YK5

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。

YK5 

YK5 是一种有效的选择性 Hsp70 抑制剂。YK5 在癌细胞中选择性地,紧密地与胞质 Hsp70s 结合。YK5 通过干扰活性致癌 Hsp70/Hsp90/ 配体蛋白复合物的形成而发挥其生物活性。

YK5

YK5 Chemical Structure

CAS No. : 1268273-23-9

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生物活性

YK5 is a potent and selective Hsp70 inhibitor. YK5 selectively and tightly binds to the cytosolic Hsp70s in cancer cells. YK5 has biological activity partly by interfering with the formation of active oncogenic Hsp70/Hsp90/client protein complexes[1].

IC50 & Target

HSP70

 

HSP90

 

体外研究
(In Vitro)

YK5 shows selectively and tightly binds to the cytosolic Hsp70s[1].
YK5 (0.5, 1, 5 µM; 72 h) degrades the expression of Hsp90/Hsp70-onco-client proteins and also leads to the inhibition of cell proliferation in SKBr3 cells[1].
YK5 (0.5, 1, 5 µM; 24 h) induces the degradation of HER2, Raf-1, Akt kinases, and also induces apoptosis in SKBr3 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 Proliferation Assay[1]

Cell Line: SKBr3 cells
Concentration: 0.5, 1, 5 µM
Incubation Time: 72 h
Result: Degraded the expression of Hsp90/Hsp70-onco-client proteins and also led to the inhibition of cell proliferation in SKBr3 cells.

Western Blot Analysis[1]

Cell Line: SKBr3 cells
Concentration: 0.5, 1, 5 µM
Incubation Time: 24 h
Result: Induced the degradation of HER2, Raf-1, Akt kinases, and also induced apoptosis in SKBr3 cells.

分子量

432.50

Formula

C18H24N8O3S

CAS 号

1268273-23-9

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]. Rodina A, et al. Identification of an allosteric pocket on human hsp70 reveals a mode of inhibition of this therapeutically important protein. Chem Biol. 2013 Dec 19;20(12):1469-80.

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Linamarin(Synonyms: Phaseolunatin)

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。

Linamarin (Synonyms: Phaseolunatin)

Linamarin 是一种天然产物,具有抗肿瘤活性。

Linamarin(Synonyms: Phaseolunatin)

Linamarin Chemical Structure

CAS No. : 554-35-8

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生物活性

Linamarin, a natural compound, possesses anticancer activity[1].

分子量

247.25

Formula

C10H17NO6

CAS 号

554-35-8

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]. Christopher Avwoghokoghene Idibie, et al. Cytotoxicity of purified cassava linamarin to a selected cancer cell lines. Bioprocess Biosyst Eng. 2007 Jul;30(4):261-9.

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AR antagonist 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。

AR antagonist 3 

AR antagonist 3 是一种有效的选择性 androgen receptor (AR) 拮抗剂,IC50 为 0.47 µM。AR antagonist 3 呈剂量依赖性降低 FRET 信号 (IC50= 18.05 μM)。当瘤内给药时,AR antagonist 3 可有效抑制肿瘤生长。

AR antagonist 3

AR antagonist 3 Chemical Structure

CAS No. : 349573-58-6

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生物活性

AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC50 of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally[1].

IC50 & Target

IC50: 0.47 µM (AR)[1]

体外研究
(In Vitro)

AR antagonist 3 (compound T1-12) (0.01, 0.1, 1, 10, 100 µM) shows excellent AR antagonistic activity (eGFP IC50= 0.47 μM; PSA IC50= 1.42 μM)[1].
AR antagonist 3 (0.01, 0.1, 1, 10, 100 µM) inhibits the proliferation of LNCaP cells[1].
AR antagonist 3 (0.1, 1, 10 µM; 48 h) reduces the protein expression levels of c-Myc and KLK3[1].
AR antagonist 3 (0.01, 0.1, 1, 10, 100 µM) exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM)[1].
AR antagonist 3 (10 µM; 2 h) reduces the DHT-mediated translocation of the AR into the nucleus in LNCaP cells[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: LNCaP-ARR2PB-eGFP cells
Concentration: 0.01, 0.1, 1, 10, 100 µM
Incubation Time:
Result: Showed excellent AR antagonistic activity (eGFP IC50= 0.47 μM; PSA IC50= 1.42 μM).

