2. Epigenetics
  3. DNA Methyltransferase
  4. (R)-GSK-3685032

(R)-GSK-3685032 is the R-enantiomer of GSK-3685032. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition.

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(R)-GSK-3685032

(R)-GSK-3685032 Chemische Struktur

CAS. Nr. : 2170140-50-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Beschreibung

(R)-GSK-3685032 is the R-enantiomer of GSK-3685032. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition[1][2].

IC50 & Target[1]

DNMT1

 

Molekulargewicht

420.53

Formel

C22H24N6OS
CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

N#CC1=C(N2CCC(CC2)N)N=C(C(C#N)=C1CC)S[C@H](C3=CC=CC=C3)C(N)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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)

Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 60 mg/mL (142.68 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 2.3780 mL 11.8898 mL 23.7795 mL
5 mM 0.4756 mL 2.3780 mL 4.7559 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.

  • Molaritätsrechner

  • Verdünnungsrechner

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

Mass
=
Concentration
×
Volume
×
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

×
Volume (final)

V2

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

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(per animal)

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Number of animals

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

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 2.3780 mL 11.8898 mL 23.7795 mL 59.4488 mL
5 mM 0.4756 mL 2.3780 mL 4.7559 mL 11.8898 mL
10 mM 0.2378 mL 1.1890 mL 2.3780 mL 5.9449 mL
15 mM 0.1585 mL 0.7927 mL 1.5853 mL 3.9633 mL
20 mM 0.1189 mL 0.5945 mL 1.1890 mL 2.9724 mL
25 mM 0.0951 mL 0.4756 mL 0.9512 mL 2.3780 mL
30 mM 0.0793 mL 0.3963 mL 0.7927 mL 1.9816 mL
40 mM 0.0594 mL 0.2972 mL 0.5945 mL 1.4862 mL
50 mM 0.0476 mL 0.2378 mL 0.4756 mL 1.1890 mL
60 mM 0.0396 mL 0.1982 mL 0.3963 mL 0.9908 mL
80 mM 0.0297 mL 0.1486 mL 0.2972 mL 0.7431 mL
100 mM 0.0238 mL 0.1189 mL 0.2378 mL 0.5945 mL
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(R)-GSK-3685032 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:

(R)-GSK-36850322170140-50-6DNA MethyltransferaseDNMTsDNA MTasesselectiveR-enantiomerDNA methyltransferasemethylated modificationcancerInhibitorinhibitorinhibit

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