Carbonic anhydrase inhibitor 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。

Carbonic anhydrase inhibitor 12 

碳酸酐酶抑制剂12是一种有效的 CA II 抑制剂,对 CA I 也有抑制活性(CA II与CA I的 Kis分别为1.72 nM和271 nM)。碳酸酐酶抑制剂12对不同的肿瘤细胞系具有较强的抗癌活性。

Carbonic anhydrase inhibitor 12

Carbonic anhydrase inhibitor 12 Chemical Structure

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生物活性

Carbonic anhydrase inhibitor 12 is a potent CA II inhibitor, also has inhibitory activity in CA I (Kis of 1.72 and 271 nM in CA II and CA I, respectively). Carbonic anhydrase inhibitor 12 has potent anticancer activity against different cancer cell lines[1].

IC50 & Target

Ki: 1.72 nM (CA II), 271 nM (CA I)[1]

体外研究
(In Vitro)

Carbonic anhydrase inhibitor 12 (Compound 14h) (10 μM; 48 hours; single) has great influence on the specificity and the inhibitory potency against the different cancer cell lines[1].
Carbonic anhydrase inhibitor 12 (2.4 μM in MCF-7 and 2.5 μM MDA-MB-231; 48 hours) can arrest the cell cycle of MCF-7 and MDA-MB-231 cells at the G2/M phase[1].
Carbonic anhydrase inhibitor 12 (2.4 μM in MCF-7 and 2.5 μM MDA-MB-231; 48 hours) demonstrates an increase in the early apoptotic and late apoptotic phase in comparison to the control untreated cells[1].

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

Cell Proliferation Assay

Cell Line: MCF-7, T47D, MDA-MB-231, COLO 205, HCT-116, HT29, SW-620, A549, SK-OV-3 and NCI-ADR-RES[1]
Concentration: 10 μM
Incubation Time: 48 hours
Result: Showed a mean growth inhibitory activity of 55.12% and a broad range of antiproliferative activity against most of the tested cancer cell lines.

Cell Cycle Analysis

Cell Line: MCF-7 and MDA-MB-231[1]
Concentration: 2.4 μM in MCF-7, 2.5 μM MDA-MB-231
Incubation Time: 48 hours
Result: Arrested the cell cycle of MCF-7 and MDA-MB-231 cells at the G2/M phase.

Apoptosis Analysis

Cell Line: MCF-7 and MDA-MB-231[1]
Concentration: 2.4 μM in MCF-7, 2.5 μM MDA-MB-231
Incubation Time: 48 hours
Result: Demonstrated an increase in the early apoptotic and late apoptotic phase in comparison to the control untreated cells.

分子量

640.53

Formula

C27H22BrN5O5S2

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]. Abdel-Mohsen HT, et al. Application of the dual-tail approach for the design and synthesis of novel Thiopyrimidine-Benzenesulfonamide hybrids as selective carbonic anhydrase inhibitors. Eur J Med Chem. 2022;228:114004.

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(Rac)-BIO8898

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。

(Rac)-BIO8898 

(Rac)-BIO8898 是一种 CD40-CD154 共刺激相互作用抑制剂。(Rac)-BIO8898 抑制 CD154 与 CD40-Ig 结合,IC50 为 25 μM。

(Rac)-BIO8898

(Rac)-BIO8898 Chemical Structure

CAS No. : 402564-79-8

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生物活性

(Rac)-BIO8898 is a CD40-CD154 co-stimulatory interaction inhibitor. (Rac)-BIO8898 inhibits CD154 binding to CD40-Ig with an IC50 of 25 μM[1].

分子量

909.13

Formula

C53H64N8O6

CAS 号

402564-79-8

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]. Laura F Silvian, et al. Small molecule inhibition of the TNF family cytokine CD40 ligand through a subunit fracture mechanism. ACS Chem Biol. 2011 Jun 17;6(6):636-47.