Cell Proliferation Assay[1]

Cell Line: LNCaP, 22Rv1, C4-2, PC3, DU145 cells
Concentration: 0.01, 0.1, 1, 10, 100 µM
Incubation Time: 3 days
Result: Inhibited the proliferation of LNCaP cells.

体内研究
(In Vivo)

AR antagonist 3 (intratumorally injected; 2.5 mg/kg; every week for 25 days) inhibits tumor growth and the final tumor growth inhibition is 65%[1].

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

Animal Model: 6 weeks-old male CB17 SCID mice (specificpathogen-free grade), 18-24 g[1]
Dosage: 2.5 mg/kg
Administration: intratumorally injected; week; 25 days
Result: Inhibited tumor growth and the final tumor growth inhibition is 65%.

分子量

306.38

Formula

C15H18N2O3S

CAS 号

349573-58-6

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]. Chai X, et al. Discovery of N-(4-(Benzyloxy)-phenyl)-sulfonamide Derivatives as Novel Antagonists of the Human Androgen Receptor Targeting the Activation Function 2. J Med Chem. 2022, 65(3):2507-2521.

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BGTC

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。

BGTC 

BGTC 是一种非氨基酸阳离子脂质。BGTC 可用于核酸递送。

BGTC

BGTC Chemical Structure

CAS No. : 182056-06-0

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生物活性

BGTC is a non-amino acid cationic lipid. BGTC can be used for delivery of nucleic acids[1].

分子量

642.96

Formula

C36H66N8O2

CAS 号

182056-06-0

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]. Hajri A, et, al. Combined suicide gene therapy for pancreatic peritoneal carcinomatosis using BGTC liposomes. Cancer Gene Ther. 2004 Jan;11(1):16-27.

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GRPR antagonist-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。

GRPR antagonist-1 

GRPR antagonist-1 是一种有效的胃泌素释放肽受体 (GRPR) 拮抗剂,对某些癌细胞具有细胞毒性 (在PC3、Pan02、HGC-27 细胞中的 IC50 分别是 4.97、4.36、3.40 μM)。GRPR antagonist-1 通过降低 Bcl-2 水平、增加 Bax 水平,来抑制 HGC-27 细胞活力,引起细胞凋亡。具有抗癌活性。

GRPR antagonist-1

GRPR antagonist-1 Chemical Structure

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生物活性

GRPR antagonist-1 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 4.97, 4.36 and 3.40 μM in PC3, Pan02 and HGC-27 cells, respectively). GRPR antagonist-1 inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis. Anticancer activity[1].

IC50 & Target

IC50: 4.97 μM (GRPR) in PC3, 4.36 μM (GRPR) in Pan02, 3.40 μM (GRPR) in HGC-27[1]

体外研究
(In Vitro)

GRPR antagonist-1 (compound 5a) (0.032-100 μM; 48 hours) has the cytotoxicity against certain cancer cells, also reduces PC3, Pan02, HGC-27, and HepG2 cell viability combined with HDAC inhibitor (1 μM)[1].
GRPR antagonist-1 (1, 2, 8 μM; 24 hours) increases the rate of late apoptosis/necrosis, inducing apoptosis of HGC-27 cells[1].
GRPR antagonist-1 (0.8, 4 μM; 24 hours) inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis[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 Proliferation Assay

Cell Line: PC3, HepG2, HGC-27, Pan02, and HK2 cells[1]
Concentration: 0.032-100 μM
Incubation Time: 48 hours
Result: Showed the cytotoxicity against these cancer cells, also reduced PC3, Pan02, HGC-27, and HepG2 cell viability combined with HDAC inhibitor (1 μM).

Apoptosis Analysis

Cell Line: HGC-27[1]
Concentration: 1, 2, 8 μM
Incubation Time: 24 hours
Result: Increased the rate of late apoptosis/necrosis, inducing apoptosis of HGC-27 cells.

Western Blot Analysis

Cell Line: HGC-27[1]
Concentration: 0.8, 4 μM
Incubation Time: 24 hours
Result: Inhibited HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis.

分子量

558.59

Formula

C29H33F3N4O4

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]. Yu, Mj., et al. Structure–activity relationship studies on Pd176252 derivatives leading to discovery of novel GRP receptor antagonist with potent anticancer activity. Med Chem Res 30, 2069–2089 (2021).

