Substrates and Inhibitors

A fluorogenic substrate for caspase 3. The 7-amido-4-trifluoromethylcoumarin derivatives have better membrane permeability than the 7-amido-4-methylcoumarin derivatives.

Cleavage of R110 peptides by caspases generates strongly fluorescent R110 that can be monitored fluorimetrically at 510-530 nm with excitation of 488 nm.This R110 substrate is specific for caspases 3 and 7.

A fluorogenic substrate for caspase 3, a protease that is rapidly activated when cells are exposed to apoptotic conditions and that cleaves poly(ADP-ribose) polymerase.

The non-fluorescent R110 substrates generate the bright green fluorescent rhodamine 110 product that has Ex/Em = 494/521 nm, and can be easily detected with a FITC filter set. In general, R110 substrates are much more sensitive than the AMC-, AFC- or 4-nitroaniline-based substrates. This R110 substrate is used for...

PI/PS (4:1, w/w) unilamellar vesicle, prepared with L-alpha-phosphatidylinositol (Liver, Bovine) (sodium salt) and L-alpha-phosphatidylserine (Brain, Porcine) (sodium salt). Lipid monolayer was formed by sonication. Application: Useful as a substrate for PI-3 kinase activity assays and other lipid kinases....

PPACK is a synthetic peptide derivative that irreversibly and specifically inhibits thrombin-mediated platelet activation by binding with high affinity to the active site of thrombin (Ki = 0.24 nM). It has been used as an anticoagulant (100 µM) and to study thrombin-mediated fibrin deposition, angiogenesis, and...

LL-37 (13-37) is an anticancer peptide fragment of LL-37 (Cay-24461). It inhibits the ATPase activity of ATP-binding cassette transporter 2, subfamily G (ABCG2) when used at a concentration of 1 µM. LL-37 (13-37) induces cytotoxicity in wild-type SW620 cells and SW620 cells overexpressing P-glycoprotein (P-gp), also...

Chemokine (C-X-C motif) ligand 9 (CXCL9) (74-103) is a C-terminal fragment of mature CXCL9. It binds to the glycosaminoglycan heparin in a cell-free assay (Kd = 3.1 nM). CXCL9 (74-103) inhibits the binding of CXCL8 or CXCL11 to heparin, as well as chemokine (C-C motif) ligand 2 (CCL2) binding to heparan sulfate, in...

Aureobasidin A is a cyclic depsipeptide that has been found in A. pullulans and has diverse biological activities. It inhibits inositol phosphorylceramide synthase, an enzyme involved in sphingolipid biosynthesis (Kis = 0.18 and 0.23 for the C. albicans and S. cerevisiae enzymes, respectively). Aureobasidin A also...

Retatrutide is a triple agonist of the glucagon receptor (GCGR), glucagon-like peptide 1 receptor (GLP-1R), and gastric inhibitory polypeptide receptor (GIP receptor), also known as the glucose-dependent insulinotropic polypeptide receptor. It induces cAMP accumulation in HEK293 cells expressing the human GCGR,...

PE 22-28 is a peptide inhibitor of the two-pore domain potassium channel K2P2.1/TREK1 (IC50 = 0.1 nM in HEK293 cells expressing the human channel) and a fragment of spadin (Cay-36762). It is selective for K2P2.1/TREK1 over K2P10.1 /TREK2, K2P13.1/TRAAK, K2P18.1/TRESK, and K2P3.1/TASK1 in HEK293 cells expressing the...

[pGlu4]-Myelin basic protein peptide is a substrate for PKC. It is selectively phosphorylated by PKC over PKA and phosphorylase kinase.Formal Name: 5-oxo-L-prolyl-L-lysyl-L-arginyl-L-prolyl-L-seryl-L-glutaminyl-L-arginyl-L-seryl-L-lysyl-L-tyrosyl-L-leucine, trifluoroacetate salt. Synonyms: [pGlu4]-MBP Peptide....