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EGFR-IN-30

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。

EGFR-IN-30 

EGFR-IN-30 是一种有效的 EGFR 抑制剂,对 EGFR (WT)、EGFR (L858R/T790M/C797S) 的 IC50 分别为 1-10 nM、<1 nM。EGFR-IN-30 具有用于细胞增殖类疾病,类如肿瘤等研究的潜力。

EGFR-IN-30

EGFR-IN-30 Chemical Structure

CAS No. : 2726463-68-7

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生物活性

EGFR-IN-30 is a potent EGFR inhibitor with IC50s of 1-10 nM, <1 nm for egfr (wt), (l858r>[1].

IC50 & Target[1]

EGFR (WT)

1-10 nM (IC50)

EGFR (L858R/T790M/C797S)

<1 nM (IC50)

体外研究
(In Vitro)

EGFR-IN-30 (compound 27) inhibits A431 cell (IC50=100-1000 nM),Ba/F3_L858R/T790M/C797S cell (IC50<10 nm), ba>50<10 nm)[1].

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

分子量

610.49

Formula

C28H33BrN7O2P

CAS 号

2726463-68-7

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]. Shansong Zheng, et al. Tricyclic compounds as EGFR inhibitors. WO2021208918A1.

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DHODH-IN-19

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。

DHODH-IN-19 

DHODH-IN-19 是一种有效的 DHODH 抑制剂。DHODH 存在于人类线粒体的内膜中,是一种含铁的黄素依赖性酶。DHODH-IN-19 抑制肿瘤生长。DHODH-IN-19具有研究癌症和炎症疾病的潜力 (摘自专利 WO2021238881A1,化合物 1)。

DHODH-IN-19

DHODH-IN-19 Chemical Structure

CAS No. : 2742675-85-8

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生物活性

DHODH-IN-19 is a potent inhibitor of DHODH. DHODH is present in the inner membrane of human mitochondria and is an iron-containing flavin-dependent enzyme. DHODH-IN-19 inhibits tumor growth. DHODH-IN-19 has the potential for the research of cancer and inflammation disease (extracted from patent WO2021238881A1, compound 1)[1].

分子量

521.84

Formula

C22H18ClF6N3O3

CAS 号

2742675-85-8

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]. Shuhui Chen, et al. Triazolones. Patent WO2021238881A1.

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TMI-1(Synonyms: WAY-171318)

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。

TMI-1 (Synonyms: WAY-171318)

TMI-1 是去整合素金属酶 17 (ADAM17) 和其它基质金属蛋白酶 MMPs 的有效抑制剂。TMI-1 能有效抑制 LPS 诱导的人原代单核细胞和人全血中 TNF-α 的分泌。TMI-1 在三阴性 (TN) 和 ERBB2 过度表达的乳腺肿瘤细胞系中选择性诱导 Caspase 依赖的细胞凋亡。

TMI-1(Synonyms: WAY-171318)

TMI-1 Chemical Structure

CAS No. : 287403-39-8

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生物活性

TMI-1 is a potent inhibitor of disintegrin metalloenzyme 17 (ADAM17) and other MMPs. TMI-1 inhibits LPS-induced TNF-α secretion in human primary monocytes, and human whole blood[1]. TMI-1 selectively induces caspase-dependent apoptosis in triple negative (TN) and ERBB2-overexpressing breast tumor cell lines[2].

IC50 & Target

ADAM17

8.4 nM (IC50)

分子量

398.50

Formula

C17H22N2O5S2

CAS 号

287403-39-8

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]. Zhang Y, et al. Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-converting enzyme/matrix metalloprotease inhibitor for the treatment of rheumatoid arthritis. J Pharmacol Exp Ther. 2004 Apr;309(1):348-55.

    [2]. Mezil L, et al. Tumor selective cytotoxic action of a thiomorpholin hydroxamate inhibitor (TMI-1) in breast cancer. PLoS One. 2012;7(9):e43409.

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SHR902275

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。

SHR902275 

SHR902275 是一种有效、选择性和口服活性 RAF 抑制剂,靶向 RAS 突变癌症。 对于 cRAF、bRAFwt 和 bRAFV600E,SHR902275 对 cRAF, bRAFwt, bRAFV600EIC50 分别为 1.6 nM、10 nM、5.7 nM。 SHR902275 显示细胞生长抑制作用,对 H358、A375、Calu6 和 SK-MEL2 细胞的 GI50 分别为 1.5 和 0.17 nM、0.4 nM 和 0.32 nM .

SHR902275

SHR902275 Chemical Structure

CAS No. : 2695506-82-0

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生物活性

SHR902275 is a potent, selective, and orally active RAF inhibitor targeting RAS mutant cancers. SHR902275 has IC50s of 1.6 nM, 10 nM, and 5.7 nM for cRAF, bRAFwt, and bRAFV600E, respectively. SHR902275 shows cell growth inhibition with GI50s of 1.5 and 0.17 nM, 0.4 nM and 0.32 nM for H358, A375, Calu6, and SK-MEL2 cells respectively[1].

IC50 & Target[1]

c-Raf

1.6 nM (IC50)

BRafV600E

5.7 nM (IC50)

BRAFWT

10 nM (IC50)

分子量

512.48

Formula

C26H23F3N4O4

CAS 号

2695506-82-0

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]. Zhao P, et al. Discovery of spiro amide SHR902275: A potent, selective, and efficacious RAF inhibitor targeting RAS mutant cancers. Eur J Med Chem. 2022;228:114040.

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UR-MB108

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。

UR-MB108 

UR-MB108 (Compound 57) 是一种有效的、选择性的 ABCG2 (BCRP) 抑制剂,IC50 值为 79 nM。UR-MB108 在血浆中很稳定。

UR-MB108

UR-MB108 Chemical Structure

CAS No. : 2412461-98-2

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生物活性

UR-MB108 (Compound 57) is a potent, selective ABCG2 (BCRP) inhibitor with an IC50 of 79 nM. UR-MB108 is stable in blood plasma[1].

IC50 & Target

IC50: 79 nM (ABCG2 (BCRP))[1]

分子量

666.77

Formula

C40H38N6O4

CAS 号

2412461-98-2

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]. Frauke Antoni, et al. Tariquidar-related triazoles as potent, selective and stable inhibitors of ABCG2 (BCRP). Eur J Med Chem. 2020 Apr 1;191:112133.

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DHODH-IN-20

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。

DHODH-IN-20 

DHODH-IN-20 (Compound 133) 是一种有效的 DHODH 抑制剂。DHODH 存在于人类线粒体的内膜中,是一种含铁的黄素依赖性酶。DHODH-IN-20 抑制肿瘤生长。DHODH-IN-20 具有研究急性髓细胞白血病的潜力。

DHODH-IN-20

DHODH-IN-20 Chemical Structure

CAS No. : 2639835-02-0

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生物活性

DHODH-IN-20 (Compound 133) is a potent inhibitor of DHODH. DHODH is present in the inner membrane of human mitochondria and is an iron-containing flavin-dependent enzyme. DHODH-IN-20 inhibits tumor growth. DHODH-IN-20 has the potential for the research of acute myelogenous leukemia[1].

分子量

479.47

Formula

C24H25F4N3O3

CAS 号

2639835-02-0

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]. Sabnis RW. Biaryl Compounds as Dihydroorotate Dehydrogenase Inhibitors for Treating Acute Myelogenous Leukemia (AML). ACS Med Chem Lett. 2022;13(2):158-159.

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HPK1-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。

HPK1-IN-21 

HPK1-IN-21 是一种有效的 HPK1 激酶抑制剂 (Ki=0.8 nM),HPK1-IN-21 也具有口服活性。

HPK1-IN-21

HPK1-IN-21 Chemical Structure

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生物活性

HPK1-IN-21 is a potent inhibitor of HPK1 kinase inhibitor (Ki=0.8 nM), HPK1-IN-21 also has orally active[1].

IC50 & Target

HPK1

0.8 nM (Ki)

体外研究
(In Vitro)

HPK1-IN-21 (compound 25; 0.001, 0.01, 0.1, 1, 10, 100 μM, 4 hours) inhibits the activity of HPK1 kinase[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 pan T cells
Concentration: 0.001, 0.01, 0.1, 1, 10, 100 μM
Incubation Time: 4 hours
Result: Resulted in the inhibition of HPK1 kinase activity

体内研究
(In Vivo)