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DX3-213B

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。

DX3-213B 

DX3-213B 是一种高效口服活性氧化磷酸化 (OXPHOS) 复合物 I (complex I) 抑制剂 (IC50=3.6 nM)。DX3-213B 损害ATP生成 (IC50=11 nM),并阻止MIA PaCa-2 细胞生长 (GI50=11 nM)。DX3-213B 用于胰腺癌的研究。

DX3-213B

DX3-213B Chemical Structure

CAS No. : 2749555-66-4

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生物活性

DX3-213B is a highly potent, orally active oxidative phosphorylation (OXPHOS) complex I inhibitor (IC50=3.6 nM). DX3-213B impairs ATP generation (IC50=11 nM), and blocks MIA PaCa-2 cell growth (GI50=11 nM). DX3-213B is used for the research of the pancreatic cancer[1].

分子量

478.57

Formula

C20H28F2N2O5S2

CAS 号

2749555-66-4

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]. Xue D, et al. Multiparameter Optimization of Oxidative Phosphorylation Inhibitors for the Treatment of Pancreatic Cancer. J Med Chem. 2022;65(4):3404-3419.

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Trk-IN-9

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。

Trk-IN-9 

Trk-IN-9 (Compound 12) 是一种有效的 TRK 抑制剂。Trk-IN-9 抑制 Km-12 细胞系的增殖。Trk-IN-9 以浓度依赖性方式诱导 Km-12 细胞凋亡。Trk-IN-9 抑制 TRK 的磷酸化以阻断下游通路。Trk-IN-9具有研究NTRK融合癌症的潜力。

Trk-IN-9

Trk-IN-9 Chemical Structure

CAS No. : 2758623-12-8

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生物活性

Trk-IN-9 (Compound 12) is a potent inhibitor of TRK. Trk-IN-9 inhibits the proliferation of Km-12 cell lines. Trk-IN-9 induces the apoptosis of Km-12 cells in a concentration-dependent manner. Trk-IN-9 inhibits the phosphorylation of TRK to block downstream pathways. Trk-IN-9 has the potential for the research of NTRK-fusion cancers[1].

分子量

454.93

Formula

C23H24ClFN6O

CAS 号

2758623-12-8

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]. Wu T, et al. Rational drug design to explore the structure-activity relationship (SAR) of TRK inhibitors with 2,4-diaminopyrimidine scaffold. Eur J Med Chem. 2022;230:114096.

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GRPR antagonist-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。

GRPR antagonist-2 

GRPR antagonist-2 是一种有效的胃泌素释放肽受体 (GRPR) 拮抗剂,对某些癌细胞具有细胞毒性 (在 HGC-27 和 Pan02 细胞中的 IC50 分别是 0.77 和 2.5 μM)。具有抗癌活性。

GRPR antagonist-2

GRPR antagonist-2 Chemical Structure

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生物活性

GRPR antagonist-2 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 0.77 and 2.5 μM in HGC-27 and Pan02 cells, respectively). Anticancer activity[1].

IC50 & Target

IC50: 0.77 μM (GRPR) in HGC-27, 2.5 μM (GRPR) in Pan02[1]

体外研究
(In Vitro)

GRPR antagonist-2 (compound 6e) (0.032-100 μM; 48 hours) has the cytotoxicity against certain cancer cells, also reduces PC3, Pan02, HGC-27, and HepG2 cell viability combined with HDAC inhibitor (1 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.

Cell Proliferation Assay

Cell Line: PC3, HepG2, HGC-27, Pan02, and HK2 cells[1]
Concentration: 0.032-100 μM
Incubation Time: 48 hours
Result: Showed the cytotoxicity against these cancer cells, also reduced PC3, Pan02, HGC-27, and HepG2 cell viability combined with HDAC inhibitor (1 μM).

分子量

559.58

Formula

C28H32F3N5O4

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]. Yu, Mj., et al. Structure–activity relationship studies on Pd176252 derivatives leading to discovery of novel GRP receptor antagonist with potent anticancer activity. Med Chem Res 30, 2069–2089 (2021).

