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64048-12-0

中文名稱 4,44喬,4喬(2,3,4,5-Thiophentetrayl)tetrakis-pyridine
英文名稱 2,3,4,5-TETRA-(4-PYRIDYL) THIOPHENE
CAS 64048-12-0
分子式 C24H16N4S
分子量 392.48
MOL 文件 64048-12-0.mol
更新日期 2024/12/26 10:14:08
64048-12-0 結構式 64048-12-0 結構式

基本信息

中文別名
2,3,4,5-四-(4-吡啶)噻吩
2,3,4,5-四(4-吡啶基)噻吩
4,4?4喬,4喬?(2,3,4,5-Thiophentetrayl)tetrakis-pyridine
英文別名
¥
GANT58
,4¥
4,4¥
Nsc75503
Hh/Gli Antagonist, GANT58
2,3,4,5-TETRA-(4-PYRIDYL) THIOPHENE
1,2,3,4-Tetrakis(4-pyridyl)thiophene
GANT58 (2,3,4,5-Tetra(4-pyridyl)thiophene
-(2,3,4,5-Thiophentetrayl)tetrakis-pyridine
所屬類別
生物化工:激動劑抑制劑

物理化學性質

熔點252-253℃
沸點414.1±40.0 °C(Predicted)
密度1.254
儲存條件Keep in dark place,Sealed in dry,2-8°C
溶解度二甲基亞砜:>10mg/mL
酸度系數(pKa)4.50±0.10(Predicted)
形態(tài)黃色固體
顏色白色至淡黃色

安全數據

WGK Germany3
4,44喬,4喬(2,3,4,5-Thiophentetrayl)tetrakis-pyridine價格(試劑級)
報價日期產品編號產品名稱CAS號包裝價格
2024/11/08HY-132824,44喬,4喬(2,3,4,5-Thiophentetrayl)tetrakis-pyridine
GANT 58
64048-12-05mg512元
2024/11/08HY-132824,44喬,4喬(2,3,4,5-Thiophentetrayl)tetrakis-pyridine
GANT 58
64048-12-010mM * 1mLin DMSO563元
2024/11/08HY-132824,44喬,4喬(2,3,4,5-Thiophentetrayl)tetrakis-pyridine
GANT 58
64048-12-010mg818元

常見問題列表

生物活性
GANT 58 是一種有效的 Gli 拮抗劑,抑制 GLI1 誘導的轉錄,IC50 為 5 μM。
靶點

IC50: 5 μM (Gli)

體外研究

GANT58 is a downstream inhibitor of Hh signaling. GANT58 is an indeed inhibitor of Hh signaling downstream of Smo and Sufu. GANT58 mainly acts at the nuclear level because transcription induced by GLI1 with a mutated nuclear export signal is still blocked. GANT58 efficiently inhibits in vitro tumor cell proliferation in a GLI-dependent manner and successfully blocks cell growth using human prostate cancer cells harboring downstream activation of the Hh pathway. GANT58 (NSC75503) has been shown to inhibit transcriptional activation by GLI1 (as well as by the other GLI species). GANT58 has been shown to inhibit GLI transactivation.

體內研究

Nude mice are injected s.c. with GLI1-positive 22Rv1 prostate cancer cells, and tumors are established (median size ≈250 mm 3 ). Nude mice are treated with daily s.c. injections at a concentration of 50 mg/kg of cyclopamine, GANT61, GANT58, or solvent only (n=4-5 for each group). However, after 3 days, cyclopamine-treated animals presented with severe ulcerations at the injection sites. Therefore, changing the treatment regimen to injections only every second day. To be able to compare all compounds, this protocol is also introduced for the GANTs, although mice treated with these compounds showed no such signs of toxicity. All injections are done 2-3 cm away from the tumors. During an 18-day treatment period, suppression of tumor cell growth is observed for all compounds. Treatment with cyclopamine or GANT58 results in the inhibition of additional xenograft growth and limited the increase in tumor size.

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