HPK1-IN-21 (1, 25 mg/kg) shows 13% oral bioavailability in mouse when oral dose used 25 mg/kg[1]. Pharmacokinetic Parameters of HPK1-IN-21 in mice
[1]

compd LM H/R/Ma,d Hep H/R/Mb,d mouse iv CL,Vssc mouse F%c
25 6.9/8.7/38 9.5/18/33 57,1.9 13%


aLM = Liver microsome predicted clearance (mL/min/kg), H =human, R = rat, M = mouse. bHep = Hepatocyte clearance measuredin mL/min/kg, H = human, R = rat, M = mouse. cMouse PK:C57BL/6, 1 mg/kg iv dose or 25 mg/kg po dose, blood clearance measured in mL/min/kg, Vss = volume of distribution (L/kg). dHLM and Hep clearance values represent arithmetic means of two determinations. Six female (6-9 weeks) C57BL/6 mice, 15-25 g, 1 mg/kg iv (solution in 35% PEG400 in water); 25 mg/kg po (suspension in 0.5% methylcellulose, 0.2% Tween in water)[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: Six female (6-9 weeks) C57BL/6 mice, 15-25 g[1]
Dosage: 1, 25 mg/kg
Administration:
Result: Showed 13% oral bioavailability in mice when oral dose used 25 mg/kg.

分子量

445.92

Formula

C22H25ClFN5O2

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]. Discovery of Spiro-azaindoline Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1). ACS Med Chem Lett. 2021, 13(1):84-91.

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Cicaprost(Synonyms: ZK 96480)

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。

Cicaprost (Synonyms: ZK 96480)

Cicaprost (ZK 96480) 是一种前列环素受体 (IP) 激动剂。Cicaprost可引起动脉的浓度依赖性舒张,EC50 为 5.8 nM 。

Cicaprost(Synonyms: ZK 96480)

Cicaprost Chemical Structure

CAS No. : 94079-80-8

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生物活性

Cicaprost (ZK 96480) is a prostacyclin receptor (IP) agonist. Cicaprost causes a concentration-dependent relaxation of the artery with an EC50 of 5.8 nM [1]

体外研究
(In Vitro)

Cicaprost significantly reduces proliferation of human pulmonary artery smooth muscle cells (HPASMC) stimulated by fetal bovine serum (FBS). Cicaprost displays marked antiproliferative activity at 30 nM[2].
Cicaprost stimulates [3H]cyclic AMP production with EC50 values of 1.5-22 nM, and stimulates [3H]inositol phosphate production (EC50 values 49-457 nM) in all but the SK-N-SH cells[3].

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: HPASMC
Concentration: 10 pM, 100 pM, 1 nM, 10 nM, 100 nM, 1 μM, and 10 μM
Incubation Time:
Result: Dose-dependently inhibited proliferation with an EC50 of 24.1 nM.

体内研究
(In Vivo)

Cicaprost alters pain perception and inflammatory response in mice lacking prostacyclin receptor. Intravenous injection of Cicaprost (1 μg/kg) causes hypotension of ∼30 mm Hg in anaesthetized wild-type mice[4].

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

Animal Model: Wild-type (+/+) and IP−/− mice[4]
Dosage: 1 μg/kg
Administration: Intravenous injection
Result: Caused hypotension of ∼30 mm Hg in anaesthetized wild-type mice, whereas there was no change in blood pressure in IP-deficient mice even at 10 μg/kg.

分子量

374.47

Formula

C22H30O5

CAS 号

94079-80-8

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]. Nicole Ferko, et al. NO synergism with cicaprost in the canine pulmonary artery. BioPharm Journal ONLINE 2:2 (1998).

    [2]. Lucie H Clapp, et al. Differential effects of stable prostacyclin analogs on smooth muscle proliferation and cyclic AMP generation in human pulmonary artery. Am J Respir Cell Mol Biol. 2002 Feb;26(2):194-201.

    [3]. Kevin B S Chow, et al. Protein kinase A-dependent coupling of mouse prostacyclin receptors to Gi is cell-type dependent. Eur J Pharmacol. 2003 Aug 1;474(1):7-13.

    [4]. T Murata, et al. Altered pain perception and inflammatory response in mice lacking prostacyclin receptor. Nature. 1997 Aug 14;388(6643):678-82.