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10Z-Hymenialdisine(Synonyms: (Z)-Hymenialdisine; Hymenialdisine)

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。

10Z-Hymenialdisine (Synonyms: (Z)-Hymenialdisine; Hymenialdisine)

10Z-Hymenialdisine ((Z)-Hymenialdisine) 是一种天然的生物活性吡咯生物碱。10Z-Hymenialdisine 是一种泛激酶抑制剂,具有抗癌活性。

10Z-Hymenialdisine(Synonyms: (Z)-Hymenialdisine;  Hymenialdisine)

10Z-Hymenialdisine Chemical Structure

CAS No. : 82005-12-7

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生物活性

10Z-Hymenialdisine ((Z)-Hymenialdisine) is a natural bioactive pyrrole alkaloid. 10Z-Hymenialdisine is a pan kinase inhibitor, and has anticancer activities[1].

体外研究
(In Vitro)

10Z-Hymenialdisine displays a moderate effect on (ARK5, VEGFR-2, SAK and PDGFR) protein kinases. 10Z-Hymenialdisine shows a potent inhibition of RAF/MEK-1/MAPK cascade with an IC50 value of 6 nM[1].

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

分子量

324.13

Formula

C11H10BrN5O2

CAS 号

82005-12-7

中文名称

2,5-已炔二醇;已炔二醇

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]. Ashraf N E Hamed, et al. Bioactive pyrrole alkaloids isolated from the Red Sea: marine sponge Stylissa carteri. Z Naturforsch C J Biosci. 2018 Apr 25;73(5-6):199-210.

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Keap1-Nrf2-IN-4

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。

Keap1-Nrf2-IN-4 

Keap1-Nrf2-IN-4 是一种有效的 neddylation 抑制剂。Keap1-Nrf2-IN-4 对 MGC-803 细胞表现出较强的抗增殖活性 (IC50=2.55 µM)。Keap1-Nrf2-IN-4 阻断胃癌细胞的迁移能力并诱导细胞凋亡 apoptosis。Keap1-Nrf2-IN-4 抑制肿瘤生长且无明显毒性。

Keap1-Nrf2-IN-4

Keap1-Nrf2-IN-4 Chemical Structure

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生物活性

Keap1-Nrf2-IN-4 is a potent neddylation inhibitor. Keap1-Nrf2-IN-4 exhibits potent anti-proliferation activity against MGC-803 cells (IC50=2.55 µM). Keap1-Nrf2-IN-4 blocks the migration ability and induces apoptosis of gastric cancer cells. Keap1-Nrf2-IN-4 inhibits tumor growth without obvious toxicity[1].

体外研究
(In Vitro)

Keap1-Nrf2-IN-4 (compound 4g) (72 h) shows anti-proliferation activity (IC50 s of 2.55, 3.88, 3.74, 2.89 µM in MGC-803, MCF-7, A549, HepG-2 cells, respectively)[1].
Keap1-Nrf2-IN-4 inhibits neddylation of cullin1, cullin3, cullin5[1].
Keap1-Nrf2-IN-4 blocks the migration ability of MGC-803 without cell cycle arrest[1].
Keap1-Nrf2-IN-4 (24, 48 h) induces apoptosis of MGC-803 and HGC-27 cells in concentration- and time-dependent manners[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 Proliferation Assay[1]

Cell Line: MGC-803, MCF-7, A549, HepG-2 cells
Concentration:
Incubation Time: 72 h
Result: Showed anti-proliferation activity (IC50 of 2.55, 3.88, 3.74, 2.89 µM in MGC-803, MCF-7, A549, HepG-2 cells, respectively).

Apoptosis Analysis[1]

Cell Line: MGC-803, HGC-27 cells
Concentration: 2.5, 5, 7.5 µM for MGC-803 cells; 3, 6, 9 µM for HGC-27 cells
Incubation Time: 24 h, 48 h
Result: Induced apoptosis of MGC-803 and HGC-27 cells in concentration- and time-dependent manners.

体内研究
(In Vivo)

Keap1-Nrf2-IN-4 (50, 100 mg/kg; i.g.; per day for 21 days) exhibits antitumor activity on xenograft model without obvious side effect[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: 5-6 weeks, 18-20 g, NOD SCID mice (xenograft tumor model)[1]
Dosage: 50, 100 mg/kg
Administration: i.g.; per day, 21 days
Result: Exihibited good antitumor activity on xenograft model without obvious side effect.

