An LSD1 inhibitor
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Alternative(s)
45336GSK690
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GSK690 (hydrochloride)

Item No. 45320

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[2-(4-methylphenyl)-5-[(3R)-3-pyrrolidinylmethoxy]-3-pyridinyl]-benzonitrile, monohydrochloride
CAS Number
2436760-79-9
Molecular Formula
C24H23N3O • HCl
Formula Weight
405.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
CC(C=C1)=CC=C1C(N=C2)=C(C3=CC=C(C=C3)C#N)C=C2OC[C@@H]4CCNC4.Cl
InChi Code
InChI=1S/C24H23N3O.ClH/c1-17-2-6-21(7-3-17)24-23(20-8-4-18(13-25)5-9-20)12-22(15-27-24)28-16-19-10-11-26-14-19;/h2-9,12,15,19,26H,10-11,14,16H2,1H3;1H/t19-;/m1./s1
InChi Key
DBTSJYXXWZFXNJ-FSRHSHDFSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $49

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    5 mg

    $135

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    10 mg

    $221

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    25 mg

    $429

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    Product Description

    GSK690 is a lysine-specific demethylase 1 (LSD1) inhibitor (IC50 = 0.09 µM in a cell-free assay).1 It is selective for LSD1 over monoamine oxidase A (MAO-A; IC50 = >200 µM). GSK690 inhibits LSD1 activity in THP-1 acute myeloid leukemia cells (IC50 = 1.4 µM). GSK690 potentiates reductions in viability of SJCRH30 rhabdomyosarcoma cells induced by the histone deacetylase (HDAC) inhibitor JNJ-26481585 (Item No. 14088).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hitchin, J.R., Blagg, J., Burke, R., et al. Development and evaluation of selective, reversible LSD1 inhibitors derived from fragments. MedChemComm 4, 1513 (2013).

    2. Haydn, T., Metzger, E., Schuele, R., et al. Concomitant epigenetic targeting of LSD1 and HDAC synergistically induces mitochondrial apoptosis in rhabdomyosarcoma cells. Cell Death Dis. 8(6), e2879 (2017).