2. Epigenetics
  3. Histone Demethylase
  4. KDM4-IN-2

KDM4-IN-2 (Compound 19a) is a potent and selective KDM4/KDM5 dual inhibitor with Kis of 4 and 7 nM for KDM4A and KDM5B, respectively.

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KDM4-IN-2

KDM4-IN-2 Estructura química

No. CAS : 2369607-62-3

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KDM4-IN-2 Related Antibodies

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Ver todos los productos específicos de isoformas Histone Demethylase:

Ver todas las isoformas
KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

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Descripciòn

KDM4-IN-2 (Compound 19a) is a potent and selective KDM4/KDM5 dual inhibitor with Kis of 4 and 7 nM for KDM4A and KDM5B, respectively[1].

IC50 & Target

KDM4

 

Cellular Effect
Cell Line Type Value Description References
HeLa EC50
13.4 μM
Compound: 19a
Inhibition of full length human wild type KDM5B transfected in HeLa cells assessed as decrease in demethylation of H3K4Me3 measured after 24 hrs by cell analyser based immunofluorescence assay
Inhibition of full length human wild type KDM5B transfected in HeLa cells assessed as decrease in demethylation of H3K4Me3 measured after 24 hrs by cell analyser based immunofluorescence assay
[PMID: 31158747]
HeLa EC50
4.7 μM
Compound: 19a
Inhibition of FLAG tagged full length wild type human KDM4A transfected in HeLa cells assessed as decrease in demethylation of H3K9Me3 measured after 24 hrs by cell analyser based immunofluorescence assay
Inhibition of FLAG tagged full length wild type human KDM4A transfected in HeLa cells assessed as decrease in demethylation of H3K9Me3 measured after 24 hrs by cell analyser based immunofluorescence assay
[PMID: 31158747]
Sf9 IC50
0.043 μM
Compound: 19a
Inhibition of N-terminal GST-tagged recombinant human KDM4B (1 to 500 residues) expressed in baculovirus infected Sf9 insect cells assessed as decrease in demethylation of substrate using peptide (ARTKQTARK(Me3)STGGKAPRKQLA-GGKbiotin) as substrate and 2OG
Inhibition of N-terminal GST-tagged recombinant human KDM4B (1 to 500 residues) expressed in baculovirus infected Sf9 insect cells assessed as decrease in demethylation of substrate using peptide (ARTKQTARK(Me3)STGGKAPRKQLA-GGKbiotin) as substrate and 2OG
[PMID: 31158747]
Peso molecular

426.51

Fòrmula

C25H26N6O
No. CAS
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=CC=NC(N3C=C(CCN4CCC5(CCC6=C5C=CC=C6)CC4)C=N3)=C2N=CN1
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvente y solubilidad
In Vitro: 

DMSO : 4 mg/mL (9.38 mM; ultrasonic and warming and heat to 60°C; 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 2.3446 mL 11.7231 mL 23.4461 mL
5 mM 0.4689 mL 2.3446 mL 4.6892 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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V2

In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Pureza y Documentación
Referencias

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3446 mL 11.7231 mL 23.4461 mL 58.6153 mL
5 mM 0.4689 mL 2.3446 mL 4.6892 mL 11.7231 mL
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KDM4-IN-2 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.

Keywords:

KDM4-IN-22369607-62-3Histone DemethylaseInhibitorinhibitorinhibit

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Nombre del producto:
KDM4-IN-2
Cat. No.:
HY-128343
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