233624

Cryptocrome Activator, KL001

The Cryptocrome Activator, KL001 modulates the biological activity of Cryptocrome. This small molecule/inhibitor is primarily used for Biochemicals applications.

• Synonyme(s) : Cryptocrome Activator, KL001, N-(3-(9H-Carbazol-9-yl)-2-hydroxypropyl)-N-(furan-2-ylmethyl)methanesulfonamide, CRY Activator, KL001
• Formule empirique (notation de Hill): C₂₁H₂₂N₂O₄S
• Numéro CAS: 309928-48-1
• Poids moléculaire : 398.48
• Numéro MDL: MFCD02086647
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: off-white
• Solubilité: DMSO: 50 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C
• Chaîne SMILES: OC(CN(CC1=CC=CO1)S(=O)(C)=O)CN2C3=C(C=CC=C3)C4=C2C=CC=C4

Description

Description générale

A cell-permeable carbazole compound that competes against FAD (flavin adenine dinucleotide) for cryptocrome (CRY) 1 & 2 binding, displaying little affinity toward other clock proteins (PER1/2, CLOCK, or BMAL1) or inhibitory activity against casein kinase (CKIα, CKIδ, and CK2) activity even at concentrations as high as 100 µM. Shown to selectively stabilize cellular CRY1/2 protein, but not mRNA, by preventing FBXL3-mediated CRY1/2 ubiquitination and proteasomal degradation, effectively lengthening the period and reducing the amplitude of the circadian transcription rhythms of Bmal1 and Per2 promoter-mediated transcription activity (IC₅₀ of intensity reduction = 14 and 0.82 µM, respectively, in U2OS reporter assay). KL001 is also reported to block glucagon-induced Pck1 and G6pc mRNA upregulation as well as glucose production in primary murine hepatocyte cultures (IC₅₀<8 µM). Longdaysin (Cat. No. 438075), in comparison, exerts its circadian perturbation activity via casein kinase inhibition.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
Cryptocrome protein

Reversible: yes

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Autres remarques

Hirota, T., et al. 2012. Science337, 1094.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Pictogrammes: GHS07
• Mention d'avertissement: Warning
• Mentions de danger: H302
• Conseils de prudence: P264 - P270 - P301 + P312 - P501
• Classification des risques: Acute Tox. 4 Oral
• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable