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SRPK1 inhibitor DBS1

Chemical Structure : SRPK1 inhibitor DBS1

CAS No.:

SRPK1 inhibitor DBS1 (Docking Blocker of SRPK1)

Catalog No.: PC-49774Not For Human Use, Lab Use Only.

SRPK1 inhibitor DBS1 (Docking Blocker of SRPK1) is a 20-mer peptide, cell-penetrating, non-ATP-competitive inhibitor of SRPK1 with ITC Kd of 5.6 uM, inhibits kinase activity of SRPK1 in a competitive manner against the substrate SRSF1 (Ki=2.12 uM), but not ATP.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

SRPK1 inhibitor DBS1 (Docking Blocker of SRPK1) is a 20-mer peptide, cell-penetrating, non-ATP-competitive inhibitor of SRPK1 with ITC Kd of 5.6 uM, inhibits kinase activity of SRPK1 in a competitive manner against the substrate SRSF1 (Ki=2.12 uM), but not ATP.
DBS1 inhibited both SRPKs but not CLK1 or Akt/PKB, confirming it specifically targets the SRPK docking groove.
DBS1 inhibited SR protein phosphorylation in treated cells, switches the VEGF pre-mRNA splicing from VEGF165 to VEGF165b dose-dependently.
DBS1 is noncytotoxic to HUVECs and could potently inhibit angiogenesis.
Cotreatment of DBS1 with ATP-competitive inhibitor of SRPK1 (SRPIN340) inhibits angiogenesis more effectively.

Physicochemical Properties

M.Wt
Formula
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

References

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