分子量

390.56

Formula

C26H34N2O

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 B, et al. Discovery of a cinnamyl piperidine derivative as new neddylation inhibitor for gastric cancer treatment. Eur J Med Chem. 2021; 226:113896.

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TRK-IN-12

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。

TRK-IN-12 

TRK-IN-12 (Compound 9e) 是一种有效的 TRK 抑制剂 (TRKG595R IC50 = 13.1 nM)。TRK-IN-12 是一种大环衍生化合物。TRK-IN-12 在 Ba/F3-LMNA-NTRK1 细胞系中显示出显着的抗增殖活性 (IC50 = 0.080 μM)。TRK-IN-12 在 Ba/F3-LMNA-NTRK1-G595R 细胞系中显示出比对照药物 LOXO-101 更好的抑制作用 (IC50 = 0.646 μM)。

TRK-IN-12

TRK-IN-12 Chemical Structure

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生物活性

TRK-IN-12 (Compound 9e) is a potent inhibitor of TRK (TRKG595R IC50 = 13.1 nM). TRK-IN-12 is a macrocyclic derivative compound. TRK-IN-12 shows significant antiproliferative activity in the Ba/F3-LMNA-NTRK1 cell line (IC50 = 0.080 μM). TRK-IN-12 has shown a better inhibitory effect (IC50 = 0.646 μM) than control drug LOXO-101 in Ba/F3-LMNA-NTRK1-G595R cell line[1].

分子量

439.89

Formula

C18H19ClFN5O3S

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]. Li P, et al. Design, synthesis and biological evaluation of macrocyclic derivatives as TRK inhibitors [published correction appears in Bioorg Med Chem Lett. 2022 Jan 15;56:128502]. Bioorg Med Chem Lett. 2021;53:128409.

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4-Methyl withaferin 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。

4-Methyl withaferin A 

4-Methyl withaferin A 是 withaferin A 类似物,具有抗肿瘤活性。

4-Methyl withaferin A

4-Methyl withaferin A Chemical Structure

CAS No. : 1777780-94-5

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生物活性

4-Methyl withaferin A is a withaferin A-analogue with anti-tumor activity[1].

体外研究
(In Vitro)

Methyl withaferin A is against HeLa cell, A-549 cell, and MCF-7 cells with IC50 values of 2.1±0.01 µM,4.0±0.5 µM, and 1.1±0.2 µM, respectively.

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

分子量

484.62

Formula

C29H40O6

CAS 号

1777780-94-5

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]. Gabriel G Llanos, et al. Structure-based design, synthesis, and biological evaluation of withaferin A-analogues as potent apoptotic inducers. Eur J Med Chem. 2017 Nov 10;140:52-64.

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AR antagonist 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。

AR antagonist 3 

AR antagonist 3 是一种有效的选择性 androgen receptor (AR) 拮抗剂,IC50 为 0.47 µM。AR antagonist 3 呈剂量依赖性降低 FRET 信号 (IC50= 18.05 μM)。当瘤内给药时,AR antagonist 3 可有效抑制肿瘤生长。

AR antagonist 3

AR antagonist 3 Chemical Structure

CAS No. : 349573-58-6

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生物活性

AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC50 of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally[1].

IC50 & Target

IC50: 0.47 µM (AR)[1]

体外研究
(In Vitro)

AR antagonist 3 (compound T1-12) (0.01, 0.1, 1, 10, 100 µM) shows excellent AR antagonistic activity (eGFP IC50= 0.47 μM; PSA IC50= 1.42 μM)[1].
AR antagonist 3 (0.01, 0.1, 1, 10, 100 µM) inhibits the proliferation of LNCaP cells[1].
AR antagonist 3 (0.1, 1, 10 µM; 48 h) reduces the protein expression levels of c-Myc and KLK3[1].
AR antagonist 3 (0.01, 0.1, 1, 10, 100 µM) exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM)[1].
AR antagonist 3 (10 µM; 2 h) reduces the DHT-mediated translocation of the AR into the nucleus in LNCaP 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: LNCaP-ARR2PB-eGFP cells
Concentration: 0.01, 0.1, 1, 10, 100 µM
Incubation Time:
Result: Showed excellent AR antagonistic activity (eGFP IC50= 0.47 μM; PSA IC50= 1.42 μM).

