SKF-77434 HBr is a novel potent and selective dopamine D1-like receptor partial agonist. It is the N-Allyl analog ofSKF38393. The direct-acting dopamine D-1 agonists SKF 38393 [(+-)-7-bromo-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-be nzazepin e HCl], SKF 77434 [(+-)-7,8-dihydroxy-3-allyl-1-phenyl-2,3,4,5-tetrahydro-1H-benzazepine HCl] and SKF 75670 [3-methyl-7,8-dihydroxyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benza zep ine HBr] fully substituted for cocaine, whereas the peripherally active dopamine D-1 agonist fenoldopam did not. […]

SKF38393 (also known as SKF-38393A) is a novel potent and selective dopamine D1 receptor agonist with IC50 of 110 nM, the (+)-enantiomer is the active isomer. Agonism of the D1DR by SKF 38393 is correlated to induced desynchronization of electroencephalographic activity in rats. SKF 38393 also demonstrated agonism of the serotonin SR-2C (5-HT1C receptor). SKF […]

Dioctyl decanedioate (decadioic acid, dioctyl ester; Decanedioic acid, dioctyl ester; decanedioicaciddioctylester; Dioctyl-1,10-decanedioate) is a biochemical.

BAY-524 is a novel and potent Bub1 inhibitor with an IC50 of 450 nM for human Bub1 in the presence of 2 mM ATP. It demonstrated potent Bub1 kinase inhibition both in vitro and in intact cells. The kinase Bub1 functions in the spindle assembly checkpoint (SAC) and in chromosome congression, but the role of […]

PROTAC-VHL-ligand or Protein degrader 1 is a novel and potent small molecule ligand for VHL (Von Hippel-Lindau), an E3 ligase which has been targeted by many PROTACs (proteolysis-targeting chimeras) degarders. Small molecule-induced protein degradation is an attractive strategy for the development of chemical probes. One method for inducing targeted protein degradation involves the use of […]

Bucladesine (DC2797; DC-2797; Dibutyryl-cAMP) is a potent and cell-permeable PKA activator and a cAMP analog that mimics the action of endogenous cAMP. It is a cyclic nucleotide derivative (structurally similar to cAMP) and is also a phosphodiesterase inhibitor. Dibutyryl-cAMP preferentially activates cAMP-dependent protein kinase. The products releaes butyrate due to intracellular and extracellular esterase action. […]

BAY-677 is an inactive and negative control for BAY-678. BAY-678 is a novel, potent, orally bioavailable, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).

R(+)-SKF-38393A (the R-isomer of SKF3839A) is a novel potent and selective dopamine D1 receptor agonist with IC50 of 110 nM, the (+)-enantiomer is the active isomer. Agonism of the D1DR by SKF 38393 is correlated to induced desynchronization of electroencephalographic activity in rats. SKF 38393 also demonstrated agonism of the serotonin SR-2C (5-HT1C receptor). SKF […]

BLU-782 has been discontinued. BLU-782 (also known as ALK2-IN-1) is a novel, potent, selective, and oral bioactive inhibitor of ALK2 (Activin receptor-like kinase) mutant R206H with binding IC50 of

TH-263 is a diaryl sulfonamide derivativeused as a negative control for the type III allosteric LIM-kinase (LIMK) inhibitors TH-257, TH-255 and TH-251. LIM kinases belong to the family of cytoplasmic tyrosine-like kinases with dual specificity (serine/threonine and tyrosine). However, known LIMK substrate are usually phosphorylated at serine and threonine residues LIM kinases comprises LIM kinase […]