(S)-Coriolic acid(Synonyms: 13(S)-HODE)

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)-Coriolic acid (Synonyms: 13(S)-HODE)

(S)-Coriolic acid (13(S)-HODE) ,亚油酸的15-脂氧合酶 (15-LOX) 代谢产物,作为内源性配体激活 PPARγ。(S)-Coriolic acid 是一种重要的细胞内信号剂,在各种生物系统中参与细胞增殖和分化。(S)-Coriolic acid 诱导线粒体功能障碍 (mitochondrial dysfunction) 和气道上皮损伤。

(S)-Coriolic acid(Synonyms: 13(S)-HODE)

(S)-Coriolic acid Chemical Structure

CAS No. : 29623-28-7

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生物活性

(S)-Coriolic acid (13(S)-HODE), the product of 15-lipoxygenase (15-LOX) metabolism of linoleic acid, functions as the endogenous ligand to activate PPARγ. (S)-Coriolic acid is an important intracellular signal agent and is involved in cell proliferation and differentiation in various biological systems. (S)-Coriolic acid induces mitochondrial dysfunction and airway epithelial injury[1][2][3].

体外研究
(In Vitro)

(S)-Coriolic acid (25μM) causes mitochondrial structural alterations and injury in bronchial epithelium[2].
(S)-Coriolic acid (30 nM; 6 hours; E-FABP-/- keratinocytes) induces K1 expression through NF-κB activation. (S)-Coriolic acid increases the phosphorylation of IκBαat serine 32, which induces IκB degradation and thereby activates NF-κB. (S)-Coriolic acid also increases the phosphorylation of Ikkinase-bat tyrosine 199, which promotes IκBα phosphorylation and subsequent NF-kB activation[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

(S)-Coriolic acid (0-0.6 mg per mouse; Intranasally once a day for 3 consecutive days) causes severe airway dysfunction, airway neutrophilia, mitochondrial dysfunction and epithelial injury[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c mice (6-8 weeks)[2]
Dosage: 0-0.6 mg per mouse
Administration: Intranasally once a day for 3 consecutive days
Result: BALB/c mice developed features of mitochondrial dysfunction such as reduction in mitochondrial membrane potential, reduction in complex IV activity in lung mitochondria, and increase in the levels of cytochrome c in lung cytosol.

分子量

296.44

Formula

C18H32O3

CAS 号

29623-28-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Yuan H, et al. 15-Lipoxygenases and its metabolites 15(S)-HETE and 13(S)-HODE in the development of non-small cell lung cancer. Thorax. 2010;65(4):321-326.

    [2]. Mabalirajan U, et al. Linoleic acid metabolite drives severe asthma by causing airway epithelial injury. Sci Rep. 2013;3:1349.

    [3]. Ogawa E, et al. Epidermal FABP (FABP5) regulates keratinocyte differentiation by 13(S)-HODE-mediated activation of the NF-κB signaling pathway. J Invest Dermatol. 2011;131(3):604-612.

    [4]. Yuan H, et al. 15-Lipoxygenases and its metabolites 15(S)-HETE and 13(S)-HODE in the development of non-small cell lung cancer. Thorax. 2010;65(4):321-326.

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CHM-1(Synonyms: NSC656158)

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。

CHM-1 (Synonyms: NSC656158)

CHM-1 是一种微管失稳剂,可抑制微管蛋白聚合。CHM-1 是一种有效且选择性的抗人肝癌有丝分裂的抗肿瘤活性。CHM-1 通过激活 Cdc2 激酶活性诱导人肝癌细胞 G2-M 期阻滞,从而诱导细胞生长抑制和凋亡。

CHM-1(Synonyms: NSC656158)

CHM-1 Chemical Structure

CAS No. : 154554-41-3

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生物活性

CHM-1, a microtubule-destabilizing agent, inhibits tubulin polymerization. CHM-1 is a potent and selective antimitotic antitumor activity against human hepatocellular carcinoma. CHM-1 induces growth inhibition and apoptosis via G2-M phase arrest in human hepatocellular carcinoma cells by activation of Cdc2 kinase activity[1][2][3].

IC50 & Target

IC50: 0.75 μM (HA22T)[1]

体外研究
(In Vitro)

CHM-1 (0-100μM; 24 hours) induces significant concentration-dependent growth inhibition in HA22T, Hep3B, and HepG2 cells, with the most potent effects observed in HA22T cells (IC50 = 0.75 μM)[1].
CHM-1 (0-10 μM; 24 hours) significantly increases the binding of cyclin B1 to Cdc2 in HA22T cells[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.

Cell Viability Assay[1]

Cell Line: HA22T, Hep3B, and HepG2 cells
Concentration: 0-100 μM
Incubation Time: 24 hours
Result: Induced G2-M arrest of the cell cycle followed by apoptosis.

