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  2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Anti-infection
  3. HSP Bacterial Antibiotic Parasite
  4. Radicicol

Radicicol  (Synonyms: 根赤殼菌素; Monorden)

目錄號(hào): HY-N6769 純度: 99.63%
COA 產(chǎn)品使用指南 技術(shù)支持

Radicicol 是一種 Hsp90 抑制劑，導(dǎo)致蛋白酶體降解，IC50 <1 μM。Radicicol 抑制 PDK，IC50 為 230 μM (PDK1) 和 400 μM (PDK3)。Radicicol 也是一種抗真菌和抗瘧疾的抗生素，通過(guò)靶向惡性瘧原蟲(chóng)的拓?fù)洚悩?gòu)酶 VIB 破壞線粒體復(fù)制。Radicicol 還抑制脂肪團(tuán)和肥胖相關(guān)蛋白 (FTO)，IC50 為 16.04 μM。

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Radicicol Chemical Structure

Radicicol Chemical Structure

CAS No. : 12772-57-5

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規(guī)格 價(jià)格 是否有貨 數(shù)量
1 mg ￥1950
In-stock
5 mg ￥4800
In-stock
10 mg   詢價(jià)  
50 mg   詢價(jià)  

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Customer Review

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Radicicol is an inhibitor of Hsp90 with an IC50 value < 1 μM, and leads to proteasomal degradation[1]. Radicicol exhibits inhibition on PDK with IC50s of 230 μM (PDK1) and 400 μM (PDK3). Radicicol is an antifungal and antimalarial antibiotic, impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB[2]. Radicicol is also an inhibitor of fat mass and obesity-associated protein (FTO), with an IC50 value of 16.04 μM[3].

IC50 & Target

HSP90

1 μM (IC50)

Plasmodium

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
3Y1 cell line IC50
0.7 μM
Compound: 1 (radicicol)
Concentration to inhibit growth of normal rat fibroblast cells (3Y1-B cells) after 72 h exposure
Concentration to inhibit growth of normal rat fibroblast cells (3Y1-B cells) after 72 h exposure
[PMID: 12773056]
A549 IC50
0.1 μM
Compound: 14
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
[PMID: 28749671]
A549 GI50
1.43 μM
Compound: Radicicol
Growth inhibition of human A549 cells after 48 hrs by SRB assay
Growth inhibition of human A549 cells after 48 hrs by SRB assay
[PMID: 24797798]
HeLa IC50
0.1 μM
Compound: 14
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
[PMID: 28749671]
J774.A1 IC50
2.35 μM
Compound: Radicicol
Cytotoxicity against mouse J774.A1 cells after 72 hrs by MTS assay
Cytotoxicity against mouse J774.A1 cells after 72 hrs by MTS assay
[PMID: 28835791]
MCF7 IC50
0.03 μM
Compound: 1
Antiproliferative activity against human MCF7 cells by MTT assay
Antiproliferative activity against human MCF7 cells by MTT assay
[PMID: 16499313]
MCF7 IC50
0.0892 μM
Compound: 2, RDC
Cytotoxicity against human MCF7 cells after 24 hrs
Cytotoxicity against human MCF7 cells after 24 hrs
[PMID: 18487051]
MCF7 IC50
0.4 μM
Compound: 14
Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
[PMID: 28749671]
NRK IC50
0.29 μM
Compound: 1 (radicicol)
Concentration to inhibit growth of normal rat kidney epithelial cells (NRK cells) after 72 hr exposure
Concentration to inhibit growth of normal rat kidney epithelial cells (NRK cells) after 72 hr exposure
[PMID: 12773056]
SK-BR-3 IC50
0.00364 μM
Compound: 2, RDC
Cytotoxicity against human SKBR3 cells after 24 hrs
Cytotoxicity against human SKBR3 cells after 24 hrs
[PMID: 18487051]
T-cell EC50
9.1 μM
Compound: 1, monorden
Reactivation of latent HIV1 NL4-3-Luc expression in human naive CD4+ T cells treated 7 days post-infection measured after 48 hrs by luminescence plate reader analysis
Reactivation of latent HIV1 NL4-3-Luc expression in human naive CD4+ T cells treated 7 days post-infection measured after 48 hrs by luminescence plate reader analysis
[PMID: 24495105]
Vero IC50
0.2 μM
Compound: 1
Antiviral activity against HSV1 F infected in african green monkey Vero cells assessed as reduction of virus-induced cytopathic effect by cellular replication assay
Antiviral activity against HSV1 F infected in african green monkey Vero cells assessed as reduction of virus-induced cytopathic effect by cellular replication assay
[PMID: 12828470]
體外研究
(In Vitro)

