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Merck
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Key Documents

SML2074

Sigma-Aldrich

FX1

≥98% (HPLC)

別名:

(5Z)-5-(5-Chloro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)-4-oxo-2-thioxo-3-thiazolidinepropanoic acid, (Z)-3-(5-(5-Chloro-2-oxoindolin-3-ylidene)-4-oxo-2-thioxothiazolidin-3-yl)propanoic acid

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About This Item

実験式（ヒル表記法）:
C14H9ClN2O4S2
CAS番号:
1426138-42-2
分子量:
368.82
UNSPSCコード:
12352200
NACRES:
NA.77

アッセイ

≥98% (HPLC)

形状

powder

色

red-brown

保管温度

2-8°C

関連するカテゴリー

生物化学的／生理学的作用

FX1 is a BCL6 inhibitor that effectively blocks BCL6 N-terminal BTB domain-mediated corepressors chromosome recruitment (by 61-87%/SMRT and 67-82%/BCOR; 50 μM FX1 for 30 min) and selectively suppresses BCL6-depenent growth (GI50 16-54 μM; >125 μM against BCL6-independent cells) in diffuse large B cell lymphoma (DLBCL) cultures, exhibiting greater affinity than its structure analog 79-6 or BCL6 corepressor SMRT for BTB domain (KD = 7 μM/FX1, 30 μM/SMRT, 129 μM/79-6). FX1 shows greater efficacy than 79-6 in reversing BCL6/corepressors-mediated target genes repression in vitro (IC50 = 35 μM vs. 318 μM with 79-6 by HEK293T-based reporter assay) and in suppressing OCI-Ly7 DLBCL xenograft tumor growth mice in vivo (100% vs. 45% suppression with respective compound via 25 mg/kg/day i.p.).

保管分類コード

11 - Combustible Solids

WGK

WGK 3

引火点(°F)

Not applicable

引火点(℃)

Not applicable

試験成績書（COA）

製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。

以前この製品を購入いただいたことがある場合

文書ライブラリで、最近購入した製品の文書を検索できます。

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Mariano G Cardenas et al.
The Journal of clinical investigation, 126(9), 3351-3362 (2016-08-03)
Diffuse large B cell lymphomas (DLBCLs) arise from proliferating B cells transiting different stages of the germinal center reaction. In activated B cell DLBCLs (ABC-DLBCLs), a class of DLBCLs that respond poorly to current therapies, chromosomal translocations and amplification lead
William McCoull et al.
Journal of medicinal chemistry, 60(10), 4386-4402 (2017-05-10)
Inhibition of the protein-protein interaction between B-cell lymphoma 6 (BCL6) and corepressors has been implicated as a therapeutic target in diffuse large B-cell lymphoma (DLBCL) cancers and profiling of potent and selective BCL6 inhibitors are critical to test this hypothesis.
H S Madapura et al.
Oncogene, 36(32), 4619-4628 (2017-04-04)
B-cell CLL/lymphoma 6 (BCL6) exerts oncogenic effects in several human hematopoietic malignancies including chronic myeloid leukemia (CML), where BCL6 expression was shown to be essential for CML stem cell survival and self-renewal during imatinib mesylate (IM) treatment. As several lines
Wendy Béguelin et al.
Cancer cell, 30(2), 197-213 (2016-08-10)
The EZH2 histone methyltransferase mediates the humoral immune response and drives lymphomagenesis through formation of bivalent chromatin domains at critical germinal center (GC) B cell promoters. Herein we show that the actions of EZH2 in driving GC formation and lymphoma

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