EHT 1610

SKU: orb1707342

Description

EHT 1610 is a highly potent and selective DYRK1A/B inhibitor with sub-nanomolar IC50 values. It demonstrates anti-leukemic activity in research settings by disrupting cell cycle progression and promoting apoptosis in vitro, supporting its investigation in oncology and cell signaling studies.

Research Area

Cell Biology, Protein Biochemistry, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1425945-60-3
• MW: 383.4
• Purity: 98.59% (May vary between batches)
• Formula: C₁₈H₁₄FN₅O₂S
• SMILES: COC(=N)c1nc2ccc3ncnc(Nc4ccc(OC)cc4F)c3c2s1
• Target: CDK,GSK-3,DYRK,NF-κB,Tyrosinase
• Solubility: DMSO:4.5 mg/mL (11.74 mM)

Bioactivity

• Target IC50:
  GSK-3β:221 nM|GSK-3α:7.44 nM|β-glucuronidase:93.2 nM|CLK4:59 nM|CLK2:88.8 nM|DYRK1A:0.22 nM|DYRK1A:0.36 nM|DYRK1B:0.28 nM|DYRK1B:0.59 nM|DYRK2:10.8 nM|CLK1:22.8 nM
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• In Vivo:
  In a murine model of aggressive leukemia, EHT 1610 (20 mg/kg/d; i.p.; twice a day; 3 weeks) demonstrates antileukemia activity when administered intraperitoneally.
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• In Vitro:
  EHT 1610 triggers apoptosis in primary ALL cells that exhibit resistance to cytarabine treatment. EHT 1610 demonstrates a dose-dependent induction of apoptosis in B- and T-cell lines as well as primary human pediatric cells. Treatment with EHT 1610 for a duration of 72 hours leads to the inhibition of DYRK1A, resulting in the disruption of DYRK1A-mediated FOXO1 and STAT3 signaling pathways. This disruption ultimately leads to selective cell death in leukemic B cells. Exposure to EHT 1610 at concentrations ranging from 2.5 to 10 μM for a period of 4-5 hours results in the inhibition of phosphorylation of FOXO1, STAT3, and cyclin D3. This inhibition leads to the regulation of late cell-cycle progression, mitochondrial ROS levels, and DNA damage, respectively.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

DYRK2, DYRK1B, DYRK1A, DYRK3, CLK1, CLK2, Clk4, GSK-3α, GSK3α, GSK3β, GSK-3β, GSK3, EHT5372, EHT-5372, EHT 5372, EHT1610, EHT-1610, EHT 1610, p65, NFκB, NFkB, NF-kB, Tyrosinase

Compound Identifiers

PubChem CID

71529602