Western Blot Analysis[1]

Cell Line: HA22T cells
Concentration: 0-10 μM
Incubation Time: 24 hours
Result: Induced change in expressed and phosphorylated status of G2-M regulators in human hepatocellular carcinoma cells.

体内研究
(In Vivo)

CHM-1 (10 mg/kg; I.p.) induces a dose-dependent inhibition of HA22T tumor growth[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.

Animal Model: Male severe combined immunodeficient mice (HA22T)[1]
Dosage: 10 mg/kg
Administration: I.p.
Result: Induced a dose-dependent inhibition of HA22T tumor growth.

分子量

283.25

Formula

C16H10FNO3

CAS 号

154554-41-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Wang SW, et al. CHM-1, a novel synthetic quinolone with potent and selective antimitotic antitumor activity against human hepatocellular carcinoma in vitro and in vivo. Mol Cancer Ther. 2008 Feb;7(2):350-60.

    [2]. Liu CW, et al. CHM-1, a novel microtubule-destabilizing agent exhibits antitumor activity via inducing the expression of SIRT2 in human breast cancer cells. Chem Biol Interact. 2018 Jun 1;289:98-108.

    [3]. Tsai AC, et al. CHM-1, a new vascular targeting agent, induces apoptosis of human umbilical vein endothelial cells via p53-mediated death receptor 5 up-regulation. J Biol Chem. 2010 Feb 19;285(8):5497-506.

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MRTX849 acid

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。

MRTX849 acid 

MRTX849 acid 可用来合成PROTAC LC-2。LC-2 是一种有效且首创的 PROTAC,能够降解内源性 KRAS G12C (DC50,介于0.25 和0.76 μM之间)。

MRTX849 acid

MRTX849 acid Chemical Structure

CAS No. : 2561529-96-0

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生物活性

MRTX849 acid, a derivative of MRTX849, can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50s between 0.25 and 0.76 μM)[1][2].

IC50 & Target[1]

KRas G12C

 

体外研究
(In Vitro)

LC-2 induces degradation of endogenous KRASG12C in multiple KRAS mutant cancer cell (NCI-H2030, MIA PaCa-2, SW1573, NCI-H23 and NCI-H358 cells) with DC50s between 0.25 and 0.76 μM. LC-2-induced KRASG12C degradation occurs via a bona fide PROTAC mechanism. MIA PaCa-2, NCI-H23, and SW1573 cells are treated with 2.5 μM of LC-2 for 6, 24, 48, and 72 h. In all three cell lines, maximal KRAS degradation occurred within 24 h and was sustained up to 72 h[1].
LC-2-induced (2.5 μM; 6-24 hours) KRAS G12C degradation modulates Erk signaling in homozygous and heterozygous KRAS mutant cell lines[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

662.15

Formula

C34H37ClFN7O4

CAS 号

2561529-96-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Bond MJ, et al. Targeted Degradation of Oncogenic KRASG12C by VHL-Recruiting PROTACs. ACS Cent Sci. 2020;6(8):1367-1375.

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Harmane-d2(Synonyms: 哈尔满碱 d2)

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。

Harmane-d2 (Synonyms: 哈尔满碱 d2)

Harmane-d2 是 Harmane 的氘代物。Harmane,一种 β-咔啉生物碱 (BCA),是有效的神经毒素,可引起严重的动作震颤和精神病学表现。Harmane 对 I1 咪唑啉受体 (I1-Imidazoline receptor, IC50=30 nM) 的选择性是对 α2-肾上腺素受体 (IC50=18 μM) 的 1000 倍。Harmane 还是有效和选择性的单胺氧化酶抑制剂 (对 MAO A/BIC50 值分别为 0.5 μM 和 5 μM)。

Harmane-d2(Synonyms: 哈尔满碱 d2)

Harmane-d2 Chemical Structure

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生物活性

Harmane-d2 is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively)[1][2][3][4].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

184.23

Formula

C12H8D2N2

中文名称

哈尔满碱 d2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Louis ED, et, al. Blood harmane concentrations and dietary protein consumption in essential tremor. Neurology. 2005 Aug 9;65(3):391-6.

    [3]. Musgrave IF, et, al. Harmane produces hypotension following microinjection into the RVLM: possible role of I(1)-imidazoline receptors. Br J Pharmacol. 2000 Mar;129(6):1057-9.

    [4]. Glover V, et, al. β-Carbolines as selective monoamine oxidase inhibitors:In vivo implications

    [5]. Umezawa K, et, al. Comutagenic effect of norharman and harman with 2-acetylaminofluorene derivatives. Proc Natl Acad Sci U S A. 1978 Feb;75(2):928-30.

