TrxR-IN-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。

TrxR-IN-3 

TrxR-IN-3 (Compound 2c) 是一种有效的 TrxR 抑制剂。TrxR-IN-3 对五种人类癌细胞系表现出有效的抗增殖活性,尤其是对乳腺肿瘤细胞。TrxR-IN-3 通过调节乳腺癌细胞中表达的凋亡相关蛋白增加 ROS 水平并导致显着的细胞凋亡。TrxR-IN-3 还通过促进 LC3-II 和 Beclin-1 的表达,降低 LC3-I 和 p62 蛋白的表达,触发自噬体和自溶酶体的形成。

TrxR-IN-3

TrxR-IN-3 Chemical Structure

CAS No. : 2445565-58-0

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生物活性

TrxR-IN-3 (Compound 2c) is a potent inhibitor of TrxR. TrxR-IN-3 exhibits potent antiproliferative activities against five human cancer cell lines, especially against breast tumor cells. TrxR-IN-3 increases ROS levels and resulted in marked apoptosis by regulating apoptosis-related proteins expressed in the breast cancer cells. TrxR-IN-3 also triggers the formation of autophagosomes and autolysosomes by promoting the expression of LC3-II and Beclin-1 and diminishing the expression of LC3-I and p62 proteins[1].

分子量

268.23

Formula

C14H11F3O2

CAS 号

2445565-58-0

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]. Qian J, et al. Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy. Eur J Med Chem. 2020 Oct 15;204:112610.

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Trk-IN-8

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-8 

Trk-IN-8 是一种有效的 TRKA 抑制剂,对 TRKAa、TRKA(G595R) 和 TRKC(G623R) 的 IC50 分别为 0.42、0.89 和 1.5 nM (WO2021115401A1, compound 3)。

Trk-IN-8

Trk-IN-8 Chemical Structure

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生物活性

Trk-IN-8 is a potent TRK inhibitor with IC50s of 0.42, 0.89 and 1.5 nM for TRKAa, TRKA(G595R) and TRKC(G623R), respectively (WO2021115401A1, compound 3)[1].

分子量

386.36

Formula

C18H16F2N6O2

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]. Fluorine-containing heterocyclic derivatives with macrocyclic structure and use thereof. WO2021115401A1.

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PI3K-IN-26

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。

PI3K-IN-26 

PI3K-IN-26 是一种有效的 PI3K 抑制剂,对 SU-DHL-6 细胞的 IC50 为 36 nM (WO2016066142A1, compound 1)。

PI3K-IN-26

PI3K-IN-26 Chemical Structure

CAS No. : 1918151-65-1

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生物活性

PI3K-IN-26 is a potent PI3K inhibitor with an IC50 of 36 nM for SU-DHL-6 cells (WO2016066142A1, compound 1)[1].

分子量

402.47

Formula

C21H18N6OS

CAS 号

1918151-65-1

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]. Certain protein kinase inhibitors. WO2016066142A1.

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P-gp inhibitor 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。

P-gp inhibitor 4 

P-gp inhibitor 4 (Compound 8b) 是一种选择性的 P-glycoprotein 调节剂,EC50 值为 94 nM。P-gp inhibitor 4 增加药物通过胃肠道屏障的能力,恢复 doxorubicin 在耐药癌细胞中的毒性。

P-gp inhibitor 4

P-gp inhibitor 4 Chemical Structure

CAS No. : 2652001-05-1

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生物活性

P-gp inhibitor 4 (Compound 8b) is a selective P-glycoprotein modulator with an EC50 of 94 nM. P-gp inhibitor 4 increases drug transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells[1].

IC50 & Target

EC50: 94 nM (P-glycoprotein)[1]

体外研究
(In Vitro)

P-gp inhibitor 4 (Compound 8b) (0-1 μM, 48 h) significantly increases the cytotoxic effect of antineoplastic drug with co-administration[1].
P-gp inhibitor 4 does not alter the physiological properties of Caco-2 cells barrier model[1].
P-gp inhibitor 4 selectively reduces the activity of P-gp and increases the transport of multiple P-gp substrates across gastro-intestinal barrier[1].

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

Cell Proliferation Assay[1]

Cell Line: MDCK-MDR1
Concentration: 100 nM, 500 nM and 1 μM
Incubation Time: 48 h
Result: Showed no cytotoxicity. Significantly increased the cytotoxic effect of antineoplastic drug.

Cell Viability Assay[1]

Cell Line: Caco-2 cells
Concentration: 0.1 nM-100 µM
Incubation Time: 72 h
Result: Displayed a dose-dependence cytotoxicity that was significant at ≥ 10 μM concentration. Did not reduce cell viability at 100 nM.