Cell Proliferation Assay[1]

Cell Line: LNCaP, 22Rv1, C4-2, PC3, DU145 cells
Concentration: 0.01, 0.1, 1, 10, 100 µM
Incubation Time: 3 days
Result: Inhibited the proliferation of LNCaP cells.

体内研究
(In Vivo)

AR antagonist 3 (intratumorally injected; 2.5 mg/kg; every week for 25 days) inhibits tumor growth and the final tumor growth inhibition is 65%[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: 6 weeks-old male CB17 SCID mice (specificpathogen-free grade), 18-24 g[1]
Dosage: 2.5 mg/kg
Administration: intratumorally injected; week; 25 days
Result: Inhibited tumor growth and the final tumor growth inhibition is 65%.

分子量

306.38

Formula

C15H18N2O3S

CAS 号

349573-58-6

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]. Chai X, et al. Discovery of N-(4-(Benzyloxy)-phenyl)-sulfonamide Derivatives as Novel Antagonists of the Human Androgen Receptor Targeting the Activation Function 2. J Med Chem. 2022, 65(3):2507-2521.

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Octanal

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。

Octanal 

Octanal 是一种芳香醛,具有抗氧化和抗菌活性。Octanal 对 Hela 细胞具有细胞毒性。

Octanal

Octanal Chemical Structure

CAS No. : 124-13-0

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生物活性

Octanal is an aromatic aldehyde, with antioxidant and antimicrobial activities. Octanal shows cytotoxicity against Hela cells[1].

IC50 & Target

Human Endogenous Metabolite

 

分子量

128.21

Formula

C8H16O

CAS 号

124-13-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Pure form -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
  • [1]. Kehai Liu, et al. Isolation and biological activities of decanal, linalool, valencene, and octanal from sweet orange oil. J Food Sci. 2012 Nov;77(11):C1156-61.

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Roslin 2 bromide(Synonyms: Benzylhexamethylenetetramine bromide)

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。

Roslin 2 bromide (Synonyms: Benzylhexamethylenetetramine bromide)

Roslin 2 bromide (Benzylhexamethylenetetramine bromide) 是一种具有抗癌作用的 p53 再激活剂。Roslin 2 bromide 结合 FAK,破坏 FAK 和 p53 的结合。

Roslin 2 bromide(Synonyms: Benzylhexamethylenetetramine bromide)

Roslin 2 bromide Chemical Structure

CAS No. : 29574-21-8

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生物活性

Roslin 2 bromide (Benzylhexamethylenetetramine bromide) is a p53 reactivator with anticancer effects. Roslin 2 bromide binds FAK, disrupts the binding of FAK and p53[1].

体外研究
(In Vitro)

Roslin 2 bromide decreases cancer cell viability and clonogenicity in a p53-dependent manner. Roslin 2 bromide increases p53 transcriptional activity that is inhibited by FAK using p21, Mdm-2, and Bax-promoter targets. Roslin 2 bromide also causes increased expression of p53 targets: p21, Mdm-2 and Bax proteins[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)

Roslin 2 (60 mg/kg; i.p; 5 days/week) bromide significantly decreases tumor growth, disrupts the complex of FAK and p53, and up-regulates p21 in HCT116 p53+/+ but not in HCT116 p53-/- xenografts in vivo[1].

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

分子量

311.22

Formula

C13H19BrN4

CAS 号

29574-21-8

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]. Vita M Golubovskaya, et al. Disruption of focal adhesion kinase and p53 interaction with small molecule compound R2 reactivated p53 and blocked tumor growth. BMC Cancer. 2013 Jul 11;13:342.

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DX3-213B

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。

DX3-213B 

DX3-213B 是一种高效口服活性氧化磷酸化 (OXPHOS) 复合物 I (complex I) 抑制剂 (IC50=3.6 nM)。DX3-213B 损害ATP生成 (IC50=11 nM),并阻止MIA PaCa-2 细胞生长 (GI50=11 nM)。DX3-213B 用于胰腺癌的研究。

DX3-213B

DX3-213B Chemical Structure

CAS No. : 2749555-66-4

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生物活性

DX3-213B is a highly potent, orally active oxidative phosphorylation (OXPHOS) complex I inhibitor (IC50=3.6 nM). DX3-213B impairs ATP generation (IC50=11 nM), and blocks MIA PaCa-2 cell growth (GI50=11 nM). DX3-213B is used for the research of the pancreatic cancer[1].

