Merck

SML3321

Sigma-Aldrich

GK921

≥98% (HPLC)

別名:
3-(2-Phenylethynyl)-2-[2-(1-pyrrolidinyl)ethoxy]pyrido[2,3-b]pyrazine, 3-(Phenylethynyl)-2-(2-(pyrrolidin-1-yl)ethoxy)pyrido[3,2-b]pyrazine, GK 921, GK-921
Empirical Formula (Hill Notation):
C21H20N4O
CAS番号:
分子量:
344.41
MDL番号:

品質水準

アッセイ

≥98% (HPLC)

形状

powder

, Faint yellow to very dark orange

溶解性

DMSO: 2 mg/mL, clear (Warmed)

保管温度

2-8°C

InChI

1S/C21H20N4O/c1-2-7-17(8-3-1)10-11-19-21(26-16-15-25-13-4-5-14-25)24-18-9-6-12-22-20(18)23-19/h1-3,6-9,12H,4-5,13-16H2

InChI key

MNYJJHBAEYKXEG-UHFFFAOYSA-N

類似品目との比較

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当該品目
SML2445SML2448R2033
GK921 ≥98% (HPLC)

Sigma-Aldrich

SML3321

GK921

PKS21004 ≥98% (HPLC)

Sigma-Aldrich

SML2445

PKS21004

PK4C9 ≥98% (HPLC)

Sigma-Aldrich

SML2448

PK4C9

RK-682 ≥98% (HPLC)

Sigma-Aldrich

R2033

RK-682

form

powder

form

powder

form

powder

form

powder

color

, Faint yellow to very dark orange

color

white to beige

color

white to very dark brown

color

white to tan

solubility

DMSO: 2 mg/mL, clear (Warmed)

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO, heptane and xylene: ≥8 mg/mL

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

−20°C

Quality Level

100

Quality Level

-

Quality Level

-

Quality Level

100

生物化学的/生理学的作用

GK921 is an orally active transglutaminase 2 (TG2, TGase 2) inhibitor (IC50 = 7.71 μM) that effectively inhibits TG2-mediated I-κBα and p53 polymerization. GK921 induces growth arrest/cell death in renal cell carcinoma (RCC) cultures (ave GI50 = 9.05 μM) and abrogates RCC with increase in p53 level in mice in vivo (8 mg/kg 5x per wk; ACHN or CAKI-1 cells).

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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  • もしTO09019TOなどのロット番号を見つけた場合は、最初の2文字を除いたロット番号09019TOを入力します。

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Tracy J Berg et al.
Cancer research, 81(8), 2101-2115 (2021-01-24)
The tumor microenvironment plays an essential role in supporting glioma stemness and radioresistance. Following radiotherapy, recurrent gliomas form in an irradiated microenvironment. Here we report that astrocytes, when pre-irradiated, increase stemness and survival of cocultured glioma cells. Tumor-naïve brains increased
Yuanyuan Hou et al.
Journal of immunology research, 2021, 4754454-4754454 (2021-09-07)
Propofol is a known intravenous hypnotic drug used for induction and maintenance of sedation and general anesthesia. Emerging studies also reveal a neuroprotective effect of propofol in diverse diseases of neuronal injuries via modulating microglia activation. In this study, we
Bo Mi Ku et al.
Journal of cancer research and clinical oncology, 140(5), 757-767 (2014-03-13)
To test whether transglutaminase 2 (TGase 2) inhibitor GK921 alone reverses renal cell carcinoma (RCC) tumor growth. RCC is resistant to both radiation and chemotherapy, and the prognosis remains poor. Despite the recent therapeutic success of vascular endothelial growth factor

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