分子量

714.85

Formula

C38H38N2O8S2

CAS 号

2652001-05-1

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]. Contino M, et al. One molecule two goals: A selective P-glycoprotein modulator increases drug transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells. Eur J Med Chem. 2020 Dec 15;208:112843.

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AKT-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。

AKT-IN-10 

AKT-IN-10 是一种有效的 AKT 抑制剂。蛋白激酶 B (PKB,也称为 AKT) 是细胞中 PI3K/AKT/mTOR 信号传导的核心,其功能对细胞生长、存活、分化和代谢很重要。AKT-IN-10 具有研究乳腺癌和前列腺癌的潜力 (摘自专利 WO2021185238A1,化合物 4)。

AKT-IN-10

AKT-IN-10 Chemical Structure

CAS No. : 2709045-56-5

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生物活性

AKT-IN-10 is a potent inhibitor of AKT. Protein kinase B (PKB, also known as AKT) is central to PI3K/AKT/mTOR signaling in cells, and its function is important for cell growth, survival, differentiation and metabolism. AKT-IN-10 has the potential for the research of breast and prostate cancer (extracted from patent WO2021185238A1, compound 4)[1].

IC50 & Target

AKT[1]

分子量

484.03

Formula

C26H34ClN5O2

CAS 号

2709045-56-5

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]. Xin Li, et al. Thickened dicyclic derivatives, their preparation methods and their application in medicine. Patent WO2021185238A1.

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KRAS G12D inhibitor 3 TFA

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。

KRAS G12D inhibitor 3 TFA 

KRAS G12D inhibitor 3 TFA 是一种 KRAS G12D 抑制剂,其 IC50 小于500 nM,具有抗肿瘤作用 (WO2022002102A1; compound 146)。

KRAS G12D inhibitor 3 TFA

KRAS G12D inhibitor 3 TFA Chemical Structure

CAS No. : 2757095-12-6

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生物活性

KRAS G12D inhibitor 3 TFA is a KRAS G12D inhibitor with an IC50 of <500 nm. kras g12d inhibitor 3 tfa has antitumor effects (wo2022002102a1; compound 146)[1].

IC50 & Target[1]

KRas G12D

<500 nM (IC50)

分子量

748.11

Formula

C36H32ClF6N5O4

CAS 号
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

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RMS3

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。

RMS3 

RMS3 是一种汉防己碱类似物,是一种有效的 P-糖蛋白 (P-gp) 抑制剂。RMS3 对癌细胞具有显着的抗增殖和细胞毒作用。RMS3 导致 PARP 裂解,这是细胞凋亡的标志物。RMS3 具有强抗癌特性。

RMS3

RMS3 Chemical Structure

CAS No. : 2497686-66-3

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生物活性

RMS3, a tetrandrine analogue, is a potent P-glycoprotein (P-gp) inhibitor. RMS3 has markedly antiproliferative and cytotoxic effects on cancer cells. RMS3 causes PARP cleavage, a marker for cells undergoing apoptosis. RMS3 has strong anticancer property[1].

分子量

676.72

Formula

C38H39F3N2O6

CAS 号

2497686-66-3

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]. RamonaSchütz, et al. Synthesis, biological evaluation and toxicity of novel tetrandrine analogues. Eur J Med Chem. 2020 Dec 1;207:112810.

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Cereblon inhibitor 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。

Cereblon inhibitor 1 

Cereblon inhibitor 1 是一种异吲哚啉衍生物,一种 cereblon E3 泛素连接酶调节药物。 Cereblon inhibitor 1 具有用于癌症研究的潜力。

Cereblon inhibitor 1

Cereblon inhibitor 1 Chemical Structure

CAS No. : 2672489-14-2

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生物活性

Cereblon inhibitor 1, an isoindoline derivative, is a cereblon E3 ubiquitin ligase modulating drug. Cereblon inhibitor 1 has the potential for cancer research[1].

IC50 & Target[1]

Cereblon

 

体外研究
(In Vitro)

Cereblon inhibitor 1 (compound CM-48) suppresses MM.1S cell proliferation (IC50=0.0365 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

620.05

Formula

C32H28ClF2N5O4

CAS 号

2672489-14-2

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]. Hui Liu, et al. Isoindoline derivative and its application. WO2021147889A1.