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MDM2-IN-21

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。

MDM2-IN-21 

MDM2-IN-21 是一种有效的 MDM2 抑制剂。MDM2-IN-21 可用于癌症研究。

MDM2-IN-21

MDM2-IN-21 Chemical Structure

CAS No. : 939981-88-1

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生物活性

MDM2-IN-21 is a potent MDM2 inhibitor. MDM2-IN-21 can be used for the research of cancer[1].

IC50 & Target

MDM2[1]

体外研究
(In Vitro)

The IC50 values of MDM2-IN-21 are 0.03 μM and 0.8 μM in homogeneous time resolved fluorescence (HTRF) assay and the wild-type p53 cell lines[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.

分子量

607.61

Formula

C34H40Cl2N4O2

CAS 号

939981-88-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Vu B, et al. Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development. ACS Med Chem Lett. 2013;4(5):466-469.

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Ro 0437626

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。

Ro 0437626 

Ro 0437626 是一种选择性嘌呤能 (P2X1) 受体拮抗剂 (IC50 = 3 μM),但对 P2X2、P2X3 和 P2X2/3 受体的亲和力较低 (IC50 > 100 μM)。

Ro 0437626

Ro 0437626 Chemical Structure

CAS No. : 134362-79-1

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生物活性

Ro 0437626 is a selective purinergic (P2X1) receptor antagonist (IC50 = 3 μM), but shows low affinity for P2X2, P2X3 and P2X2/3 receptors (IC50 > 100 μM)[1].

IC50 & Target

IC50: 3 μM (P2X1 receptor)

体外研究
(In Vitro)

Ro 0437626 reduces PMA-evoked Ca2+entry with 6.8 ± 4.7% of control[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Ro 0437626 (1 and 10 μmol/kg; i.v.) causes a reduction in postinfusion isovolumetric contractions[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female rat (urethane-anaesthetized)[3]
Dosage: 1 and 10 μmol/kg
Administration: I.v.
Result: Caused a reduction in postinfusion isovolumetric contractions.

分子量

525.66

Formula

C27H35N5O4S

CAS 号

134362-79-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Jaime-Figueroa S, et al. Discovery and synthesis of a novel and selective drug-like P2X(1) antagonist. Bioorg Med Chem Lett. 2005;15(13):3292-3295.

    [2]. Harper MT, et al. Phorbol ester-evoked Ca2+ signaling in human platelets is via autocrine activation of P(2X1) receptors, not a novel non-capacitative Ca2+ entry. J Thromb Haemost. 2010;8(7):1604-1613.

    [3]. King BF, et al. Investigation of the effects of P2 purinoceptor ligands on the micturition reflex in female urethane-anaesthetized rats. Br J Pharmacol. 2004;142(3):519-530.

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C6 Ceramide(Synonyms: C6-Cer; N-Hexanoylsphingosine)

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。

C6 Ceramide (Synonyms: C6-Cer; N-Hexanoylsphingosine)

C6-ceramide是一种神经酰胺途径激活剂,对多种癌细胞系具有活性。C6-ceramide 可用作化疗剂的佐剂,以增强抗肿瘤作用。

C6 Ceramide(Synonyms: C6-Cer;  N-Hexanoylsphingosine)

C6 Ceramide Chemical Structure

CAS No. : 124753-97-5

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生物活性

C6-ceramide, a ceramide pathway activator, shows activity against a variety of cancer cell lines. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects[1][2].

分子量

397.63

Formula

C24H47NO3

CAS 号

124753-97-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Zhu Q, et, al. C6-ceramide synergistically potentiates the anti-tumor effects of histone deacetylase inhibitors via AKT dephosphorylation and α-tubulin hyperacetylation both in vitro and in vivo. Cell Death Dis. 2011 Jan 27;2(1):e117.

    [2]. Liu L, et, al. C6-ceramide treatment inhibits the proangiogenic activity of multiple myeloma exosomes via the miR-29b/Akt pathway. J Transl Med. 2020 Aug 3;18(1):298.

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Intoplicine dimesylate(Synonyms: RP 60475 dimesylate)

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。

Intoplicine dimesylate (Synonyms: RP 60475 dimesylate) 纯度: 98.28%

Intoplicine (RP 60475) dimesylate,一种 7H 苯并 [e] 吡啶并 [4,3-b] 吲哚系列的抗肿瘤衍生物,是一种 DNA 拓扑异构酶 III 抑制剂。Intoplicine dimesylate 与 DNA (KA = 2 x 105 /M) 强烈结合,从而增加线性 DNA 的长度。

Intoplicine dimesylate(Synonyms: RP 60475 dimesylate)

Intoplicine dimesylate Chemical Structure

CAS No. : 133711-99-6

规格 价格 是否有货 数量
5 mg ¥8000 In-stock
10 mg ¥13000 In-stock
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Intoplicine dimesylate 相关产品

相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus

生物活性

Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 105 /M) and thereby increases the length of linear DNA[1][2].

