General description
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 Actions
Cell permeable: yes
Primary Target
CK2, SRPK1
Reversible: yes
Target IC50: 0.2 & 2.4 µ
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Morooka, S., et al. 2015. Mol. Pharmacol.88, 316.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 370.31. Empirical Formula: C14H9F3N4O3S. Assay: ≥. 98% (HPLC). Quality Level: 100. form: solid. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, protect from light. color: yellow. solubility: DMSO: 20 . mg/mL. storage temp.: 2-8°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 12352204
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 5383560001