分子量

478.57

Formula

C20H28F2N2O5S2

CAS 号

2749555-66-4

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]. Xue D, et al. Multiparameter Optimization of Oxidative Phosphorylation Inhibitors for the Treatment of Pancreatic Cancer. J Med Chem. 2022;65(4):3404-3419.

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2-NP

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。

2-NP 

2-NP 是一种选择性的 STAT1 转录增强剂。2-NP 可以增强 IFN-γ 抑制人乳腺癌和纤维肉瘤细胞增殖的能力。

2-NP

2-NP Chemical Structure

CAS No. : 65182-56-1

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生物活性

2-NP is a selective enhancer of STAT1 transcription. 2-NP can enhance the ability of IFN-γ to inhibit the proliferation of human breast cancer and fibrosarcoma cells[1].

分子量

222.25

Formula

C14H10N2O

CAS 号

65182-56-1

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]. Lynch RA, et, al. A small-molecule enhancer of signal transducer and activator of transcription 1 transcriptional activity accentuates the antiproliferative effects of IFN-gamma in human cancer cells. Cancer Res. 2007 Feb 1;67(3):1254-61.

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5,15-Diphenylporphyrin(Synonyms: 5,15-DPP)

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。

5,15-Diphenylporphyrin (Synonyms: 5,15-DPP)

5,15-Diphenylporphyrin (5,15-DPP) 是一种选择性 STAT3-SH2 拮抗剂,对 STAT3 和 STAT1 的 IC50 分别为 0.28 µM 和 10 µM。

5,15-Diphenylporphyrin(Synonyms: 5,15-DPP)

5,15-Diphenylporphyrin Chemical Structure

CAS No. : 22112-89-6

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生物活性

5,15-Diphenylporphyrin (5,15-DPP) is a selective STAT3-SH2 antagonist (IC50s of 0.28 µM and 10 µM for STAT3 and STAT1, respectively)[1].

分子量

462.54

Formula

C32H22N4

CAS 号

22112-89-6

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]. Uehara Y, et al. Novel high-throughput screening system for identifying STAT3-SH2 antagonists. Biochem Biophys Res Commun. 2009;380(3):627-631.

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Trk-IN-9

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。

Trk-IN-9 

Trk-IN-9 (Compound 12) 是一种有效的 TRK 抑制剂。Trk-IN-9 抑制 Km-12 细胞系的增殖。Trk-IN-9 以浓度依赖性方式诱导 Km-12 细胞凋亡。Trk-IN-9 抑制 TRK 的磷酸化以阻断下游通路。Trk-IN-9具有研究NTRK融合癌症的潜力。

Trk-IN-9

Trk-IN-9 Chemical Structure

CAS No. : 2758623-12-8

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生物活性

Trk-IN-9 (Compound 12) is a potent inhibitor of TRK. Trk-IN-9 inhibits the proliferation of Km-12 cell lines. Trk-IN-9 induces the apoptosis of Km-12 cells in a concentration-dependent manner. Trk-IN-9 inhibits the phosphorylation of TRK to block downstream pathways. Trk-IN-9 has the potential for the research of NTRK-fusion cancers[1].

分子量

454.93

Formula

C23H24ClFN6O

CAS 号

2758623-12-8

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]. Wu T, et al. Rational drug design to explore the structure-activity relationship (SAR) of TRK inhibitors with 2,4-diaminopyrimidine scaffold. Eur J Med Chem. 2022;230:114096.

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Linamarin(Synonyms: Phaseolunatin)

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。

Linamarin (Synonyms: Phaseolunatin)

Linamarin 是一种天然产物,具有抗肿瘤活性。

Linamarin(Synonyms: Phaseolunatin)

Linamarin Chemical Structure

CAS No. : 554-35-8

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生物活性

Linamarin, a natural compound, possesses anticancer activity[1].

分子量

247.25

Formula

C10H17NO6

CAS 号

554-35-8

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]. Christopher Avwoghokoghene Idibie, et al. Cytotoxicity of purified cassava linamarin to a selected cancer cell lines. Bioprocess Biosyst Eng. 2007 Jul;30(4):261-9.

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