标签归档：tryptophan

多肽定制Tryptophan Motif Peptide 编码

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名称 Tryptophan Motif Peptide
编码
别名 Tryptophan Motif Peptide
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） GGWSHW-NH2
序列（三字母缩写） H-Gly-Gly-Trp-Ser-His-Trp-NH2?(trifluoroacetate salt)
基本描述 TP-5
溶解度
分子量 727.79
化学式 C35H41N11O7
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents Tryptophan Motif Peptide 编码
Figures Tryptophan Motif Peptide 编码
Reference Sipes, J. J. Cell Biol. 121, 469 (1993) Shultz-Cherry, S. et al. J. Biol. Chem. 270, 7304 (1995)
C端
N端
化学桥

RG108(Synonyms: N-Phthalyl-L-tryptophan)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

RG108 (Synonyms: N-Phthalyl-L-tryptophan) 纯度: 99.61%

RG108 (N-Phthalyl-L-tryptophan) 是一种非核苷的 DNA 甲基转移酶 (DNMTs) 抑制剂 (IC50=115 nM)，RG108 (N-Phthalyl-L-tryptophan) 阻断 DNA 甲基转移酶的活性位点。RG108 (N-Phthalyl-L-tryptophan) 引起抑癌基因的去甲基化和再激活，但不影响着丝粒卫星序列的甲基化。

RG108(Synonyms: N-Phthalyl-L-tryptophan)

RG108 Chemical Structure

CAS No. : 48208-26-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥932 In-stock
10 mg ￥847 In-stock
50 mg ￥3530 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

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生物活性

RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC50=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences[1][2][3].

IC50 & Target[1]

CpG methylase M.SssI

115 nM (IC50)

体外研究
(In Vitro)

RG108 effectively blocks DNA methyltransferases in vitro and does not cause covalent enzyme trapping in human cell lines. Incubation of cells with low micromolar concentrations of RG108 results in significant demethylation of genomic DNA without any detectable toxicity. Intriguingly, RG108 causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences[1]. In another study, the synthesis and in vitro analysis of a biotinylated RG108 conjugate is investigated to evaluate the interactions with DNA methyltransferase enzymes[2]. In a recent study, it is shown RG108 can significantly reduce the DNA methyltransferases activity in SM derived iPS cells as compared to the native SMs[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

334.33

Formula

C19H14N2O4
CAS 号

48208-26-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (299.11 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9911 mL 14.9553 mL 29.9106 mL
5 mM 0.5982 mL 2.9911 mL 5.9821 mL
10 mM 0.2991 mL 1.4955 mL 2.9911 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (6.22 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.22 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (6.22 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.22 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.22 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.22 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

  • 4.

    请依序添加每种溶剂： PBS

    Solubility: 1 mg/mL (2.99 mM); Clear solution; Need ultrasonic and warming and heat to 70°C

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Brueckner B, et al. Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases. Cancer Res. 2005 Jul 15;65(14):6305-11.

    [2]. Schirrmacher E, et al. Synthesis and in vitro evaluation of biotinylated RG108: a high affinity compound for studying binding interactions with human DNA methyltransferases. Bioconjug Chem. 2006 Mar-Apr;17(2):261-6.

    [3]. Pasha Z, et al. Efficient non-viral reprogramming of myoblasts to stemness with a single small molecule to generate cardiac progenitor cells. PLoS One. 2011;6(8):e23667.
Kinase Assay
[1]

The substrate DNA for the in vitro methylation assay is a 798 bp fragment (−423/+375 relative to the initiation codon) from the promoter region of the human p16Ink4a gene. The methylation reaction contains 350 to 400 ng substrate DNA and 4 units of M.SssI methylase (0.5 μM) in a final volume of 50 μL. Inhibitors are added to final concentrations of 10, 100, 200, and 500 μM, respectively. Reactions are done at 37°C for 2 hours. After completion, the reaction is inactivated at 65°C for 15 minutes and the DNA is purified using PCR Purification kit. Three hundred nanograms of purified DNA is digested for 3 hours at 60°C with 30 units of BstUI and analyzed on 2% Tris-borate EDTA agarose gels.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Brueckner B, et al. Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases. Cancer Res. 2005 Jul 15;65(14):6305-11.

    [2]. Schirrmacher E, et al. Synthesis and in vitro evaluation of biotinylated RG108: a high affinity compound for studying binding interactions with human DNA methyltransferases. Bioconjug Chem. 2006 Mar-Apr;17(2):261-6.

    [3]. Pasha Z, et al. Efficient non-viral reprogramming of myoblasts to stemness with a single small molecule to generate cardiac progenitor cells. PLoS One. 2011;6(8):e23667.

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Indoximod(Synonyms: 1-Methyl-D-tryptophan; NLG-8189)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Indoximod (Synonyms: 1-Methyl-D-tryptophan; NLG-8189) 纯度: 99.39%

Indoximod (1-Methyl-D-tryptophan) 是一种具有口服活性的吲哚胺2,3-双加氧酶(IDO) 途径抑制剂。Indoximod 充当Trp模拟物，调节mTOR中。Indoximod 是一种可用于癌症研究的免疫代谢佐剂。

Indoximod(Synonyms: 1-Methyl-D-tryptophan; NLG-8189)

Indoximod Chemical Structure

CAS No. : 110117-83-4

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250 mg ￥500 In-stock
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  • Targeted Diversity Library
  • Rare Diseases Drug Library

生物活性

Indoximod (1-Methyl-D-tryptophan) is an orally active indoleamine 2,3-dioxygenase (IDO) pathway inhibitor. Indoximod acts as a Trp mimetic in regulating mTOR. Indoximod is an immunometabolic adjuvant used for the research of cancer[1][2].