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GRP78-IN-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。

GRP78-IN-1 

GRP78-IN-1 与 GRP78 残基具有多种相互作用,结合能为 -8.07 kcal/mol。GRP78-IN-1 在癌细胞中显示出有效的细胞毒性、抗增殖作用。GRP78-IN-1 在乳腺癌细胞中表现出有前景的凋亡和伤口愈合特性。

GRP78-IN-1

GRP78-IN-1 Chemical Structure

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生物活性

GRP78-IN-1 exhibits several interactions with GRP78 residues with binding energy of -8.07 kcal/mol. GRP78-IN-1 shows the potent cytotoxic, anti-proliferative in cancer cells. GRP78-IN-1 exhibits promising apoptosis in breast cancer cells and wound healing properties[1].

IC50 & Target

Grp78

 

体外研究
(In Vitro)

GRP78-IN-1 (compound 3i) (0.01, 0.1, 1, 10, 100 µM; 48 h) shows the most potent cytotoxic effect (IC50s of 2.06, 12.57, 9, 18, 4.9, 2.19, 62.48 µM in MCF-1, PANC-1, HCT-116, PC-3, A549, MDA-MB-231 and FR-2 cells, respectively)[1].
GRP78-IN-1 (1, 2, 4, 6 µM) shows a steady increase in the expression of pro-apoptotic proteins viz. Par-4, apoptotic cascade in BAX and cleaved caspase 9 cells[1].
GRP78-IN-1 (1, 2, 4, 6 µM; 48 h) inhibits the motility of MCF-7 and A549 cells in a dose-dependent manner[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: MCF-1, MDA-MB-231, PANC-1, HCT-116, PC-3, A549, FR-2cells
Concentration: 0.01, 0.1, 1, 10, 100 µM
Incubation Time: 48 h
Result: Showed the most promising cytotoxic effect (IC50s is 2.06, 12.57, 9, 18, 4.9, 2.19, 62.48 µM in MCF-1, PANC-1, HCT-116, PC-3, A549, MDA-MB-231 and FR-2 cells, respectively).

Western Blot Analysis[1]

Cell Line: BCL-2, BAX, cleaved caspase 9, MCF-7, A549 cells
Concentration: 1, 2, 4, 6 µM
Incubation Time:
Result: Showed a steady increase in the expression of pro-apoptotic proteins viz. Par-4, apoptotic cascade in BAX and cleaved caspase 9 cells.

分子量

342.40

Formula

C21H23FO3

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]. Rasool JU, et al. Palladium catalyzed migratory heck coupling of arteannuin B and boronic acids: An approach towards the synthesis of antiproliferative agents in breast and lung cancer cells. Bioorg Chem. 2022, 122:105694.

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MIF-IN-4 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。

MIF-IN-4 hydrochloride 

MIF-IN-4 hydrochloride 是有效的巨噬细胞移动抑制因子 (MIF) 抑制剂(pIC50=5.01-6)。MIF 是一种细胞因子,最初被发现在抑制巨噬细胞迁移中发挥作用。

MIF-IN-4 hydrochloride

MIF-IN-4 hydrochloride Chemical Structure

CAS No. : 2489514-05-6

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生物活性

MIF-IN-4 hydrochloride is potent macrophage migration inhibitory factor (MIF) inhibitor (pIC50=5.01-6). MIF is a cytokine originally found to play a role in inhibiting macrophage migration[1].

分子量

493.00

Formula

C26H29ClN6O2

CAS 号

2489514-05-6

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]. Kin Chiu Fong, et al. Compounds as inhibitors of macrophage migration inhibitory factor. WO2020186220A1.

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Corydamine(Synonyms: 刻叶紫堇胺)

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。

Corydamine (Synonyms: 刻叶紫堇胺)

Corydamine 是一种 3-芳基异喹啉生物碱, 一种有效的 DNA 拓扑异构酶 I/II (DNA topoisomerase I/II) 抑制剂。Corydamine 具有抗癌活性。

Corydamine(Synonyms: 刻叶紫堇胺)

Corydamine Chemical Structure

CAS No. : 49870-84-0

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生物活性

Corydamine, 3-arylisoquinoline alkaloid, is a potent DNA topoisomerase I/II inhibitor. Corydamine has anti-cancer activity[1].

