CP-67804

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。

CP-67804 

CP-67804,喹诺酮类衍生物,是一种拓扑异构酶 II (topoisomerase II) 靶向制剂。CP-67804有效增强真核生物拓扑异构酶 II 介导的DNA切割。CP-67804 具有潜在的抗肿瘤作用。

CP-67804

CP-67804 Chemical Structure

CAS No. : 103978-08-1

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生物活性

CP-67804 is a quinolone derivative, is a topoisomerase II-targeted agent. CP-67804 effectively enhances DNA cleavage mediated by eukaryotic topoisomerase II. CP-67804 has potential as an antineoplastic agent[1].

IC50 & Target[1]

Topoisomerase II

 

体外研究
(In Vitro)

CP-67804 increases topoisomerase II-mediated DNA breakages by enhancing the enzyme’s forward rate of cleavage[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

345.30

Formula

C18H13F2NO4

CAS 号

103978-08-1

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]. Robinson MJ, et al. Effects of quinolone derivatives on eukaryotic topoisomerase II. A novel mechanism for enhancement of enzyme-mediated DNA cleavage. J Biol Chem. 1991;266(22):14585-14592.

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GS-493

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。

GS-493 

GS-493 是一种选择性的酪氨酸磷酸酶 SHP2 (PTPN11) 抑制剂,IC50 为 71 nM,对 SHP2 的活性比 SHP1 和 PTP1B 高 29 倍和 45 倍。 GS-493 抑制细胞运动和癌细胞生长。GS-493 具有抗肿瘤活性。

GS-493

GS-493 Chemical Structure

CAS No. : 1710337-31-7

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生物活性

GS-493 is a selective protein tyrosine phosphatase SHP2 (PTPN11) inhibitor with an IC50 of 71 nM. GS-493 is 29- and 45-fold more active toward SHP2 than related SHP1 and PTP1B. GS-493 blocks cellular motility and growth of cancer cells. Antitumor activity[1].

IC50 & Target

IC50: 71 nM (SHP2); 2.08 μM (SHP1); 3.17 μM (PTP1B)[1]

体外研究
(In Vitro)

GS-493 (0.0625-10 μM) blocks hepatocyte growth factor (HGF)-stimulated epithelial-mesenchymal transition of human pancreatic adenocarcinoma (HPAF) cells[1].
GS-493 (40 μM, a couple of days) blocks growth of the human NSCL cancer cell line LXFA 526L in soft agar and decreases the number of tumor cell colonies to 32%[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)

GS-493 (46 mg/kg; i.p.; daily for 27 days) inhibits tumor growth significantly in a murine xenograft model[1].

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

Animal Model: Nude mouse xenograft model (strain NMRI nu/nu mice)
Dosage: 46 mg/kg (45.93 mg in 3 mL DMSO per kg)
Administration: i.p.; daily for 27 days
Result: Inhibited tumor growth significantly.

分子量

510.44

Formula

C21H14N6O8S

CAS 号

1710337-31-7

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]. Grosskopf S, et al. Selective inhibitors of the protein tyrosine phosphatase SHP2 block cellular motility and growth of cancer cells in vitro and in vivo. ChemMedChem. 2015;10(5):815-826.

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N-5984(Synonyms: KRP-204)

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。

N-5984 (Synonyms: KRP-204)

N-5984 (KRP-204) 是一种有效的、具有选择性的 β3-adrenergic receptor 激动剂。N-5984 具有发展成为治疗临床肥胖和糖尿病有效药物的潜力。

N-5984(Synonyms: KRP-204)

N-5984 Chemical Structure

CAS No. : 220475-76-3

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生物活性

N-5984 (KRP-204) is a potent and selective agonist of β3-adrenergic receptor. N-5984 has the potential for developing as one of the clinically effective drugs for obesity and diabetes mellitus[1].

IC50 & Target

β-adrenoceptor

 

分子量

391.85

Formula

C20H22ClNO5

CAS 号

220475-76-3

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]. Yanagisawa T, et al. Selectivity and potency of agonists for the three subtypes of cloned human beta-adrenoceptors expressed in Chinese hamster ovary cells. Tohoku J Exp Med. 2000;192(3):181-193.

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MS-PPOH

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。

MS-PPOH 

MS-PPOH 是一种有效的选择性细胞色素 P450 (CYP) 环氧化酶抑制剂。MS-PPOH 抑制 CYP2C8CYP2C9IC50 分别为 15 和 11 µM。

MS-PPOH

MS-PPOH Chemical Structure

CAS No. : 206052-02-0

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生物活性

MS-PPOH is a potent and selective cytochrome P450 (CYP) epoxygenase inhibitor[1]. MS-PPOH inhibits CYP2C8 and CYP2C9 with IC50s of 15 and 11 µM, respectively[2].

体外研究
(In Vitro)

MS-PPOH blocks cellular EET synthesis. MS-PPOH inhibits tonic (basal) cell invasion and migration and reduces the 11,12-EET (1.0 μM)-induced cell motility[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: PC-3 cells
Concentration: 2.0 and 10.0 μM
Incubation Time: 24 hours
Result: Inhibited tonic (basal) cell invasion and migration.