IC50 & Target

Topoisomerase I

 

Topoisomerase II

 

体外研究
(In Vitro)

With 1-hour exposure to Intoplicine dimesylate at final concentrations of 2.5 micrograms/mL and 10.0 micrograms/mL, 26% and 54% of the assessable specimens shows positive in vitro responses, respectively[2].
With continuous exposure to Intoplicine dimesylate at concentrations of 0.25 micrograms/mL and 2.5 micrograms/mL, 16% and 71% of the assessable specimens showed positive responses, respectively[2].
Activity is seen against breast (71%), non-small-cell lung (69%), and ovarian (45%) cancer colony-forming units at a Intoplicine dimesylate concentration of 10.0 micrograms/mL after 1-hour exposure[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

At the highest non-toxic dose (HNTD) (6 mg/kg/injection, total dose, 36 mg/kg), intoplicine dimesylate shows highly active with a T/C of 0% and a corresponding total log cell kill of 3[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

540.65

Formula

C23H32N4O7S2

CAS 号

133711-99-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

DMSO : 115 mg/mL (212.71 mM; Need ultrasonic)

H2O : 100 mg/mL (184.96 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8496 mL 9.2481 mL 18.4963 mL
5 mM 0.3699 mL 1.8496 mL 3.6993 mL
10 mM 0.1850 mL 0.9248 mL 1.8496 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 (sealed storage, away from moisture and 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。

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: ≥ 5.75 mg/mL (10.64 mM); Clear solution

    此方案可获得 ≥ 5.75 mg/mL (10.64 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 57.5 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: ≥ 5.75 mg/mL (10.64 mM); Clear solution

    此方案可获得 ≥ 5.75 mg/mL (10.64 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 57.5 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: ≥ 5.75 mg/mL (10.64 mM); Clear solution

    此方案可获得 ≥ 5.75 mg/mL (10.64 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 57.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Riou JF, et al. Intoplicine (RP 60475) and its derivatives, a new class of antitumor agents inhibiting both topoisomerase I and II activities. Cancer Res. 1993;53(24):5987-5993.

    [2]. Eckardt JR, et al. Activity of intoplicine (RP60475), a new DNA topoisomerase I and II inhibitor, against human tumor colony-forming units in vitro. J Natl Cancer Inst. 1994;86(1):30-33.

    [3]. Bissery MC, et al. Antitumor activity of intoplicine (RP 60475, NSC 645008), a new benzo-pyrido-indole: evaluation against solid tumors and leukemias in mice. Invest New Drugs. 1993;11(4):263-277.

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BM-1244

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。

BM-1244  纯度: 98.77%

BM-1244 是一种有效的 Bcl-xL/Bcl-2 抑制剂,对 Bcl-xL 和 Bcl-2 的Ki 分别为 134 和 450 nM。BM-1244 抑制衰老成纤维细胞 (SnCs),EC50 为 5 nM。

BM-1244

BM-1244 Chemical Structure

CAS No. : 1619923-32-8

规格 价格 是否有货 数量
1 mg ¥5000 In-stock
5 mg ¥11000 In-stock
10 mg ¥17000 In-stock
25 mg ¥32000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

BM-1244 相关产品

相关化合物库:

  • Bioactive Compound Library Plus

生物活性

BM-1244 is a potent Bcl-xL/Bcl-2 inhibitor with Kis of 134 and 450 nM for Bcl- xL and Bcl-2, respectively. BM-1244 inhibits senescent fibroblasts (SnCs) with an EC50 of 5 nM. (From patent WO2019033119A1)[1].

分子量

1159.79

Formula

C54H59ClF4N6O8S4

CAS 号

1619923-32-8

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 : 200 mg/mL (172.45 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.8622 mL 4.3111 mL 8.6223 mL
5 mM 0.1724 mL 0.8622 mL 1.7245 mL
10 mM 0.0862 mL 0.4311 mL 0.8622 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    90% (20% SBE-β-CD in saline)

    Solubility: 5 mg/mL (4.31 mM); Suspended solution; Need ultrasonic

    此方案可获得 5 mg/mL (4.31 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 50.0 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
*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]. Jill Hopkins, et al. Treatment of ophthalmic conditions such as macular degeneration, glaucoma, and diabetic retinopathy using pharmaceutical agents that eliminate senescent cells. WO2019033119A1.

    [2]. Kim R. Unknotting the roles of Bcl-2 and Bcl-xL in cell death. Biochem Biophys Res Commun. 2005;333(2):336-343.

