SRPK Inhibitor

SPHINX31 is a potent and selective SRPK1 inhibitor, with an IC₅₀ of 5.9 nM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1). SPHINX31 also decreases the mRNA expression of pro-angiogenic VEGF-A₁₆₅a isoform. SPHINX31 can be used to research neovascular eye disease.

SRPIN340 is an ATP-competitive serine-arginine-rich protein kinase (SRPK) inhibitor, with a K_i of 0.89 μM for SRPK1.

SRPKIN-1 is a covalent and irreversible SRPK1/2 inhibitor with IC₅₀s of 35.6 and 98 nM, respectively. Anti-angiogenesis effect.

MSC-1186, a chemical probe, is a highly selective pan-SRPK inhibitor. MSC-1186 has activity for SRPK1, SRPK2 and SRPK3 with IC₅₀ values of 2.7 nM, 81 nM and 0.6 nM, respectively. MSC-1186 can be used for the research of cancer.

Srpk1-IN-1 (compound 12) is a potent inhibitor of SRPK1, with IC₅₀ of 0.3 nM.

SRPIN803 is a potent CK2 and SRPK1 dual inhibitor, with IC₅₀s of 203 nM and 2.4 μM, respectively. SRPIN803 exhibits antiangiogenic activity. SRPIN803 can be used for the research of age-related macular degeneration.

SPHINX is a selective SRPK1 inhibitor with an IC₅₀ value of 0.58 μM. SPHINX effectively reduces Choroidal Neovascularization (CNV) in vivo. SPHINX can be used for the research of (age-related macular degenaration) AMD.

SRSF1-IN-1 is a SRSF1 inhibitor. SRSF1-IN-1 inhibits SRSF1 expression, thereby modulating the splicing of Bcl-x pre-mRNA. SRSF1-IN-1 inhibits the proliferation of various cancer cells. SRSF1-IN-1 induces apoptosis in gastric cancer cells, reduces Bcl-xl expression, and upregulates cleaved PARP and caspase 3. SRSF1-IN-1 induces autophagy and promotes cell death. SRSF1-IN-1 exhibits anti-tumor activity in a mouse gastric cancer xenograft model. SRSF1-IN-1 can be used for the research of various cancers including liver cancer, gastric cancer, breast cancer, colon cancer, glioma, and melanoma.

Antiangiogenic agent 5 (compound 17) has anti-angiogenic activity. Antiangiogenic agent 5 show inhibition to SRPK1, with IC₅₀ of 1.3 nM.

LK1/2-IN-3 (compound 3) is a potent and selective CLK1 and CLK2 inhibitor with IC₅₀ values of 1.1, 2.1, 130, 260, 260 nM for CLK1, CLK2, SRPK1, SRPK2, SRPK3, respectively. CLK1/2-IN-3 shows anti-proliferative activity. CLK1/2-IN-3 reduces the levels of endogenous phosphorylated SR proteins and increases the expression of S6K mRNAs.