体内研究
(In Vivo)

MS-PPOH (20 mg/kg/day, i.v.) for 6 days significantly reduced renal levels of epoxyeicosatrienoic acids (EETs) in Dahl salt-resistant rats on 2% NaCl drinking solution[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.

Animal Model: Six-week-old male stroke-prone spontaneously hypertensive rats (SHRSP)[3]
Dosage: 20 mg/kg/day
Administration: Intravenously
Result: Treatment had negligible effects on systolic blood pressure (SBP) in saline-drinking SHRSP after 1 week, 160 vs. 167 mmHg, or 2 weeks of treatment, 171 vs. 175 mmHg, for vehicle vs. MS-PPOH, respectively.

分子量

323.41

Formula

C16H21NO4S

CAS 号

206052-02-0

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]. Kasem Nithipatikom, et al. Inhibition of carcinoma cell motility by epoxyeicosatrienoic acid (EET) antagonists. Cancer Sci. 2010 Dec;101(12):2629-36.

    [2]. Jun Yang, et al. Cytochrome P450 2C24: Expression, Tissue Distribution, High-Throughput Assay, and Pharmacological Inhibition. Acta Pharm Sin B. 2012 Apr;2(2):137-145.

    [3]. Jing Li, et al. Pharmacological manipulation of arachidonic acid-epoxygenase results in divergent effects on renal damage. Front Pharmacol. 2014 Aug 15;5:187.

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Heptelidic acid(Synonyms: 萜烯七脂酸; Koningic 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。

Heptelidic acid (Synonyms: 萜烯七脂酸; Koningic acid)

Heptelidic acid (Koningic acid) 是一种倍半萜类抗生素 (antibiotic)。Heptelidic acid 通过下调 caspase 从而抑制 Etoposide 诱导的细胞凋亡。Koningic acid (KA) 是一种特异性 GAPDH 抑制剂,IC50 为 90 μM。

Heptelidic acid(Synonyms: 萜烯七脂酸; Koningic acid)

Heptelidic acid Chemical Structure

CAS No. : 57710-57-3

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生物活性

Heptelidic acid (Koningic acid) is a sesquiterpene antibiotic[1]. Heptelidic acid inhibits Etoposide-induced apoptosis via downregulation of caspases[2]. Koningic acid (KA) is a specific GAPDH inhibitor with an IC50of 90 μM[3].

IC50 & Target[2]

Caspase-3

 

体外研究
(In Vitro)

Heptelidic acid is a sesquiterpene antibiotic, found in the culture filtrate of three different strains of fungi isolated from soil samples. Heptelidic acid produces organisms, fermentation, isolation and characterization[1].
Heptelidic acid inhibits Etoposide-induced apoptosis in human leukemia U937 cells[2].Heptelidic acid inhibits caspase- 3 induction in U937 cells with an IC50 value of 40 μM after 8 h of Etoposide treatment[2].
Heptelidic acid (Koningic acid; KA), a natural product obtained from the Trichoderma fungus, can directly bind to the active site of human GAPDH. The expression of T. koningii KAr-GAPDH successfully rescued cell viability in human cells treated with Heptelidic acid. HEK293T cells expressing T. koningii KAr-GAPDH exhibited complete cell viability after treatment with 0-200 μM Heptelidic acid with the IC50=5 μM[3].

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

Cell Viability Assay[3]

Cell Line: HEK293T cells expressing KAr-GAPDH or EV (top left)
Concentration: 0.1, 1, 10, 100, 1000 μM
Incubation Time: 24 hours
Result: IC50=5 μM.

体内研究
(In Vivo)

Heptelidic acid (Koningic acid; KA) is bioavailable and induces dynamic changes to glycolysis in vivo[3].

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

Animal Model: 6-week old female Foxn1nu mice bearing BT-474 tumor[3]
Dosage: 1, 2.5, 5, and 10 mg/kg
Administration: Daily intraperitoneal (IP) injections, 24 hours
Result: 1 mg/kg was determined to be the maximum tolerated dose (MTD) based upon behavioral monitoring and adverse events at higher doses (hemolysis, hematuria, and anemia).

分子量

280.32

Formula

C15H20O5

CAS 号

57710-57-3

中文名称

萜烯七脂酸

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]. Y Itoh, et al. A new sesquiterpene antibiotic, heptelidic acid producing organisms, fermentation, isolation and characterization. J Antibiot (Tokyo). 1980 May;33(5):468-73.

    [2]. Jin Hee Kim, et al. Heptelidic acid, a sesquiterpene lactone, inhibits Etoposide-induced apoptosis in human leukemia U937 cells. J Microbiol Biotechnol. 2009 Aug;19(8):787-91.

    [3]. Maria V Liberti, et al. A Predictive Model for Selective Targeting of the Warburg Effect through GAPDH Inhibition with a Natural Product. Cell Metab. 2017 Oct 3;26(4):648-659.e8.

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HSP90-IN-10

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。

HSP90-IN-10 

HSP90-IN-10 (Compound 16s) 是一种有效的 HSP90 抑制剂。 HSP90-IN-10 对 HCC1954 乳腺癌细胞具有很强的抗增殖能力,IC50 值为 6 µM。HSP90-IN-10 不抑制正常上皮细胞的生长。HSP90-IN-10 还诱导细胞凋亡 (apoptosis)。

HSP90-IN-10

HSP90-IN-10 Chemical Structure

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生物活性

HSP90-IN-10 (Compound 16s) is a potent inhibitor of HSP90. HSP90-IN-10 exhibits high antiproliferative potency against HCC1954 breast cancer cells with the IC50 value of 6 µM. HSP90-IN-10 does not inhibit the growth of normal epithelial cells. HSP90-IN-10 also induces apoptosis[1].

分子量

543.54

Formula

C30H26FN3O6

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]. Piven YA, et al. Novel O-acylated (E)-3-aryl-6,7-dihydrobenzisoxazol-4(5H)-one oximes targeting HSP90-HER2 axis in breast cancer cells. Bioorg Med Chem. 2022 Jan 1;53:116521.

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AG957(Synonyms: Tyrphostin AG957; NSC 654705)

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。

AG957 (Synonyms: Tyrphostin AG957; NSC 654705)

AG957 (Tyrphostin AG957;NSC 654705) 是一种酪氨酸激酶抑制剂,具有抗 BCR/ABL 酪氨酸激酶活性。AG957抑制 p210bcr/abl 酶活性,IC50 为 2.9 μM。

AG957(Synonyms: Tyrphostin AG957;  NSC 654705)

AG957 Chemical Structure

CAS No. : 140674-76-6

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生物活性

AG957 (Tyrphostin AG957;NSC 654705) is a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity[1][2]. AG957 is a bcr/abl kinase inhibitor with an IC50 of 2.9 μM for p210bcr/abl autokinase activity[3].

体外研究
(In Vitro)

AG957 inhibit p210bcr-abl tyrosine kinase activity. AG957 inhibits DNA synthesis as early as 2 h (60% inhibition at 20 microM). AG957 inhibits p210bcr-abl tyrosine phosphorylation in living cells by 1 h without an inhibition of total protein phosphorylation[1]. Tyrphostin AG957, a protein tyrosine kinase (PTK) inhibitor which has activity against the p210BCR/ABL kinase, on beta1 integrin function in CML progenitors[2].
AG957 (0.1-100 μM ) pretreatment results in significant inhibition of proliferation of chronic myelogenous leukemia (CML) colony-forming cells (CFC) CML CFC[2].
AG957 (25 μM) partially inhibits phosphorylation of several proteins that are BCR/ABL PTK substrates and are involved in normal integrin signaling in BCR/ABL expressing cells[2].

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

Cell Proliferation Assay[2]

Cell Line: CML and CFC
Concentration: 0, 0.1, 1, 10, 100 μM
Incubation Time: Pretreatment for 1 hour
Result: A significant dose-dependent inhibition of CML CFC growth was seen following preincubation with AG957.

Western Blot Analysis[2]

Cell Line: K562 and BCR/ABL-tranfected M07e cells (MBA-4)
Concentration: 25 μM
Incubation Time: 24 hours
Result: Partially inhibited tyrosine phosphorylation of p210BCR/ABL, the focal adhesion protein paxillin, the p85 regulatory subunit of the PI3K and the adapter protein cbl in K562 cells.
Inhibited phosphorylation of these proteins as well as the adapter protein crkl in MBA4 cells.

体内研究
(In Vivo)

AG957 (10 mg/kg; intratracheally 1 h before intratracheal LPS challenge) blocks c-Abl activity in the lung of mice[4].

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

Animal Model: C57BL/6J mice[4]
Dosage: 10 mg/kg
Administration: Intratracheally 1 h before intratracheal LPS challenge
Result: LPS induced significant phosphorylation of paxillin at Y31 and Y118. Inhibition of c-Abl by AG957 attenuated LPS-induced phosphorylation of paxillin at both sites.
LPS induced significant phosphorylation of VE-cadherin in DMSO-treated mice, which was attenuated in AG957-treated mice.

分子量

273.28

Formula

C15H15NO4

CAS 号

140674-76-6

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]. G Kaur, et al. Tyrphostin induced growth inhibition: correlation with effect on p210bcr-abl autokinase activity in K562 chronic myelogenous leukemia. Anticancer Drugs. 1994 Apr;5(2):213-22.

    [2]. R Bhatia, et al. Tyrphostin AG957, a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity restores beta1 integrin-mediated adhesion and inhibitory signaling in chronic myelogenous leukemia hematopoietic progenitors. Leukemia. 1998 Nov;12(11):1708-17.

    [3]. P A Svingen, et al. Effects of the bcr/abl kinase inhibitors AG957 and NSC 680410 on chronic myelogenous leukemia cells in vitro. Clin Cancer Res. 2000 Jan;6(1):237-49.

    [4]. Panfeng Fu, et al. c-Abl mediated tyrosine phosphorylation of paxillin regulates LPS-induced endothelial dysfunction and lung injury. Am J Physiol Lung Cell Mol Physiol. 2015 May 15;308(10):L1025-38.

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Pyoluteorin(Synonyms: 藤黄绿菌素;藤黄绿脓菌素;黄绿脓菌素)

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。

Pyoluteorin (Synonyms: 藤黄绿菌素;藤黄绿脓菌素;黄绿脓菌素)

Pyoluteorin 是一种抗生素 (antibiotic),可抑制 Oomycete fungi,包括植物病原体 Oomycete fungi,并抑制由该真菌引起的植物病害。 Pyoluteorin 在体外诱导人三阴性乳腺癌 MDA-MB-231 细胞凋亡 (apoptosis)。 Pyoluteorin 可用于人类三阴性乳腺癌的研究。

Pyoluteorin(Synonyms: 藤黄绿菌素;藤黄绿脓菌素;黄绿脓菌素)

Pyoluteorin Chemical Structure

CAS No. : 25683-07-2

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生物活性

Pyoluteorin is an antibiotic that inhibits Oomycete fungi, including the plant pathogen Pythium ultimum, and suppresses plant diseases caused by this fungus[1]. Pyoluteorin induces human triple-negative breast cancer MDA-MB-231 cells apoptosis in vitro. Pyoluteorin can be used for the research of human triple-negative breast cancer[2].

体外研究
(In Vitro)

Pyoluteorin is an antifungal compound composed of a bichlorinated pyrrole linked to a resorcinol moiety, were identified within a 24-kb genomic region of Pseudomonas fluorescens Pf-5[1].
Pyoluteorin has significant cytotoxicity towards MCF-7 (IC50=1.84 μM). Pyoluteorin also displays significantly selective cytotoxicity against BT474, HCC1954, MAD-MB-468, MDA-MB-231, and MCF-10A cells with IC50s of 9.75±0.16, 0.94±0.01, 3.89±0.08, 0.97±0.01, and 57.01±0.76 μM, respectively[2].
Pyoluteorin (0.1-10 μM; for 24 hours) induces change of apoptosis-related protein expressions. Pyoluteorin-induced cell apoptosis in MDA-MB-231 is related to Bcl-2 family proteins and caspase cascade[2].
Pyoluteorin (0.1-10 μM; for 24 h) induces cell cycle arrest and apoptosis in human triple-negative breast cancer cells MDA-MB-231[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.

Cell Proliferation Assay[2]

Cell Line: Human triple-negative breast cancer cell MDA-MB-231
Concentration: 0, 0.032, 0.16, 0.8, 4, 20, 100 μM
Incubation Time: 24, 48, 72 hours
Result: Inhibited cells proliferation in a dose- and time-dependent manner.

Western Blot Analysis[2]

Cell Line: MDA-MB-231 cells
Concentration: 0.1, 0.3, 1, 3, 10 μM
Incubation Time: 24 hours
Result: The levels of the anti-apoptotic proteins Bcl-2, Bcl-XL and PARP were obviously decreased while the pro-apoptotic proteins BAX and caspase 3 were increased in a dose-dependent manner.

分子量

272.08

Formula

C11H7Cl2NO3

CAS 号

25683-07-2

中文名称

藤黄绿菌素;藤黄绿脓菌素;黄绿脓菌素

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]. B Nowak-Thompson, et al. Characterization of the pyoluteorin biosynthetic gene cluster of Pseudomonas fluorescens Pf-5. J Bacteriol. 1999 Apr;181(7):2166-74.

    [2]. Ting Ding, et al. Pyoluteorin induces cell cycle arrest and apoptosis in human triple-negative breast cancer cells MDA-MB-231. J Pharm Pharmacol. 2020 Jul;72(7):969-978.

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Decylubiquinone(Synonyms: 癸基泛醌)

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。

Decylubiquinone (Synonyms: 癸基泛醌)

Decylubiquinone 是泛醌 (辅酶 Q10) 的类似物。Decylubiquinone 阻止活性氧 (ROS) 的产生以响应谷胱甘肽消耗并抑制线粒体通透性转变的激活。

Decylubiquinone(Synonyms: 癸基泛醌)

Decylubiquinone Chemical Structure

CAS No. : 55486-00-5

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生物活性

Decylubiquinone is an analog of ubiquinone (coenzyme Q10). Decylubiquinone blocks reactive oxygen species (ROS) production in response to glutathione depletion and inhibits activation of the mitochondrial permeability transition[1].

体外研究
(In Vitro)

Decylubiquinone (dUb; 10 μm for 6 hours) exerts its effects on ROS by either inhibition of ROS production by cytochrome bc1 or that it scavenged ROS produced[1].
Decylubiquinone inhibits both the dichlorofluorescein (DCF) fluorescence increase resulting from H2O2 treatment and the DCF fluorescence increase resulting after glutathione (GSH) depletion using diethylmaleate mitochondrially generated ROS)[1].

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

Cell Viability Assay[1]

Cell Line: HL60 cells transfected with bcl-2 (bcl-2) (HL60 B cells)
Concentration: 10 μM
Incubation Time: 6 hours
Result: Attenuated the ROS increase in HL60 (B) cells.

分子量

322.44

Formula

C19H30O4

CAS 号

55486-00-5

中文名称

癸基泛醌

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]. Jeffrey S Armstrong, et al. The Coenzyme Q10 analog decylubiquinone inhibits the redox-activated mitochondrial permeability transition: role of mitcohondrial [correction mitochondrial] complex III. J Biol Chem. 2003 Dec 5;278(49):49079-84.

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GS-493

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。

GS-493 

GS-493 是一种选择性的酪氨酸磷酸酶 SHP2 (PTPN11) 抑制剂,IC50 为 71 nM,对 SHP2 的活性比 SHP1 和 PTP1B 高 29 倍和 45 倍。 GS-493 抑制细胞运动和癌细胞生长。GS-493 具有抗肿瘤活性。

GS-493

GS-493 Chemical Structure

CAS No. : 1710337-31-7

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生物活性

GS-493 is a selective protein tyrosine phosphatase SHP2 (PTPN11) inhibitor with an IC50 of 71 nM. GS-493 is 29- and 45-fold more active toward SHP2 than related SHP1 and PTP1B. GS-493 blocks cellular motility and growth of cancer cells. Antitumor activity[1].

IC50 & Target

IC50: 71 nM (SHP2); 2.08 μM (SHP1); 3.17 μM (PTP1B)[1]

体外研究
(In Vitro)

GS-493 (0.0625-10 μM) blocks hepatocyte growth factor (HGF)-stimulated epithelial-mesenchymal transition of human pancreatic adenocarcinoma (HPAF) cells[1].
GS-493 (40 μM, a couple of days) blocks growth of the human NSCL cancer cell line LXFA 526L in soft agar and decreases the number of tumor cell colonies to 32%[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)

GS-493 (46 mg/kg; i.p.; daily for 27 days) inhibits tumor growth significantly in a murine xenograft model[1].

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

Animal Model: Nude mouse xenograft model (strain NMRI nu/nu mice)
Dosage: 46 mg/kg (45.93 mg in 3 mL DMSO per kg)
Administration: i.p.; daily for 27 days
Result: Inhibited tumor growth significantly.

分子量

510.44

Formula

C21H14N6O8S

CAS 号

1710337-31-7

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]. Grosskopf S, et al. Selective inhibitors of the protein tyrosine phosphatase SHP2 block cellular motility and growth of cancer cells in vitro and in vivo. ChemMedChem. 2015;10(5):815-826.

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FF-10502

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。

FF-10502 

FF-10502 是 Gemcitabine 的结构类似物,是一种嘧啶核苷抗代谢物。FF-10502 抑制 DNA 聚合酶 α 和 β (DNA polymerase α/β)。FF-10502 通过对休眠细胞的作用机制显示出有益的抗癌活性。

FF-10502

FF-10502 Chemical Structure

CAS No. : 184302-49-6

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生物活性

FF-10502, a structural analog of Gemcitabine, is a pyrimidine nucleoside antimetabolite. FF-10502 inhibits DNA polymerase α and β. FF-10502 shows beneficial anticancer activity via a mechanism of action on dormant cells[1].

体外研究
(In Vitro)

FF-10502 (0.1 nM-10 μM; 72 hours) shows the growth inhibition of pancreatic cancer cell lines, with IC50s of 59.9 nM, 39.6 nM, 68.2 nM, and 331.4 nM for BxPC-3, SUIT-2, Capan-1, and MIA PaCa-2 cells, 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.

Cell Viability Assay[1]

Cell Line: Human pancreatic cancer cell lines (BxPC-3, SUIT-2, Capan-1, and MIA PaCa-2)
Concentration: 0.1 nM to 10 μM
Incubation Time: 72 hours
Result: Inhibited the growth of pancreatic cancer cell lines.

体内研究
(In Vivo)

FF-10502 (120-480 mg/kg; i.v; once weekly; for 4 weeks) shows an antitumor effect in a mouse xenograft model with the subcutaneously implanted human pancreatic cancer cell line Capan-1[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: Five-week-old female nude mice (BALB/c-nu/nu) injected with Capan-1 cells[1].
Dosage: 120 mg/kg, 240 mg/kg, 360 mg/kg, and 480 mg/kg
Administration: Tail vein injection; once weekly; for 4 weeks
Result: Suppressed tumor growth in a dose-dependent manner in mice.

分子量

261.27

Formula

C9H12FN3O3S

CAS 号

184302-49-6

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]. Shinji Mima, et al. FF-10502, an Antimetabolite with Novel Activity on Dormant Cells, Is Superior to Gemcitabine for Targeting Pancreatic Cancer Cells. J Pharmacol Exp Ther. 2018 Jul;366(1):125-135.

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ACG416B

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。

ACG416B 

ACG416B (compound 18) 是一种有效的胆碱激酶 (ChoK) 抑制剂,IC50 值为 0.4 μM。ACG416B 对 HT-29 人结肠癌细胞具有更高的 ChoK 抑制和抗增殖活性。

ACG416B

ACG416B Chemical Structure

CAS No. : 795316-15-3

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生物活性

ACG416B (compound 18) is a potent inhibitor of ChoK (choline kinase) with an IC50 of 0.4 μM. ACG416B renders higher ChoK inhibitory and antiproliferative activities against the HT-29 human colon cancer cell[1].

IC50 & Target

ChoK[1]

分子量

708.53

Formula

C38H36Br2N4

CAS 号

795316-15-3

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]. onejo-García A, et al. Influence of the linker in bispyridium compounds on the inhibition of human choline kinase. J Med Chem. 2004 Oct 21;47(22):5433-40.

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IDO1/2-IN-1 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。

IDO1/2-IN-1 hydrochloride 

IDO1/2-IN-1 hydrochloride 是第一个有效的 IDO1/IDO2 双重抑制剂,对 IDO1 和 IDO2 的 IC50 分别为 28 nM 和 144 nM。IDO1/2-IN-1 hydrochloride 具有抗肿瘤活性。具有口服活性。

IDO1/2-IN-1 hydrochloride

IDO1/2-IN-1 hydrochloride Chemical Structure

CAS No. : 2310286-60-1

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生物活性

IDO1/2-IN-1 hydrochloride (compound 4t) is the first potent IDO1/IDO2 dual inhibitor with IC50s of 28 nM and 144 nM for IDO1 and IDO2, respectively. IDO1/2-IN-1 hydrochloride exhibits antitumor activies. Orally active[1].

分子量

521.73

Formula

C16H19BrClFN8O4

CAS 号

2310286-60-1

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]. He X, et al. Discovery of the First Potent IDO1/IDO2 Dual Inhibitors: A Promising Strategy for Cancer Immunotherapy. J Med Chem. 2021;64(24):17950-17968.

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Heptelidic acid(Synonyms: 萜烯七脂酸; Koningic 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。

Heptelidic acid (Synonyms: 萜烯七脂酸; Koningic acid)

Heptelidic acid (Koningic acid) 是一种倍半萜类抗生素 (antibiotic)。Heptelidic acid 通过下调 caspase 从而抑制 Etoposide 诱导的细胞凋亡。Koningic acid (KA) 是一种特异性 GAPDH 抑制剂,IC50 为 90 μM。

Heptelidic acid(Synonyms: 萜烯七脂酸; Koningic acid)

Heptelidic acid Chemical Structure

CAS No. : 57710-57-3

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生物活性

Heptelidic acid (Koningic acid) is a sesquiterpene antibiotic[1]. Heptelidic acid inhibits Etoposide-induced apoptosis via downregulation of caspases[2]. Koningic acid (KA) is a specific GAPDH inhibitor with an IC50of 90 μM[3].

IC50 & Target[2]

Caspase-3

 

体外研究
(In Vitro)

Heptelidic acid is a sesquiterpene antibiotic, found in the culture filtrate of three different strains of fungi isolated from soil samples. Heptelidic acid produces organisms, fermentation, isolation and characterization[1].
Heptelidic acid inhibits Etoposide-induced apoptosis in human leukemia U937 cells[2].Heptelidic acid inhibits caspase- 3 induction in U937 cells with an IC50 value of 40 μM after 8 h of Etoposide treatment[2].
Heptelidic acid (Koningic acid; KA), a natural product obtained from the Trichoderma fungus, can directly bind to the active site of human GAPDH. The expression of T. koningii KAr-GAPDH successfully rescued cell viability in human cells treated with Heptelidic acid. HEK293T cells expressing T. koningii KAr-GAPDH exhibited complete cell viability after treatment with 0-200 μM Heptelidic acid with the IC50=5 μM[3].

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

Cell Viability Assay[3]

Cell Line: HEK293T cells expressing KAr-GAPDH or EV (top left)
Concentration: 0.1, 1, 10, 100, 1000 μM
Incubation Time: 24 hours
Result: IC50=5 μM.

体内研究
(In Vivo)

Heptelidic acid (Koningic acid; KA) is bioavailable and induces dynamic changes to glycolysis in vivo[3].

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

Animal Model: 6-week old female Foxn1nu mice bearing BT-474 tumor[3]
Dosage: 1, 2.5, 5, and 10 mg/kg
Administration: Daily intraperitoneal (IP) injections, 24 hours
Result: 1 mg/kg was determined to be the maximum tolerated dose (MTD) based upon behavioral monitoring and adverse events at higher doses (hemolysis, hematuria, and anemia).

分子量

280.32

Formula

C15H20O5

CAS 号

57710-57-3

中文名称

萜烯七脂酸

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]. Y Itoh, et al. A new sesquiterpene antibiotic, heptelidic acid producing organisms, fermentation, isolation and characterization. J Antibiot (Tokyo). 1980 May;33(5):468-73.

