5.38356

SRPIN803

• Synonym(e): SRPIN803, 6-(4-Hydroxy-3-methoxybenzylidene)-5-imino-2-(trifluoromethyl)-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-7(6H)-one, SRPK1 Inhibitor II, Casein Kinase II Inhibitor XIII
• Empirische Formel (Hill-System): C₁₄H₉F₃N₄O₃S
• Molekulargewicht: 370.31
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Qualitätsniveau: 100
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: yellow
• Löslichkeit: DMSO: 20 mg/mL
• Lagertemp.: 2-8°C

Beschreibung

Allgemeine Beschreibung

A cell-permeable, bioavailable, non-toxic thiadiazolopyrimidinone based compound that acts a potent, reversible and ATP-competitive dual inhibitor of CK2 & SRPK1 (IC₅₀ = 0.2 & 2.4 µM, respectively). Displays excellent selectivity in a 306-kinase panel (% inhibition at 10 µM = 82.5, 70.9, 59.9 & 13.7 for CK2α1/β, CK2α2/β, SRPK1 & SRPK2, respectively). Synergistically suppresses VEGF production in a time and dose-dependent manner and down-regulates several angiogenesis genes expression (10 µM in ARPE-19 cells). Shown to be highly efficacious than SRPIN340 (Cat. No. 504293) and significantly inhibit choroidal neovascularization in a mouse model of age-related macular degeneration (intravitreous injection or topical administration).

A cell-permeable, bioavailable, non-toxic thiadiazolopyrimidinone based compound that acts a potent, reversible and ATP-competitive dual inhibitor of CK2 & SRPK1 (IC₅₀ = 0.2 & 2.4 µM, respectively). Displays excellent selectivity in a 306-kinase panel (% inhibition at 10 µM = 82.5, 70.9, 59.9 & 13.7 for CK2α1/β, CK2α2/β, SRPK1 & SRPK2, respectively). Synergistically suppresses VEGF production in a time and dose-dependent manner and down-regulates several angiogenesis genes expression (10 µM in ARPE-19 cells). Shown to be highly efficacious than SRPIN340 (Cat. No. 504293) and significantly inhibit choroidal neovascularization in a mouse model of age-related macular degeneration (intravitreous injection or topical administration).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Biochem./physiol. Wirkung

Cell permeable: yes

Primary Target
CK2, SRPK1

Reversible: yes

Target IC₅₀: 0.2 & 2.4 &micro

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Sonstige Hinweise

Morooka, S., et al. 2015. Mol. Pharmacol.88, 316.

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable