Merck
  • SML1659
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SML1659

Sigma-Aldrich

NCT-503

≥98% (HPLC)

Synonym(s):
N-(4,6-ジメチルピリジン-2-イル)-4-(4-(トリフルオロメチル)ベンジル)ピペラジン-1-カルボチオアミド
Empirical Formula (Hill Notation):
C20H23F3N4S
CAS Number:
Molecular Weight:
408.48
PubChem Substance ID:
NACRES:
NA.77

品質水準

アッセイ

≥98% (HPLC)

形状

powder

white to beige

溶解性

DMSO: 10 mg/mL, clear

保管温度

2-8°C

SMILES string

CC1=CC(NC(N2CCN(CC3=CC=C(C(F)(F)F)C=C3)CC2)=S)=NC(C)=C1

InChI

1S/C20H23F3N4S/c1-14-11-15(2)24-18(12-14)25-19(28)27-9-7-26(8-10-27)13-16-3-5-17(6-4-16)20(21,22)23/h3-6,11-12H,7-10,13H2,1-2H3,(H,24,25,28)

InChI key

PJNSZIQUFLWRLH-UHFFFAOYSA-N

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NCT-503 ≥98% (HPLC)

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assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥97% (NMR)

form

powder

form

powder

form

powder

form

powder

color

white to beige

color

white to beige

color

white to beige

color

light orange to dark orange

solubility

DMSO: 10 mg/mL, clear

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO: 5 mg/mL (clear solution)

storage temp.

2-8°C

storage temp.

−20°C

storage temp.

2-8°C

storage temp.

2-8°C

Quality Level

100

Quality Level

-

Quality Level

100

Quality Level

100

生物化学的/生理学的作用

NCT-503は、ホスホグリセリン酸デヒドロゲナーゼ(PHGDH)の阻害剤であり、グルコース由来のセリン合成の最初の律速段階を触媒します。 NCT-503は、グルコース由来のセリン産生を減少させ、培養および異種移植腫瘍におけるPHGDH依存性がん細胞の両方の増殖を抑制し、MDA-MB-468細胞のG1/S細胞周期停止を引き起こしました。 NCT-503は、グルコース由来および外因性セリンからヌクレオチドへの1炭素単位の取込みを減少させたので、その抗がん活性に寄与する可能性があります。 NCT-503は、PHGDHのIC50値が2.5 μMであり、他のデヒドロゲナーゼのパネルに対して不活性で、168のGタンパク質共役型受容体(GPCR)のパネルにおける交差反応性は最小限でした。 NCT-503は、3-PGとNAD+の両方に関して非競合的であり、良好な安定性(アッセイ緩衝液中で48時間後に>98%)と水溶性を示すことが認められました。

おすすめ製品

NCT-503の構造的に同様の類似体であるNCT-503 Inactive Control(NCT-503不活性コントロール)は、シグマから入手できます。NCT-503不活性コントロールの詳細と購入については、ここをクリックしてください

ピクトグラム

Exclamation mark

シグナルワード

Warning

危険有害性情報

危険有害性の分類

Skin Irrit. 2

保管分類コード

11 - Combustible Solids

WGK

WGK 3

引火点(°F)

Not applicable

引火点(℃)

Not applicable


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