    [2]. Jin Hee Kim, et al. Heptelidic acid, a sesquiterpene lactone, inhibits Etoposide-induced apoptosis in human leukemia U937 cells. J Microbiol Biotechnol. 2009 Aug;19(8):787-91.

    [3]. Maria V Liberti, et al. A Predictive Model for Selective Targeting of the Warburg Effect through GAPDH Inhibition with a Natural Product. Cell Metab. 2017 Oct 3;26(4):648-659.e8.

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GLS1 Inhibitor-3

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。

GLS1 Inhibitor-3 

GLS1 Inhibitor-3 (compound C147) 是一种有效的 GLS1 抑制剂,IC50 为 27.98 nM。GLS1 Inhibitor-3 具有抗增殖活性。

GLS1 Inhibitor-3

GLS1 Inhibitor-3 Chemical Structure

CAS No. : 2435781-94-3

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生物活性

GLS1 Inhibitor-3 (compound C147) is a potent GLS1 inhibitor with an IC50 of 27.98 nM. GLS1 Inhibitor-3 shows antiproliferative activity[1].

IC50 & Target

IC50: 27.98 nM (GLS1)[1]

分子量

596.71

Formula

C30H32N10O2S

CAS 号

2435781-94-3

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]. Xu X, et al. Discovery of novel glutaminase 1 allosteric inhibitor with 4-piperidinamine linker and aromatic heterocycles. Eur J Med Chem. 2022 Jun 5;236:114337.

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PAD2-IN-2

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。

PAD2-IN-2 

PAD2-IN-2 是一种有效的 PAD2 抑制剂。PAD2-IN-2 进入 HEK293T/PAD2 细胞的 EC50 值为 5.9 μM。PAD2-IN-2 在 HEK293/PAD2 细胞中抑制组蛋白 H3 瓜氨酸化 (EC50=2.1 μM)。PAD2-IN-2 可用于癌症研究。

PAD2-IN-2

PAD2-IN-2 Chemical Structure

CAS No. : 2095107-57-4

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生物活性

PAD2-IN-2 is a potent PAD2 inhibitor. PAD2-IN-2 enters the HEK293T/PAD2 cells with an EC50 of 5.9 μM. PAD2-IN-2 inhibits histone H3 citrullination with an EC50 of 2.1 μM in HEK293/PAD2 cells. PAD2-IN-2 can be used for the research of cancer[1].

IC50 & Target[1]

PAD2

 

体外研究
(In Vitro)

PAD2-IN-2 (compound 37a; 25 μM; HEK293T/PAD2 cells) exhibits good potency with >60% occupancy in target engagement assay[1].
PAD2-IN-2 (0, 1, 5, 10, 25μM ; 72 h) enters the HEK293T/PAD2 cells with an EC50 of 5.9 μM[1].
PAD2-IN-2 (0, 1, 5, 10, 25μM, 3 h) inhibits histone H3 citrullination with an EC50 of 2.1 μM in HEK293/PAD2 cells[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)

PAD2-IN-2 (AMF30a) protects K. pneumonia pneumonia mice from Imipenem-induced mortality increase[2].

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

分子量

466.51

Formula

C24H27FN6O3

CAS 号

2095107-57-4

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]. Muth A, et al. Development of a Selective Inhibitor of Protein Arginine Deiminase 2. J Med Chem. 2017 Apr 13;60(7):3198-3211.

    [2]. Ye C, et al. Inappropriate use of antibiotics exacerbates inflammation through OMV-induced pyroptosis in MDR Klebsiella pneumoniae infection. Cell Rep. 2021 Sep 21;36(12):109750.

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EN219

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。

EN219 

EN219 是一种特异性适中的作用于 RNF114 的 N 端半胱氨酸 C8 的合成共价配体, IC50为470 nM。EN219 抑制 RNF114 介导的自身泛素化和 p21 泛素化。

EN219

EN219 Chemical Structure

CAS No. : 380351-29-1

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生物活性

EN219 is a moderately selective synthetic covalent ligand against an N-terminal cysteine (C8) of RNF114 with an IC50 of 470 nM. EN219 inhibits RNF114-mediated autoubiquitination and p21 ubiquitination[1].

IC50 & Target[1]

RNF114

470 nM (IC50)

体外研究
(In Vitro)

EN219 (1 μM; 90 min) interacts with RNF114 C8, TUBB1 C201, HSPD1 C442, and HIST1H3A C97 demonstrated by isotopic tandem orthogonal proteolysisABPP (isoTOP-ABPP) analysis[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

456.56

Formula

C17H13Br2ClN2O

CAS 号

380351-29-1

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]. Luo M, et al. Chemoproteomics-enabled discovery of covalent RNF114-based degraders that mimic natural product function. Cell Chem Biol. 2021 Apr 15;28(4):559-566.e15.