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CDK4/6-IN-6

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。

CDK4/6-IN-6 

CDK4/6-IN-6 (example A94) 是一种有效的 CDK4/CDK6 抑制剂,对CDK4/Cyclin D1 和 CDK6/Cyclin D3 的 Ki 值为 0.6 nM 和 13.9 nM。

CDK4/6-IN-6

CDK4/6-IN-6 Chemical Structure

CAS No. : 2380321-51-5

规格 是否有货
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250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

CDK4/6-IN-6 (example A94) is a potent CDK4/CDK6 inhibitor with a Ki of 0.6 nM and 13.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively[1].

IC50 & Target[1]

Cdk4/cyclin D1

0.6 nM (Ki)

cdk6/cyclin D3

13.9 nM (Ki)

体外研究
(In Vitro)

CDK4/6-IN-6 (example A94) has IC50s of 38.5 nM and 144.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3 using phospho-Rb S795 ELISA assays in JEKO-1 and MV4-1 1 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

463.93

Formula

C22H27ClFN5O3

CAS 号

2380321-51-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Ping Chen, et al. 2-amino-pyridine or 2-amino-pyrimidine derivatives as cyclin dependent kinase inhibitors. WO2019207463A1.

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MRTX849 acid

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。

MRTX849 acid 

MRTX849 acid 可用来合成PROTAC LC-2。LC-2 是一种有效且首创的 PROTAC,能够降解内源性 KRAS G12C (DC50,介于0.25 和0.76 μM之间)。

MRTX849 acid

MRTX849 acid Chemical Structure

CAS No. : 2561529-96-0

规格 是否有货
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500 mg   询价  

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生物活性

MRTX849 acid, a derivative of MRTX849, can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50s between 0.25 and 0.76 μM)[1][2].

IC50 & Target[1]

KRas G12C

 

体外研究
(In Vitro)

LC-2 induces degradation of endogenous KRASG12C in multiple KRAS mutant cancer cell (NCI-H2030, MIA PaCa-2, SW1573, NCI-H23 and NCI-H358 cells) with DC50s between 0.25 and 0.76 μM. LC-2-induced KRASG12C degradation occurs via a bona fide PROTAC mechanism. MIA PaCa-2, NCI-H23, and SW1573 cells are treated with 2.5 μM of LC-2 for 6, 24, 48, and 72 h. In all three cell lines, maximal KRAS degradation occurred within 24 h and was sustained up to 72 h[1].
LC-2-induced (2.5 μM; 6-24 hours) KRAS G12C degradation modulates Erk signaling in homozygous and heterozygous KRAS mutant cell lines[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

662.15

Formula

C34H37ClFN7O4

CAS 号

2561529-96-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Bond MJ, et al. Targeted Degradation of Oncogenic KRASG12C by VHL-Recruiting PROTACs. ACS Cent Sci. 2020;6(8):1367-1375.

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5-Iminodaunorubicin(Synonyms: 5-亚氨基柔红霉素)

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。

5-Iminodaunorubicin (Synonyms: 5-亚氨基柔红霉素) 纯度: 95.34%

5-Iminodaunorubicin 是一种醌改性蒽环类药物,具有抗肿瘤活性。5-Iminodaunorubicin 在癌细胞中可诱导 DNA 链断裂。

5-Iminodaunorubicin(Synonyms: 5-亚氨基柔红霉素)

5-Iminodaunorubicin Chemical Structure

CAS No. : 72983-78-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥4050 In-stock
5 mg ¥3500 In-stock
10 mg ¥5800 In-stock
25 mg ¥11000 In-stock
50 mg ¥17000 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

5-Iminodaunorubicin 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

5-Iminodaunorubicin is a quinone-modified anthracycline that retains antitumor activity[1]. 5-Iminodaunorubicin produces protein-concealed DNA strand breaks in cancer cells[2].

体外研究
(In Vitro)

In mouse leukemia L1210 cells, 5-Iminodaunorubicin produces protein-concealed DNA strand breaks. Many of the 5-iminodaunorubicin breaks may arise from apposed single-strand breaks (i.e., double-strand breaks)[2].

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)

In rat, 5-Iminodaunorubicin (5-ID; 1-16 mg/kg) treatment produces widening of the QRS complex, increased R- and S-wave voltage, and prolonged the Q alpha T interval. And the quinone redox cycling is suppressed in 5-Iminodaunorubicin. 5-Iminodaunorubicin shows lower cardiotoxic[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.

