.

Staurosporine (antibiotic AM-2282 or STS) is a natural product originally isolated in 1977 from the bacterium Streptomyces staurosporeus.