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Decylubiquinone(Synonyms: 癸基泛醌)

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。

Decylubiquinone (Synonyms: 癸基泛醌)

Decylubiquinone 是泛醌 (辅酶 Q10) 的类似物。Decylubiquinone 阻止活性氧 (ROS) 的产生以响应谷胱甘肽消耗并抑制线粒体通透性转变的激活。

Decylubiquinone(Synonyms: 癸基泛醌)

Decylubiquinone Chemical Structure

CAS No. : 55486-00-5

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生物活性

Decylubiquinone is an analog of ubiquinone (coenzyme Q10). Decylubiquinone blocks reactive oxygen species (ROS) production in response to glutathione depletion and inhibits activation of the mitochondrial permeability transition[1].

体外研究
(In Vitro)

Decylubiquinone (dUb; 10 μm for 6 hours) exerts its effects on ROS by either inhibition of ROS production by cytochrome bc1 or that it scavenged ROS produced[1].
Decylubiquinone inhibits both the dichlorofluorescein (DCF) fluorescence increase resulting from H2O2 treatment and the DCF fluorescence increase resulting after glutathione (GSH) depletion using diethylmaleate mitochondrially generated ROS)[1].

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

Cell Viability Assay[1]

Cell Line: HL60 cells transfected with bcl-2 (bcl-2) (HL60 B cells)
Concentration: 10 μM
Incubation Time: 6 hours
Result: Attenuated the ROS increase in HL60 (B) cells.

分子量

322.44

Formula

C19H30O4

CAS 号

55486-00-5

中文名称

癸基泛醌

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]. Jeffrey S Armstrong, et al. The Coenzyme Q10 analog decylubiquinone inhibits the redox-activated mitochondrial permeability transition: role of mitcohondrial [correction mitochondrial] complex III. J Biol Chem. 2003 Dec 5;278(49):49079-84.

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Piperafizine A

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。

Piperafizine A 

Piperafizine A (化合物 4d’) 是一种 N-单烷基化普那布林衍生物。抗癌试剂。

Piperafizine A

Piperafizine A Chemical Structure

CAS No. : 130603-59-7

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生物活性

Piperafizine A (compound 4d’) is a N-monoalkylated plinabulin derivative. Anti-cancer reagent[1].

分子量

304.34

Formula

C19H16N2O2

CAS 号

130603-59-7

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]. Asha Ganesher, et al. One pot synthesis of N-monoalkylated plinabulin derivatives via multicomponent protocol and their application as anticancer agents. J Mol Struct. 2020;1229:129830.

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Nemadipine-A

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。

Nemadipine-A 

Nemadipine-A 是 EGL-19 Ca2+ 通道 (Ca2+ channel) 的特异性抑制剂。Nemadipine-A 是一种细胞渗透性 L 型钙通道抑制剂,可使对 TRAIL 抗性的癌细胞对该配体敏感。

Nemadipine-A

Nemadipine-A Chemical Structure

CAS No. : 54280-71-6

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生物活性

Nemadipine-A is a specific inhibitor of the EGL-19 L-type Ca2+ channel[1]. Nemadipine-A, a cell-permeable L-type calcium channel inhibitor, sensitizes TRAIL-resistant cancer cells to this ligand[2].

体外研究
(In Vitro)

Nemadipine-A is a specific and highly effective inhibitor of EGL-19. Nemadipine-A (µM) is sufficient to abolish the enhanced level of paralysis observed in egl-19(ad695); crIs4 mutants[1].
Nemadipine-A strongly potentiates TRAIL-induced apoptosis in TRAIL-resistant lung cancer cells via the down-regulation of the anti-apoptotic protein survivin[2]. Nemadipine-A sensitizes H1299 lung cancer cells towards TRAIL-induced cytotoxicity[2]. Combination of Nemadipine-A (20 μM) with TRAIL (20 ng/mL) induces caspase-mediated apoptotic cell death[2].

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

Cell Viability Assay[2]

Cell Line: H1299 lung adenocarcinoma cells
Concentration: 0, 5, 10, 20, and 30 μM
Incubation Time: 8 hours
Result: H1299 cells were resistant to the apoptotic effects of TRAIL, but the co-administration of Nemadipine-A and TRAIL in these cells resulted in notably increased cytotoxicity in a dose-dependent manner.

Western Blot Analysis[2]

Cell Line: H1299 cells
Concentration: 20 μM
Incubation Time: 8 hours
Result: Co-treated with TRAIL and Nemadipine-A (T/N; 20 ng/mL and 20 μM respectively) induced cell death in H1299 cells.

分子量

419.34

Formula

C19H18F5NO4

CAS 号

54280-71-6

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]. Peter I Joyce, et al. The atypical calpains: evolutionary analyses and roles in Caenorhabditis elegans cellular. PLoS Genet. 2012;8(3):e1002602.degeneration

    [2]. Seong Ho Park, et al. Down-Regulation of Survivin by Nemadipine-A Sensitizes Cancer Cells to TRAIL-Induced Apoptosis. Biomol Ther (Seoul). 2013 Jan;21(1):29-34.

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