1. Protein Tyrosine Kinase/RTK
  2. DYRK
  3. EHT 1610

EHT 1610 is a potent inhibitor of DYRK, with IC50s of 0.36 nM (DYRK1A), 0.59 nM (DYRK1B), respectively. EHT 1610 exhibits antileukemia effect, regulates cell cycle and induces cell apoptosis-.

For research use only. We do not sell to patients.

EHT 1610 Chemical Structure

EHT 1610 Chemical Structure

CAS No. : 1425945-60-3

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Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE EHT 1610

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Description

EHT 1610 is a potent inhibitor of DYRK, with IC50s of 0.36 nM (DYRK1A), 0.59 nM (DYRK1B), respectively. EHT 1610 exhibits antileukemia effect, regulates cell cycle and induces cell apoptosis[1]-[4].

IC50 & Target

IC50: 0.36 nM (DYRK1A), 0.59 nM (DYRK1B)[1]

In Vitro

EHT 1610 induces apoptosis of primary ALL cells that were resistant to cytarabine[2].
EHT 1610 dose-dependently induces apoptosis in B- and T-cell lines and primary human pediatric[2].
EHT 1610 (; 72 h) inhibits DYRK1A, results loss of DYRK1A-mediated FOXO1 and STAT3 signaling, leading to preferential cell death in leukemic B cells[3].
EHT 1610 (2.5-10 μM; 4-5 h) inhibits phosphorylation of FOXO1, STAT3 and cyclin D3, thus regulates late cell-cycle progression, mitochondrial ROS and DNA damage, respectively[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[3]

Cell Line: MHH-CALL-4 cells
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 4, 5 hours
Result: Reduced p-cyclin D3 (Thr283), and p-FOXO1 protein level in a dose-dependent manner.
In Vivo

EHT 1610 (20 mg/kg/d; i.p.; twice a day; 3 weeks) shows antileukemia activity against in leukemic aggressive model in mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Xenograft models of B-ALL in mice (12-14 weeks old)[3]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection; twice a day, 5 days on, 2 days off; 3 weeks
Result: Reduced leukemic burden by approximately 8% and conferred a modest survival advantage.
Molecular Weight

383.40

Formula

C18H14FN5O2S

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

N=C(C(S1)=NC2=C1C3=C(NC4=CC=C(OC)C=C4F)N=CN=C3C=C2)OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light, stored under nitrogen

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (13.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6082 mL 13.0412 mL 26.0824 mL
5 mM 0.5216 mL 2.6082 mL 5.2165 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.16%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6082 mL 13.0412 mL 26.0824 mL 65.2061 mL
5 mM 0.5216 mL 2.6082 mL 5.2165 mL 13.0412 mL
10 mM 0.2608 mL 1.3041 mL 2.6082 mL 6.5206 mL
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EHT 1610 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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EHT 1610
Cat. No.:
HY-111380
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