分子量

526.54

Formula

C27H30N2O9

CAS 号

72983-78-9

中文名称

5-亚氨基柔红霉素

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 (189.92 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8992 mL 9.4960 mL 18.9919 mL
5 mM 0.3798 mL 1.8992 mL 3.7984 mL
10 mM 0.1899 mL 0.9496 mL 1.8992 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: ≥ 2.5 mg/mL (4.75 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.75 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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: ≥ 2.5 mg/mL (4.75 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.75 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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
*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]. R A Jensen, et al. Electrocardiographic and transmembrane potential effects of 5-iminodaunorubicin in the rat. Cancer Res. 1984 Sep;44(9):4030-9.

    [2]. L A Zwelling, et al. Cytotoxicity and DNA strand breaks by 5-iminodaunorubicin in mouse leukemia L1210 cells: comparison with adriamycin and 4′-(9-acridinylamino)methanesulfon-m-anisidide. Cancer Res. 1982 Jul;42(7):2687-91.

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PCSK9 degrader 1

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。

PCSK9 degrader 1 

PCSK9 degrader 1 是一种选择性的 PCSK9 降解剂,不影响 PCSK9 功能。

PCSK9 degrader 1

PCSK9 degrader 1 Chemical Structure

CAS No. : 2215931-60-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

PCSK9 degrader 1 is a selective proprotein convertase substilisin-like/kexin type 9 (PCSK9) degrader. PCSK9 degrader 1 does not affect PCSK9 function[1].

体外研究
(In Vitro)

Biphenyl acid PCSK9 degrader 1 (compound 9) binds to and thermally stabilizes PCSK9 in a complex environment such as Huh7 lysate[1].
PCSK9 degrader 1 (compound 9), with high affinity for recombinant PCSK9 and target engagement in cell lysate, could be used as a recruiting element to promote the selective degradation of PCSK9[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

631.71

Formula

C34H34FN3O6S

CAS 号

2215931-60-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Whitney L Petrilli, et al. From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9. Cell Chem Biol. 2020 Jan 16;27(1):32-40.e3.

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Ro 0437626

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。

Ro 0437626 

Ro 0437626 是一种选择性嘌呤能 (P2X1) 受体拮抗剂 (IC50 = 3 μM),但对 P2X2、P2X3 和 P2X2/3 受体的亲和力较低 (IC50 > 100 μM)。

Ro 0437626

Ro 0437626 Chemical Structure

CAS No. : 134362-79-1

规格 是否有货
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生物活性

Ro 0437626 is a selective purinergic (P2X1) receptor antagonist (IC50 = 3 μM), but shows low affinity for P2X2, P2X3 and P2X2/3 receptors (IC50 > 100 μM)[1].

IC50 & Target

IC50: 3 μM (P2X1 receptor)

体外研究
(In Vitro)

Ro 0437626 reduces PMA-evoked Ca2+entry with 6.8 ± 4.7% of control[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Ro 0437626 (1 and 10 μmol/kg; i.v.) causes a reduction in postinfusion isovolumetric contractions[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female rat (urethane-anaesthetized)[3]
Dosage: 1 and 10 μmol/kg
Administration: I.v.
Result: Caused a reduction in postinfusion isovolumetric contractions.

分子量

525.66

Formula

C27H35N5O4S

CAS 号

134362-79-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Jaime-Figueroa S, et al. Discovery and synthesis of a novel and selective drug-like P2X(1) antagonist. Bioorg Med Chem Lett. 2005;15(13):3292-3295.

    [2]. Harper MT, et al. Phorbol ester-evoked Ca2+ signaling in human platelets is via autocrine activation of P(2X1) receptors, not a novel non-capacitative Ca2+ entry. J Thromb Haemost. 2010;8(7):1604-1613.

    [3]. King BF, et al. Investigation of the effects of P2 purinoceptor ligands on the micturition reflex in female urethane-anaesthetized rats. Br J Pharmacol. 2004;142(3):519-530.

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JW67

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。

JW67 

JW67 抑制典型 Wnt 信号,其 IC50 值为 1.17 μM。JW67 影响由 β- 连环蛋白/GSK-3β/AXIN/APC/CK1 组成的多蛋白复合物,该复合物可快速降低活性 β- 连环蛋白,随后下调 Wnt 靶基因。JW67 也抑制结直肠癌细胞生长。

JW67

JW67 Chemical Structure

CAS No. : 442644-28-2

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

JW67 inhibits the canonical Wnt signaling with an IC50 of 1.17μM[1]. JW67 affects the multiprotein complex consisting of β-catenin/GSK-3β/AXIN/APC/CK1 that rapidly reduces active β-catenin with a subsequent downregulation of Wnt target genes. JW67 also inhibits colorectal cancer cell growth[1].