IC50 & Target[1]

Topoisomerase I

 

Topoisomerase II

 

分子量

350.37

Formula

C20H18N2O4

CAS 号

49870-84-0

中文名称

刻叶紫堇胺

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]. Xuemei Deng, et al. Design, synthesis and anti-hepatocellular carcinoma activity of 3-arylisoquinoline alkaloids. Eur J Med Chem. 2022 Jan 15;228:113985.

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Dezapelisib(Synonyms: INCB040093)

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。

Dezapelisib (Synonyms: INCB040093)

Dezapelisib (NCB040093) 是一种有效的磷脂酰肌醇 3-激酶 δ (PI3Kδ) 抑制剂。Dezapelisib 是一种很有前景的研究策略,可用于治疗特定的 R/R B 细胞淋巴瘤。

Dezapelisib(Synonyms: INCB040093)

Dezapelisib Chemical Structure

CAS No. : 1262440-25-4

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生物活性

Dezapelisib (NCB040093) is a potent inhibitor of phosphatidylinositol 3-kinase δ (PI3Kδ). Dezapelisib is a promising research strategy for select R/R B-cell lymphomas[1].

分子量

421.45

Formula

C20H16FN7OS

CAS 号

1262440-25-4

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]. Phillips TJ, et al. Phase 1 study of the PI3Kδ inhibitor INCB040093 ± JAK1 inhibitor itacitinib in relapsed/refractory B-cell lymphoma. Blood. 2018;132(3):293-306.

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Tubulin polymerization-IN-7

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。

Tubulin polymerization-IN-7 

Tubulin aggregation-IN-7 (compound 5) 是一种有效的tubulin 聚合抑制剂。Tubulin aggregation-IN-7 具有研究癌症疾病的潜力。

Tubulin polymerization-IN-7

Tubulin polymerization-IN-7 Chemical Structure

CAS No. : 1394017-46-9

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生物活性

Tubulin polymerization-IN-7 (compound 5) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-7 has the potential for the research of cancer diseases[1].

分子量

544.58

Formula

C28H24N4O6S

CAS 号

1394017-46-9

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]. Chen L, et al. Concise synthesis and preliminary biological evaluation of new triazolylthioacetone derivatives bearing pyridine, pyrazine, and 3,4,5-trimethoxybenzyl fragment. Bioorg Med Chem Lett. 2022;66:128721.

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HDAC-IN-30

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。

HDAC-IN-30 

HDAC-IN-30 是一种新颖的多靶点 HDAC 抑制剂,靶点主要有 HDAC1 (IC50=13.4 nM),HDAC2 (IC50=28.0 nM), HDAC3 (IC50=9.18 nM),HDAC6 (IC50=42.7 nM),HDAC8 (IC50=131 nM)。HDAC-IN-30 表现出非常强大的抗肿瘤作用。

HDAC-IN-30

HDAC-IN-30 Chemical Structure

CAS No. : 2756809-34-2

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生物活性

HDAC-IN-30 is a novel multi-target HDAC inhibitor, including HDAC1 (IC50=13.4 nM),HDAC2 (IC50=28.0 nM), HDAC3 (IC50=9.18 nM), HDAC6 (IC50=42.7 nM), HDAC8 (IC50=131 nM). HDAC-IN-30 exhibits potent antitumor efficacy[1].

IC50 & Target

HDAC1

13.4 nM (IC50)

HDAC2

28.0 nM (IC50)

HDAC3

9.18 nM (IC50)

HDAC6

42.7 nM (IC50)

HDAC8

131 nM (IC50)

体外研究
(In Vitro)

HDAC-IN-30 (compound 8 h; 0.5, 1, 2 μM; 48 hours) can effectively activate the p53 pathway by promoting the phosphorylation of p53[1]. HDAC-IN-30 (0, 1, 2.5, 5 mM; 48 hours; HepG2 cells) induces cell cycle arrest at the G2 phase in a concentration-dependent manner[1]. HDAC-IN-30 (0, 1, 2.5, 5 mM; 48 hours) possesses prominent anticancer activity in HepG2 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.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 24 hours
Result: Could effectively activate the p53 pathway by promoting the phosphorylation of p53

Cell Cycle Analysis[1]

Cell Line: HepG2 cells
Concentration: 0, 1, 2.5, 5 μM
Incubation Time: 48 hours
Result: Cells were arrested at the G2 phase in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: HepG2 cells
Concentration: 0, 1, 2.5, 5 μM
Incubation Time: 24 hours
Result: Possessed prominent anticancer activity in HepG2 cells.

