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Cat. No.: HY-117226

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GSK 690

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

GSK 690 is a reversible inhibitor of lysine specific demethylase 1 (LSD1), with a K_d value of 9 nM and a biochemical IC₅₀ of 37 nM.

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CAS No.: 2101305-84-2
Formule: C₂₄H₂₃N₃O
Masse moléculaire:369.46

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Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (270 KB)

GSK 690 Chemical Structure

CAS No.: 2101305-84-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- Cellular Effect
- In Vitro
Chemical Information
Publications (3)
Pureté et documentation
Références
Calculators
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Classifications
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Activité biologique

Description

GSK 690 is a reversible inhibitor of lysine specific demethylase 1 (LSD1), with a K_d value of 9 nM and a biochemical IC₅₀ of 37 nM.

Voir tous les produits spécifiques à Isoform Histone Demethylase :

Cellular Effect

Cell Line	Type	Value	Description	References
MOLM-13	IC₅₀	613 nM Compound: 8; GSK-354	Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 7 days by WST-8 assay Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 7 days by WST-8 assay	[PMID: 37849536]
MV4-11	IC₅₀	122 nM Compound: 8; GSK-354	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 10 days by WST-8 assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 10 days by WST-8 assay	[PMID: 37849536]
NCI-H1417	IC₅₀	213 nM Compound: 8; GSK-354	Antiproliferative activity against human NCI-H1417 cells assessed as cell growth inhibition incubated for 10 days by WST-8 assay Antiproliferative activity against human NCI-H1417 cells assessed as cell growth inhibition incubated for 10 days by WST-8 assay	[PMID: 37849536]
RD	IC₅₀	10.2 μM Compound: 46; GSK-690	Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 144 hrs Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 144 hrs	[PMID: 35525212]
RD	IC₅₀	11.43 μM Compound: 46; GSK-690	Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 72 hrs Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 72 hrs	[PMID: 35525212]
RD	IC₅₀	12.35 μM Compound: 46; GSK-690	Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 24 hrs Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 24 hrs	[PMID: 35525212]
SJRH30	IC₅₀	10.3 μM Compound: 46; GSK-690	Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 144 hrs Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 144 hrs	[PMID: 35525212]
SJRH30	IC₅₀	10.7 μM Compound: 46; GSK-690	Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 72 hrs Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 72 hrs	[PMID: 35525212]
SJRH30	IC₅₀	9.93 μM Compound: 46; GSK-690	Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 24 hrs Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 24 hrs	[PMID: 35525212]
THP-1	IC₅₀	1.4 μM Compound: 25, GSK354	Inhibition of LSD1 in human THP1 cells assessed as CD86 level after 24 hrs by ELISA Inhibition of LSD1 in human THP1 cells assessed as CD86 level after 24 hrs by ELISA	10.1039/C3MD00226H

In Vitro

GSK690 (1-10μM) acts together with JNJ-26481585 to induce cell death in all four tested RMS cells lines (RD, RH30, RMS13, and TE381.T cells)^[2].
GSK690/JNJ-26481585 cotreatment alters the balance between pro- and antiapoptotic proteins with 1 μM GSK690 for RD cells) and 10 μM GSK690 for RH30 cells^[2].
GSK690/JNJ-26481585 cotreatment induces caspase-dependent cell death with 1 μM GSK690 for RD cells and 10 μM GSK690 for RH30 cells^[2].
The addition of GSK690 further enhances the JNJ-26481585-stimulated G2/M arrest ^[2].

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

Chemical Information

CAS No. 2101305-84-2
Masse moléculaire 369.46
Formule C₂₄H₂₃N₃O
SMILES

N#CC1=CC=C(C2=CC(OC[C@H]3CNCC3)=CN=C2C4=CC=C(C)C=C4)C=C1
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (3)

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Journal Impact Factor

Oncogene

BRD4 inhibition sensitizes cervical cancer to radiotherapy by attenuating DNA repair. [Abstract]

2021 Apr;40(15):2711-2724. PMID: 33712705
Clin Exp Med

Corin: a dual inhibitor for KDM1A/HDAC1, suppresses hepatocellular carcinoma by triggering cuproptosis. [Abstract]

2025 Nov 25;26(1):33. PMID: 41286164
Research Square Preprint

2024 Nov 19.

Pureté et documentation

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Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Mould DP, et al. Development of (4-Cyanophenyl)glycine Derivatives as Reversible Inhibitors of Lysine Specific Demethylase 1. J Med Chem. 2017 Oct 12;60(19):7984-7999. [Content Brief]

[2]. Haydn T, et al. Concomitant epigenetic targeting of LSD1 and HDAC synergistically induces mitochondrial apoptosis in rhabdomyosarcoma cells. Cell Death Dis. 2017 Jun 15;8(6):e2879. [Content Brief]

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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GSK 690

3 Cited Publications

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Activité biologique
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Chemical Information
Publications (3)
Pureté et documentation
Références

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GSK 690

Publications Citing Use of MedChemExpress (MCE) GSK 690

Voir tous les produits spécifiques à Isoform Histone Demethylase

Activité biologique

Chemical Information

Publications (3)

Pureté et documentation

Références

Calculators

Help & FAQs

GSK 690 Related Classifications

HY-117226 Related Classifications