Chemicals & Small Molecules

K252a is a general kinase inhibitor that inhibits PKA (Ki = 18 nM), PKC (Ki = 25 nM), PKG (Ki = 20 nM), CaMK (Ki = 1.8 nM), and phosphorylase kinase (IC50 = 1.7 nM). It functions by acting competitively with ATP and noncompetitively with the substrate.

Doramapimod is a protein kinase inhibitor with a >330-fold selectivity for p38 MAPK compared with 12 other protein kinases. Doramapimod prevents both the kinetic activity and phosphorylation of p38 MAPK by binding to the ATP pocket as well as to a novel allosteric binding site on p38 MAPK. Doramapimod also blocks proliferation of cells expressing BCR-ABL(T315I), with an IC50 of 2-3 µM.

Cediranib, also known as AZD2171, is a highly potent inhibitor of recombinant KDR tyrosine kinase activity in vitro (IC50 < 1 nM). Inhibitory activity was also observed against the kinase associated with Flt-1 (IC50 = 5 nM), the VEGF-C and VEGF-D receptor Flt-4 (IC50 ≤ 3 nM), recombinant PDGFR-related kinase c-Kit (IC50 = 2 nM), and PDGFRβ tyrosine kinase (IC50 = 5 nM). In HUVEC, it inhibited VEGF-stimulated phosphorylation of KDR, c-Kit, PDGFR-α, PDGFR-β in a dose-dependent manner with IC50 values of 0.5, 1, 5, and 8 nM, respectively. Cediranib exhibits antitumor and antiangiogenic activity, and is a potential treatment for hypertension.

Tofacitinib, also known as Tasocitinib, is a novel inhibitor of Janus kinase 3 (JAK3), a critical cytoplasmic tyrosine kinase in the signaling pathways of multiple cytokines. Research suggests Tofacitinib acts as an immunosuppressant, preventing organ transplant rejection, and that it has potential to alleviate symptoms of autoimmune diseases, such as rheumatoid arthritis and psoriasis.

Specific inhibitor (IC50 = 1.40 µM) of phosphatidylinositol 3-kinase (PI3K).

Roscovitine is a potent inhibitor of p34cdc2 (IC50 = 0.2 µM). Also inhibits p33cdk2 and p33cdk5.

A cell-permeable, water-soluble, potent inhibitor of poly(ADP-ribose) polymerase (PARP; EC50 = 20 nM). Shown to be about 10,000 times more potent than the prototypical PARP inhibitor, 3-Aminobenzamide (Cat. No. 165350; EC50 = 200 µM). Does not act as an antioxidant at higher concentrations (1 µM to 10 mM). Exhibits neuroprotection in in vivo and in vitro models of stroke.

Specifically and reversibly blocks translocation of proteins from the endoplasmic reticulum to the Golgi apparatus and induces apoptosis in human tumor cells via caspase activation. Brefeldin A has been identified as an activator of the sphingomyelin signal transduction cycle.

Procaspase-activating compound; activates procaspase-3 to produce caspase-3 (EC50 = 0.22 µM). Also activates procaspase-7 in a less efficient manner (EC50 = 4.5 µM). Pro-apoptotic; induces apoptosis in both cancerous and non-cancerous cells dependent on procaspase-3 concentration (IC50 values are 0.003 - 1.41 and 5.02 - 9.98 µM respectively). PAC-1 had an IC50 value of 3 nM for induction of cell death, whereas in cells from adjacent normal tissue IC50 values of 3.2-8.5 µM were observed