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Merck
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重要文件

SML2419

Sigma-Aldrich

GSK690

≥98% (HPLC)

同義詞:

(R)-4-(5-(Pyrrolidin-3-ylmethoxy)-2-(p-tolyl)pyridin-3-yl) benzonitrile), (R)-4-(5-(Pyrrolidin-3-ylmethoxy)-2-p-tolylpyridin-3-yl)benzonitrile, 4-(2-(4-Methylphenyl)-5-((3R)-3-pyrrolidinylmethoxy)-3-pyridinyl)benzonitrile, GSK 354, GSK 690, GSK-354, GSK-690, GSK354

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About This Item

經驗公式(希爾表示法):
C24H23N3O
CAS號碼:
分子量::
369.46
分類程式碼代碼:
12352200
暫時無法取得訂價和供貨情況

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

2-8°C

SMILES 字串

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

InChI

1S/C24H23N3O/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/t19-/m1/s1

InChI 密鑰

IQVDLEXWAPYWDT-LJQANCHMSA-N

相關類別

生化/生理作用

GSK690 (GSK354) is a cell-permeable pyrrolidinylmethoxypyridine-based compound that inhibits lysine-specific demethylase 1 (LSD1; KDM1A) in a potent and reversible manner (IC50 = 90 nM) without affecting MAO-A activity (IC50 >200 μM). GSK690 is shown to induce the expressions of CD86 (EC50 = 1.4 μM in THP1 cells) and LY96 (EC50 = 423 nM in MV4-11 cells), and prevent adipogenesis in murine preadipocyte cultures.
Potent and reversible lysine-specific demethylase LSD1 (KDM1A) inhibitor that induces CD86 and LY96 expression and prevents adipogenesis.

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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Development and evaluation of selective, reversible LSD1 inhibitors derived from fragments
Hitchin JR, Blagg J, Burke R .
Medicinal Chemistry, 1513-1522 (2013)
Daniel P Mould et al.
Journal of medicinal chemistry, 60(19), 7984-7999 (2017-09-12)
Inhibition of lysine specific demethylase 1 (LSD1) has been shown to induce the differentiation of leukemia stem cells in acute myeloid leukemia (AML). Irreversible inhibitors developed from the nonspecific inhibitor tranylcypromine have entered clinical trials; however, the development of effective
Tinka Haydn et al.
Cell death & disease, 8(6), e2879-e2879 (2017-06-16)
The lysine-specific demethylase 1 (LSD1) is overexpressed in several cancers including rhabdomyosarcoma (RMS). However, little is yet known about whether or not LSD1 may serve as therapeutic target in RMS. We therefore investigated the potential of LSD1 inhibitors alone or
Alba Maiques-Diaz et al.
Cell reports, 22(13), 3641-3659 (2018-03-29)
Pharmacologic inhibition of LSD1 promotes blast cell differentiation in acute myeloid leukemia (AML) with MLL translocations. The assumption has been that differentiation is induced through blockade of LSD1's histone demethylase activity. However, we observed that rapid, extensive, drug-induced changes in transcription occurred
John P McGrath et al.
Cancer research, 76(7), 1975-1988 (2016-02-04)
Lysine-specific demethylase 1 (KDM1A) is a transcriptional coregulator that can function in both the activation and repression of gene expression, depending upon context. KDM1A plays an important role in hematopoiesis and was identified as a dependency factor in leukemia stem

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