IC50 & Target

IC50: 1.17μM (Wnt signaling)[1]

体外研究
(In Vitro)

JW67 (1 μM; 24 hours) increases concentration of AXIN2 and decreases the active form of β-catenin[1].
JW67 affects the expression of Wnt target genes and reduces cell growth of colon cancer cell lines[1].
JW67 shows a concentrationdependent reduction in proliferation with a GI50 value of 7.8 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.

Western Blot Analysis[1]

Cell Line: SW480 cells
Concentration: 1 μM
Incubation Time: 24 hours
Result: Increased the AXIN2 expression.

RT-PCR[1]

Cell Line: SW480 cells
Concentration: 10 or 25μM
Incubation Time: 72 hours
Result: Reduced growth of SW480 CRC cells in vitro by inhibiting cell-cycle progression at the G1/S.

分子量

394.38

Formula

C21H18N2O6

CAS 号

442644-28-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Waaler J, et al. Novel synthetic antagonists of canonical Wnt signaling inhibit colorectal cancer cell growth. Cancer Res. 2011;71(1):197-205.

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Cl-4AS-1

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。

Cl-4AS-1 

Cl-4AS-1 是一种有效的类固醇雄激素受体 (AR) 激动剂 (IC50 为 12 nM),也是 5α- 还原酶 I 型和 II 型的抑制剂 (IC50 分别为 6 和 10 nM)。

Cl-4AS-1

Cl-4AS-1 Chemical Structure

CAS No. : 188589-66-4

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生物活性

Cl-4AS-1, a potent steroidal androgen receptor (AR) agonist (IC50 = 12 nM), is also an inhibitor of 5α-reductase types I and II (IC50 = 6 and 10 nM, respectively)[1][2].

IC50 & Target

IC50: 12 nM (androgen receptor); 6 nM (5α-reductase types I); 10 nM (5α-reductase types II)[1][2]

体外研究
(In Vitro)

Cl-4AS-1 suppresses MMP-1 promoter activity in 22Rv1 human prostate cancer cells[1].
Cl-4AS-1 (10 μM) effectively promotes the AR N/C interaction, with an average maximal activity of 35.3%[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Cl-4AS-1 produces no significant reduction in prostate weight in intact animals and in castrates rats caused a significant increase of ventral prostate weight[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ORX rats[1]
Dosage: 10 mg/kg
Administration: I.s.; 7 days
Result: Effect of Cl-4AS-1 on prostate and seminal vesicle growth.

分子量

441.01

Formula

C26H33ClN2O2

CAS 号

188589-66-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Schmidt A, et al. Identification of anabolic selective androgen receptor modulators with reduced activities in reproductive tissues and sebaceous glands. J Biol Chem. 2009 Dec 25;284(52):36367-36376.

    [2]. Tolman RL, et al. 4-Methyl-3-oxo-4-aza-5alpha-androst-1-ene-17beta-N-aryl-carboxamides: an approach to combined androgen blockade [5alpha-reductase inhibition with androgen receptor binding in vitro]. J Steroid Biochem Mol Biol. 1997 Mar;60(5-6):303-9.

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SBI-581

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。

SBI-581 

SBI-581是一种口服有效的选择性的丝氨酸苏氨酸激酶 TAO3 抑制剂,IC50 值为 42 nM。SBI-581 促进 RAB11 阳性囊泡中 TKS5α 的积累。SBI-581 抑制侵袭性伪足形成。SBI-581 在小鼠腹腔注射后的药代动力学较为合理。SBI-581 具有抗肿瘤活性。

SBI-581

SBI-581 Chemical Structure

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生物活性

SBI-581 is an orally active and potent selective serine-threonine kinase TAO3 inhibitor, with an IC50 of 42 nM. SBI-581 promotes TKS5α accumulation at RAB11-positive vesicles. SBI-581 inhibits invadopodia formation. SBI-581 shows reasonable pharmacokinetics in mice using IP injection. SBI-581 shows antitumor activity[1].

IC50 & Target

IC50: 42 nM (TAO3), 237 nM (MEKK3)[1]

体外研究
(In Vitro)

SBI-581 shows moderate selectivity (> 5-10x) against the majority of a broad panel of kinases[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

SBI-581 (10 mg/kg, IP, once) displays reasonable pharmacokinetics (t1/2=1.5 hr; AUC= 1202 hr*ng/mL; Cmax= ~2 μM)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

383.44

Formula

C24H21N3O2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Iizuka S, et al. Serine-Threonine Kinase TAO3-Mediated Trafficking of Endosomes Containing the Invadopodia Scaffold TKS5α Promotes Cancer Invasion and Tumor Growth. Cancer Res. 2021 Mar 15;81(6):1472-1485.

