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

Images & Validation

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Key Properties

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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	Tyrosinase,CDK,GSK-3,DYRK,NF-κB
Solubility	DMSO:4.5 mg/mL (11.74 mM)

Bioactivity

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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 Read more...
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. Read more...
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. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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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

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Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID

71529602 ↗

Key Properties

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No computed properties available.

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EHT 1610 (orb1707342)

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EHT 1610

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Quality Guarantee

Compound Identifiers

Key Properties

Documents Download

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Protocol Information

EHT 1610 (orb1707342)

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