1481617-15-5
1481617-15-5 structure
- Name: Ipivivint
- Chemical Name: Ipivivint
- CAS Number: 1481617-15-5
- Molecular Formula: C26H21FN8
- Molecular Weight: 464.50
- Catalog: Signaling Pathways Cell Cycle/DNA Damage CDK
- Create Date: 2022-02-16 15:38:52
- Modify Date: 2024-01-15 12:17:59
-
Ipivivint, a first-in-class, orally active and potent CDC-like kinase (CLK) inhibitor, inhibits CLK1 (IC50=1.4 μM), CLK2 (IC50=0.002 μM) and CLK3 (IC50=0.022 μM). Ipivivint reduces Wnt pathway signaling gene expression through inhibiting CLK activity and serine and arginine rich splicing factor (SRSF) phosphorylation and disrupting spliceosome activity. Ipivivint can be used for the research of cancer[1].
| Name | Ipivivint |
|---|
| Description | Ipivivint, a first-in-class, orally active and potent CDC-like kinase (CLK) inhibitor, inhibits CLK1 (IC50=1.4 μM), CLK2 (IC50=0.002 μM) and CLK3 (IC50=0.022 μM). Ipivivint reduces Wnt pathway signaling gene expression through inhibiting CLK activity and serine and arginine rich splicing factor (SRSF) phosphorylation and disrupting spliceosome activity. Ipivivint can be used for the research of cancer[1]. |
|---|---|
| Related Catalog | |
| Target |
Wnt CDK1:1.4 μM (IC50) CDK2:0.002 μM (IC50) CDK3:0.022 μM (IC50) |
| In Vitro | Ipivivint (SW480 cells; 0.01~10 μM; 1 hour) potently inhibits SRSF5/6 phosphorylation[1]. Ipivivint (SW480 cells; 0.03 μM~3 μM; 48 hour) induced apoptosis[1]. .Ipivivint (HEK-293T cells; 0.03 μM~3 μM; 1 hour) inhibits Wnt/β-catenin signaling induced by Wnt3a[1]. Ipivivint (SW480 cells; 0.3~10 μM; 6 hour) increases nuclear speckle enlargement[1]. Ipivivint (SW480 cells; 0.3~3μM; 24hours) significantly decreases expression of Wnt target genes (AXIN2, LEF1, MYC, and TCF7) and TCF7L2. SM08502 (SW480 cells; 0.03~3μM; 24hours) inhibits cytoplasmic or nuclear fractions protein expression. Ipivivint (NCI–N87 cells) inhibits proliferation[1]. Ipivivint strongly inhibits Wnt pathway signaling activity (EC50 = 0.046 μM) in SW480 colon cancer cells[1]. Western Blot Analysis[1] Cell Line: SW480 cells Concentration: 0.01~10 μM Incubation Time: 1 hour Result: Potently inhibited SRSF5/6 phosphorylation. Apoptosis Analysis[1] Cell Line: SW480 cells Concentration: 0.01~10 μM Incubation Time: 0.03 μM~3 μM Result: Induced apoptosis. RT-PCR[1] Cell Line: HEK-293T cells Concentration: 0.3~3 μM Incubation Time: 1 hour Result: Inhibited Wnt/β-catenin signaling induced by Wnt3a. Immunofluorescence[1] Cell Line: SW480 cells Concentration: 0.3~10 μM Incubation Time: 6 hours Result: Increased nuclear speckle enlargement. |
| In Vivo | Ipivivint (25 mg/kg; p.o.) potently inhibits tumor SRSF6 phosphorylation[1]. Animal Model: Foxn1 mice[1] Dosage: 25 mg/kg Administration: P.o. Result: Potently inhibited tumor SRSF6 phosphorylation. |
| References |
| Molecular Formula | C26H21FN8 |
|---|---|
| Molecular Weight | 464.50 |