IC50 & Target[1]

IDO

19 μM (Ki)

体外研究
(In Vitro)

The IDO inhibitor 1-methyl-tryptophan exists in two stereoisomers with potentially different biological properties. The L isomer is the more potent inhibitor of IDO activity using the purified enzyme and in HeLa cell–based assays. However, the D isomer is significantly more effective in reversing the suppression of T cells created by IDO-expressing dendritic cells. The L isomer of 1-methyl-tryptophan functioned as a competitive inhibitor (Ki=19 μM), whereas the d isomer is much less effective. The DL mixture is intermediate, with a Ki of 35 μM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

The D isomer is more efficacious as an anticancer agent in chemo-immunotherapy regimens using NSC-26271, NSC 125973, or LY 188011, when tested in mouse models of transplantable melanoma and transplantable and autochthonous breast cancer. The D isomer of 1-methyl-tryptophan specifically targets the IDO gene because the antitumor effect of d-1-methyl-tryptophan is completely lost in mice with a disruption of the IDO gene (IDO-knockout mice). Oral administration of dl-1-methyl-tryptophan in combination with NSC 125973 can elicit regression of autochthonous breast tumors[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

218.25

Formula

C12H14N2O2
CAS 号

110117-83-4
中文名称

1-甲基-D-色氨酸
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

H2O : 5 mg/mL (22.91 mM; ultrasonic and adjust pH to 2 with HCl)

DMSO : 0.55 mg/mL (2.52 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.5819 mL 22.9095 mL 45.8190 mL
5 mM 0.9164 mL 4.5819 mL 9.1638 mL
10 mM 0.4582 mL 2.2910 mL 4.5819 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Hou DY, et al. Inhibition of indoleamine 2,3-dioxygenase in dendritic cells by stereoisomers of 1-methyl-tryptophancorrelates with antitumor responses. Cancer Res. 2007 Jan 15;67(2):792-801.

    [2]. Metz R, et al. IDO inhibits a tryptophan sufficiency signal that stimulates mTOR: A novel IDO effector pathway targeted by D-1-methyl-tryptophan. Oncoimmunology. 2012;1(9):1460-1468.

Kinase Assay
[1]

1MT enantiomers are solubilized in DMSO containing 0.1N HCl and added at concentrations of 100, 50, and 0 µM to wells containing the reaction mixture with tryptophan (0-200 µM) followed by addition of IDO enzyme. Plates are sealed and incubated 1 hr in a humidified 37°C incubator, after which the reactions are terminated by addition of 12.5 µl 30% TCA per well. Plates are then resealed in plastic wrap, incubated 30 min at 50°C to hydrolyze the reaction product N-formylkynurenine to kynurenine, and centrifuged. Supernatants are transferred to a flat-bottom 96-well plate, mixed with 100 µl Ehrlich reagent and incubated 10 min at room temperature. Absorbance at 490 nm is read[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Hou DY, et al. Inhibition of indoleamine 2,3-dioxygenase in dendritic cells by stereoisomers of 1-methyl-tryptophancorrelates with antitumor responses. Cancer Res. 2007 Jan 15;67(2):792-801.

    [2]. Metz R, et al. IDO inhibits a tryptophan sufficiency signal that stimulates mTOR: A novel IDO effector pathway targeted by D-1-methyl-tryptophan. Oncoimmunology. 2012;1(9):1460-1468.

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(S)-Indoximod(Synonyms: 1-Methyl-L-tryptophan; (S)-NLG-8189)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

(S)-Indoximod (Synonyms: 1-Methyl-L-tryptophan; (S)-NLG-8189) 纯度: 99.03%

(S)-Indoximod (1-Methyl-L-tryptophan) 是吲哚胺-2,3-双加氧酶 (IDO) 抑制剂。(S)-Indoximod 可用于癌症研究。

(S)-Indoximod(Synonyms: 1-Methyl-L-tryptophan; (S)-NLG-8189)

(S)-Indoximod Chemical Structure

CAS No. : 21339-55-9

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
100 mg ￥500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

(S)-Indoximod 相关产品

•相关化合物库:

  • Natural Product Library Plus
  • Bioactive Compound Library Plus

生物活性

(S)-Indoximod (1-Methyl-L-tryptophan) is an inhibitor of indoleamine 2,3-dioxygenase (IDO). (S)-Indoximod can be used for the research of cancer[1][2].

IC50 & Target

Indoleamine 2,3-Dioxygenase (IDO)[1]
分子量

218.25

Formula

C12H14N2O2
CAS 号

21339-55-9
中文名称

相思豆碱
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性数据
In Vitro: 

DMSO : 5 mg/mL (22.91 mM; ultrasonic and adjust pH to 5 with HCl)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.5819 mL 22.9095 mL 45.8190 mL
5 mM 0.9164 mL 4.5819 mL 9.1638 mL
10 mM 0.4582 mL 2.2910 mL 4.5819 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Huang GL, et, al. PEG-Poly(1-Methyl-l-Tryptophan)-Based Polymeric Micelles as Enzymatically Activated Inhibitors of Indoleamine 2,3-Dioxygenase. Nanomaterials (Basel). 2019 May 9;9(5):719.

    [2]. Liu X, et, al. 1-L-MT, an IDO inhibitor, prevented colitis-associated cancer by inducing CDC20 inhibition-mediated mitotic death of colon cancer cells. Int J Cancer. 2018 Sep 15;143(6):1516-1529.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务