体内研究
(In Vivo)

HDAC-IN-30 (12, 24 mg/kg; intraperitoneal injection, every two days for 4 weeks) exhibits potent anticancer activity and no side effects even at high dose (24 mg/kg)[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: HepG2 xenograft mouse model[1]
Dosage: 12, 24 mg/kg
Administration: Intraperitoneal injection, every 2 days, 4 weeks
Result: Exhibited potent anticancer activity

分子量

405.45

Formula

C22H23N5O3

CAS 号

2756809-34-2

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]. Liu Q, et al. Discovery of phthalazino [1, 2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. Eur J Med Chem. 2022, 229:114058.

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(Z)-SU5614

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。

(Z)-SU5614 

(Z)-SU5614 是一种有效的 FLT3 抑制剂,在表达组成性激活的 FLT3 的 Ba/F3 和 AML 细胞系中选择性诱导生长停滞、凋亡和细胞周期停滞。

(Z)-SU5614

(Z)-SU5614 Chemical Structure

CAS No. : 1055412-47-9

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10 mg ¥900 询问价格 & 货期
25 mg ¥1900 询问价格 & 货期
50 mg ¥3300 询问价格 & 货期
100 mg ¥5900 询问价格 & 货期

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生物活性

(Z)-SU5614 is a potent FLT3 inhibitor and selectively induces growth arrest, apoptosis, and cell cycle arrest in Ba/F3 and AML cell lines expressing a constitutively activated FLT3[1].

分子量

272.73

Formula

C15H13ClN2O

CAS 号

1055412-47-9

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]. Spiekermann K, et al. The protein tyrosine kinase inhibitor SU5614 inhibits FLT3 and induces growth arrest and apoptosis in AML-derived cell lines expressing a constitutively activated FLT3. Blood. 2003 Feb 15;101(4):1494-504.

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CDK1-IN-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。

CDK1-IN-1 

CDK1-IN-7是一种有效的 CDK1 抑制剂 (CDK1/CycB IC50=161.2 nM),具有潜在的抗增殖活性以及对肿瘤组织有选择性。CDK1-IN-7 通过凋亡内在途径以 p53 依赖的方式诱导细胞凋亡 (Apoptosis)。CDK1-IN-7 是一种潜在的靶向抗肿瘤药物。

CDK1-IN-1

CDK1-IN-1 Chemical Structure

CAS No. : 2761858-59-5

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生物活性

CDK1-IN-7 is a potent CDK1 inhibitor (CDK1/CycB IC50=161.2 nM) with potential antiproliferative activity and selectivity for cancer tissues. CDK1-IN-7 induces apoptosis in p53 dependent manner through the intrinsic apoptotic pathway. CDK1-IN-7 is a potential targeted antitumor agent[1].

IC50 & Target

CDK1/cycB

161.2 nM (IC50)

体外研究
(In Vitro)

CDK1-IN-7 (compound 7a) (10 µM, 48 hours) has the high antiproliferative activity with a mean percentage of growth inhibition of 48.5 % over NCI cancer cell lines, and caused more than 40% growth inhibition in 36 cancer cell lines from different cancer subtypes[1].
CDK1-IN-7 (0.1-100 μM, 48 hours) has better selectivity for cancer cells over normal cell lines (IC50 of 17.7 and 6.28 μM in WI-38 and HCT-116 cells, respectively; SI=2.8)[1].
CDK1-IN-7 (17.7 μM in WI-38 and 6.28 μM in HCT-116; 48 hours) has a superior activity on cancerous cells than normal cells in inducing apoptosis and arresting the cell cycle at the G2/M phase[1].
CDK1-IN-7 (17.7 μM in WI-38 and 6.28 μM in HCT-116; 48 hours) can cause cell death mainly through apoptosis rather than necrosis and confirmed that its activity is more selective to cancerous cells than normal cells[1].
CDK1-IN-7 (6.28 μM; 48 hours) induce apoptosis in p53 dependent manner through the intrinsic apoptotic pathway in HCT-116 cells[1].