Radicicol (1 μM 或 100 μM) 通過(guò)阻斷 ATP 結(jié)合來(lái)抑制 Hsp90 和 Topo VI 的活性[1]。
Radicicol (100 μM；10 分鐘) 結(jié)合 ATP 結(jié)合位點(diǎn)PDK3 的 C 端結(jié)構(gòu)域并阻止Hsp90 課題[1]的成熟。
Radicicol (0.25-18 μM；48 h) 抑制 P. falciparum 生長(zhǎng)，IC50 值為 8.563 μM，并且 (8 μM；50 h) 延遲了裂殖體到環(huán)的轉(zhuǎn)變[2]。
Radicicol (1.5 μM；40 h) 抑制線粒體 DNA 復(fù)制而不影響細(xì)胞核和頂端質(zhì)體基因組[2]。
Radicicol (0.001-5 μM；72 h) 誘導(dǎo)成肌細(xì)胞分化成肌細(xì)胞，毒性濃度為0.1 μM[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: P. falciparum?3D7
Concentration: 0.25 μM, 0.75 μM, 2 μM, 4 μM, 6 μM, 8 μM, 10 μM, 14 μM, 17 μM
Incubation Time: 48 hours
Result: Showed a dose-dependent inhibitory effect on parasite growth.

Cell Cytotoxicity Assay[5]

Cell Line: Primary myoblasts (from mice hindlimb muscles)
Concentration: 0.001, 0.01, 0.1, 1, 5 μM
Incubation Time: 72 hours
Result: Induced myoblast differentiation with a highest concentration of not inducing myoblast toxicity of 0.1 μM.
體內(nèi)研究
(In Vivo)

Radicicol (20 mg/kg or 60 mg/kg；腹腔注射；2次給藥；前后1 h) 具有腎臟保護(hù)作用，改善腎缺血再灌注 (I/R) 損傷，增加腎損傷小鼠腎臟 HSP70 mRNA 和蛋白[4]。
Radicicol (0.05 mg/20 g；皮下注射；單劑量) 通過(guò)降低 NF-kB 激活增強(qiáng)受到響尾蛇毒素?fù)p傷的骨骼肌的再生[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Renal I/R injury model in mice[4]
Dosage: 20 mg/kg or 60 mg/kg
Administration: Intraperitoneal injection; twice dosages; 1 h before and just after bilateral renal ischemia reperfusion (I/R)
Result: Showed renoprotection effect by inducing renal HSP70 expressing.
Animal Model: Male C57B1/6 mice (3-month-old, 25±2 g)[5]
Dosage: 0.05 mg/20 g
Administration: Subcutaneous injection; single dose; immediately before CTX injury (~1 min); evaluated on day one or 10 after injection
Result: Resulted heat shock protein induction and decreased NF-kB activation in muscle injured by crotoxin at days 10.
Improved the size recovery of regenerating myofibers and decreased NF-kB activation.
分子量

364.78

Formula

C18H17ClO6
CAS 號(hào)
性狀

固體

顏色

White to off-white

中文名稱

根赤殼菌素
結(jié)構(gòu)分類
初始來(lái)源
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 100 mg/mL (274.14 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.7414 mL 13.7069 mL 27.4138 mL
5 mM 0.5483 mL 2.7414 mL 5.4828 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.63%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7414 mL 13.7069 mL 27.4138 mL 68.5345 mL
5 mM 0.5483 mL 2.7414 mL 5.4828 mL 13.7069 mL
10 mM 0.2741 mL 1.3707 mL 2.7414 mL 6.8534 mL
15 mM 0.1828 mL 0.9138 mL 1.8276 mL 4.5690 mL
20 mM 0.1371 mL 0.6853 mL 1.3707 mL 3.4267 mL
25 mM 0.1097 mL 0.5483 mL 1.0966 mL 2.7414 mL
30 mM 0.0914 mL 0.4569 mL 0.9138 mL 2.2845 mL
40 mM 0.0685 mL 0.3427 mL 0.6853 mL 1.7134 mL
50 mM 0.0548 mL 0.2741 mL 0.5483 mL 1.3707 mL
60 mM 0.0457 mL 0.2284 mL 0.4569 mL 1.1422 mL
80 mM 0.0343 mL 0.1713 mL 0.3427 mL 0.8567 mL
100 mM 0.0274 mL 0.1371 mL 0.2741 mL 0.6853 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Radicicol
目錄號(hào)：
HY-N6769
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