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CDK4/6-IN-6

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。

CDK4/6-IN-6 

CDK4/6-IN-6 (example A94) 是一种有效的 CDK4/CDK6 抑制剂,对CDK4/Cyclin D1 和 CDK6/Cyclin D3 的 Ki 值为 0.6 nM 和 13.9 nM。

CDK4/6-IN-6

CDK4/6-IN-6 Chemical Structure

CAS No. : 2380321-51-5

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生物活性

CDK4/6-IN-6 (example A94) is a potent CDK4/CDK6 inhibitor with a Ki of 0.6 nM and 13.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively[1].

IC50 & Target[1]

Cdk4/cyclin D1

0.6 nM (Ki)

cdk6/cyclin D3

13.9 nM (Ki)

体外研究
(In Vitro)

CDK4/6-IN-6 (example A94) has IC50s of 38.5 nM and 144.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3 using phospho-Rb S795 ELISA assays in JEKO-1 and MV4-1 1 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

463.93

Formula

C22H27ClFN5O3

CAS 号

2380321-51-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Ping Chen, et al. 2-amino-pyridine or 2-amino-pyrimidine derivatives as cyclin dependent kinase inhibitors. WO2019207463A1.

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LP-184

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。

LP-184 

LP-184 (compound 6),一种酰基氟乙烯类似物,能够抑制肿瘤生长。LP-184 在卵巢、结肠、前列腺和胰腺细胞系中具有有效的抗癌活性,来自专利 WO2007019308A2。

LP-184

LP-184 Chemical Structure

CAS No. : 924835-67-6

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生物活性

LP-184 (compound 6), an acylfulvene analog, inhibits tumor growth. LP-184 has potent anti-cancer activity in the ovarian, colon, prostate and pancreatic cell lines. (patent WO2007019308A2).

IC50 & Target

IC50: 0.68 μM (HT29); 0.6 μM (OVCAR-3); 16 μM (AsPC-1); 0.14 μM (PC-3)

体外研究
(In Vitro)

LP-184 inhibits the growth of HT29, OVCAR-3, AsPC-1 and PC-3, with GI50s of 0.68, 0.6, 16 and 0.14 μM, respectively[1].
LP-184 displays IC50s of 800nM and 210 nM for anti-cancer activitie in the thymidine incorporation into cellular DNA (2 hour) and Trypan blue (48 hour) assay[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)

LP-184 (7.5 and 10 mg/kg; i.p.; 21 day) has potent 15 anti-tumor activity against MV522 tumors, producing 4/6 and 5/5 partial responses, respectively[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.

Animal Model: Mice (MV522 tumors) [1]
Dosage: 7.5 and 10 mg/kg
Administration: I.p; 21day
Result: Effective agent for human anti-tumor therapy.

分子量

304.34

Formula

C16H20N2O4

CAS 号

924835-67-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Trevor C. Mcmorris, et al. Illudin analogs useful as anticancer agents. WO2007019308A2.

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

SB 258719 hydrochloride

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。

SB 258719 hydrochloride 

SB 258719 hydrochloride 是一种选择性的 5-HT7 受体拮抗剂,与该受体亲和度高(pKi=7.5)。SB-258719 hydrochloride 可以用于癌症和神经系统疾病的研究 。

SB 258719 hydrochloride

SB 258719 hydrochloride Chemical Structure

CAS No. : 1217674-10-6

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SB 258719 hydrochloride 的其他形式现货产品:

SB 258719

生物活性

SB 258719 hydrochloride is a selective 5-HT7 receptor antagonist displayed high affnity (pKi=7.5) for the receptor. SB-258719 hydrochloride can be used for the research of cancer and neurological diseases[1][2].

IC50 & Target[1]

5-HT7 Receptor

7.5 (pKi)

体外研究
(In Vitro)

SB-258719 (1, 3 and 10 μM; HEK 293 cells) hydrochloride produces a concentration-related rightward-shift of the 5-CT concentration-response curve with no signifcant alteration in the maximal response to 5-CT[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

SB-258719 (5~20 mg/kg; i.p.) hydrochloride significantly attenuates the 5-CT-induced hypothermia[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Swiss Webster mice (20~25 g)[2].
Dosage: 5~20 mg/kg
Administration: I.p.
Result: Significantly attenuated the 5-CT-induced hypothermia.

分子量

374.97

Formula

C18H31ClN2O2S

CAS 号

1217674-10-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Thomas DR, et al. Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719. Br J Pharmacol. 1998;124(6):1300-1306.

    [2]. Guscott MR, et al. The hypothermic effect of 5-CT in mice is mediated through the 5-HT7 receptor. Neuropharmacology. 2003;44(8):1031-1037.

    [3]. Fatima S, et al. 5-Hydroxytryptamine promotes hepatocellular carcinoma proliferation by influencing β-catenin. Mol Oncol. 2016;10(2):195-212.

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