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

Cell Proliferation Assay

Cell Line: 60 human cancer cell lines (LOX IMVI, IGROV1, A498, COLO205 et al.)[1]
Concentration: 10 µM
Incubation Time: 48 hours
Result: Had the high antiproliferative activity with a mean percentage of growth inhibition of 48.5 % over NCI cancer cell lines, and caused more than 40% growth inhibition in 36 cancer cell lines from different cancer subtypes.

Cell Cytotoxicity Assay

Cell Line: HCT-116 and WI-38 cells[1]
Concentration: 0.1-100 μM
Incubation Time: 48 hours
Result: Had better selectivity for cancer cells over normal cell lines (IC50 of 17.7 and 6.28 μM in WI-38 and HCT-116 cells, respectively; SI=2.8).

Cell Cycle Analysis

Cell Line: HCT-116 and WI-38 cells[1]
Concentration: 17.7 μM in WI-38 and 6.28 μM in HCT-116
Incubation Time: 48 hours
Result: Exerted a superior activity on cancerous cells than normal cells in inducing apoptosis and arresting the cell cycle at the G2/M phase.

分子量

465.50

Formula

C27H23N5O3

CAS 号

2761858-59-5

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]. Elgiushy HR, et al. Identification of a promising hit from a new series of pyrazolo[1,5-a]pyrimidine based compounds as a potential anticancer agent with potent CDK1 inhibitory and pro-apoptotic properties through a multistep in vitro assessment [published online ahead of print, 2022 Jan 29]. Bioorg Chem. 2022;120:105646.

    [2]. Gangadevi S, et al. Kobophenol A Inhibits Binding of Host ACE2 Receptor with Spike RBD Domain of SARS-CoV-2, a Lead Compound for Blocking COVID-19. J Phys Chem Lett. 2021;12(7):1793-1802.

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EGFR-IN-36

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。

EGFR-IN-36 

EGFR-IN-36 是一种有效的 EGFR 抑制剂,对 EGFR (WT)、HER2 (WT)、HER2 (A775_G776insYVMA) 的 IC50 分别为 19.09 nM、120.01 nM、2.35 nM。EGFR-IN-36 具有用于野生和/或突变EGFR和/或HER2激酶介导的肿瘤研究的潜力。

EGFR-IN-36

EGFR-IN-36 Chemical Structure

CAS No. : 2711105-54-1

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生物活性

EGFR-IN-36 is a potent EGFR inhibitor with IC50s of 19.09 nM, 120.01 nM, 2.35 nM for EGFR (WT), HER2 (WT), HER2 (A775_G776insYVMA), respectively. EGFR-IN-36 has potential for wild and/or mutant EGFR and/or HER2 kinase mediated tumors research[1].

IC50 & Target[1]

EGFR (WT)

19.09 nM (IC50)

HER2(WT)

120.01 nM (IC50)

HER2 (A775_G776insYVMA)

2.35 nM (IC50)

体外研究
(In Vitro)

EGFR-IN-36 (compound 8) inhibits A431 cell (IC50=223.6 nM),A549 cell (IC50=7644.42 nM), H1975 cell (IC50=20.68 nM)[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

488.97

Formula

C26H25ClN6O2

CAS 号

2711105-54-1

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]. Yihan Wang, et al. Substituted acrylamide derivatives and their compositions and uses. WO2021185348A1.

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Gluconapin potassium

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。

Gluconapin potassium 

Gluconapin potassium 是萝卜硫素的前体。萝卜硫素是一种有效的抗癌异硫氰酸酯。

Gluconapin potassium

Gluconapin potassium Chemical Structure

CAS No. : 245550-57-6

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生物活性

Gluconapin potassium is the precursor of sulforaphane. Sulforaphane is a potent anti-cancer isothiocyanate[1].

分子量

411.49

Formula

C11H18KNO9S2

CAS 号

245550-57-6

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]. Padilla G, et al. Variation of glucosinolates in vegetable crops of Brassica rapa. Phytochemistry. 2007;68(4):536-545.

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