1425945-60-3
1425945-60-3 structure
- Name: EHT 5372
- Chemical Name: EHT 5372
- CAS Number: 1425945-60-3
- Molecular Formula: C18H14FN5O2S
- Molecular Weight: 383.40
- Catalog: Signaling Pathways Cell Cycle/DNA Damage CDK
- Create Date: 2019-02-12 15:41:49
- Modify Date: 2024-01-29 21:30:21
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EHT 5372 is a strong inhibitor of DYRK’s family kinases, with IC50s of 0.22, 0.28 nM for DYRK1A and DYRK1B, respectively.
| Name | EHT 5372 |
|---|
| Description | EHT 5372 is a strong inhibitor of DYRK’s family kinases, with IC50s of 0.22, 0.28 nM for DYRK1A and DYRK1B, respectively. |
|---|---|
| Related Catalog | |
| Target |
CLK1:22.8 nM (IC50) Clk2:88.8 nM (IC50) Clk4:59 nM (IC50) GSK3α:7.44 nM (IC50) GSK3β:221 nM (IC50) DYRK1A:0.22 nM (IC50) DYRK1B:0.28 nM (IC50) DYRK2:10.8 nM (IC50) DYRK3:93.2 nM (IC50) |
| In Vitro | EHT 5372 is a strong inhibitor of DYRK’s family kinases, with IC50s of 0.22, 0.28 nM for DYRK1A and DYRK1B, respectively[1][2]. IC50 for DYRK2 and DYRK3 were higher (10.8 and 93.2 nM, respectively) and there was no inhibition on DYRK4. EHT 5372 displayed minimal impact on the CDC2-like kinase (CLK) family, with more than 100x selectivity over CLK1 (CLK1: IC50=22.8 nM; CLK2: IC50=88.8 nM; CLK3: IC50>10 lM; CLK4: no inhibition) and on the glycogen synthase kinase 3 (GSK3) family (GSK3α: IC50=7.44 nM; GSK3β: IC50=221 nM). EHT 5372 inhibits the direct phosphorylation of Tau by DYRK1A. EHT 5372 also normalizes both Aβ-induced Tau phosphorylation and DYRK1A-stimulated Aβ production[2]. |
| Cell Assay | HEK293 cells are changed with new culture medium and treated with 0.1-10 μM DYRK1A inhibitor EHT 5372 or 0.1% DMSO as vehicle for 24 h. The kinase inhibitor is tested in at least three independent experiments performed in duplicate. Cell viability is determined using a standard assay[2]. |
| References |
| Molecular Formula | C18H14FN5O2S |
|---|---|
| Molecular Weight | 383.40 |