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DX2-201

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。

DX2-201 

DX2-201 是一种有效的选择性氧化磷酸化 (OXPHOS) 复合物 I 抑制剂,IC50 为 312 nM。DX2-201 具有抗癌作用。

DX2-201

DX2-201 Chemical Structure

CAS No. : 2749554-00-3

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生物活性

DX2-201 is a potent and selective oxidative phosphorylation (OXPHOS) complex I inhibitor with an IC50 of 312 nM. DX2-201 has anticancer effects[1].

IC50 & Target

IC50: 312 nM (OXPHOS complex I)[1]

体外研究
(In Vitro)

DX2-201 (cmpound 2) potently inhibits the mitochondrial function by depleting ATP production in MIA PaCa-2 cells when glucose is replaced by galactose in the medium, a condition that forces mammalian cells to rely on OXPHOS[1].
DX2-201 depletes ATP production with an IC50 value of 118.5 nM in the galactose-containing medium[1].
DX2-201 significantly inhibits OXPHOS complex I as determined by its inhibition of oxidation of NADH to NAD+ in the NAD/NADH assay (IC50 = 312 nM)[1].
DX2-201 inhibits MIA PaCa-2 and BxPC-3 cells growth with IC50 values of 0.4 μM and 0.6 μM, respectively[1].

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

分子量

432.55

Formula

C18H28N2O6S2

CAS 号

2749554-00-3

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]. Ding Xue, et al. Discovery and Lead Optimization of Benzene-1,4-disulfonamides as Oxidative Phosphorylation Inhibitors.J Med Chem. 2022 Jan 13;65(1):343-368. https://pubmed.ncbi.nlm.nih.gov/34982568/

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VEGFR-2/BRAF-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。

VEGFR-2/BRAF-IN-2 

VEGFR-2/BRAF-IN-2 (Compound 4a) 是一种 VEGFR-2BRAF 双重抑制剂,对 VEGFR-2、BRAFV600EBRAFWTIC50 分别为 0.111、0.089 和 0.071 µM。VEGFR-2/BRAF-IN-2 诱导细胞凋亡,在 G1 期阻滞细胞周期。

VEGFR-2/BRAF-IN-2

VEGFR-2/BRAF-IN-2 Chemical Structure

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生物活性

VEGFR-2/BRAF-IN-2 (Compound 4a) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.111, 0.089 and 0.071 µM against VEGFR-2, BRAFV600E and BRAFWT, respectively. VEGFR-2/BRAF-IN-2 induces apoptosis and arrests the cell cycle mainly in the G1 phase[1].

IC50 & Target

VEGFR2

0.111 μM (IC50)

BRafV600E

0.089 μM (IC50)

BRAFWT

0.071 μM (IC50)

分子量

608.05

Formula

C26H21ClF3N5O3S2

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]. Hassan RA, et al. Novel antiproliferative agents bearing substituted thieno[2,3-d]pyrimidine scaffold as dual VEGFR-2 and BRAF kinases inhibitors and apoptosis inducers; design, synthesis and molecular docking. Bioorg Chem. 2022 May 10;125:105861.

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Malformin A1

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。

Malformin A1 

Malformin A1 是一种从Aspergillus niger 中分离出来的环状五肽,具有抗菌活性。Malformin A1 对人结直肠癌细胞显示出有效的细胞毒活性。Malformin A1 通过激活 PARP、caspase 3、-7 和 -9 诱导细胞凋亡。

Malformin A1

Malformin A1 Chemical Structure

CAS No. : 3022-92-2

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生物活性

Malformin A1, a cyclic pentapeptide isolated from Aspergillus niger, possess a range of bioactive properties including antibacterial activity. Malformin A1 shows potent cytotoxic activities on human colorectal cancer cells. Malformin A1 induces apoptosis by activating PARP, caspase 3, -7, and -9[1].

分子量

529.72

Formula

C23H39N5O5S2

CAS 号

3022-92-2

Sequence Shortening

CCVLI (Disulfide bridge:Cys1-Cys2)

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]. Sun-Young Park, et al. Malformin A1 treatment alters invasive and oncogenic phenotypes of human colorectal cancer cells through stimulation of the p38 signaling pathway. Int J Oncol. 2017 Sep;51(3):959-966.

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SOS1-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。

SOS1-IN-10 

SOS1-IN-10 是一种有效的 SOS1 抑制剂,对 KRAS G12C-SOS1 的IC50 为 13 nM。

SOS1-IN-10

SOS1-IN-10 Chemical Structure

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生物活性

SOS1-IN-10 is a potent SOS1 inhibitor with an IC50 of 13 nM for KRAS G12C-SOS1 (WO2022017519A1, compound 8)[1].

IC50 & Target[1]

KRAS G12C-SOS1

13 nM (IC50)

分子量

450.40

Formula

C22H19F5N4O

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]. Quinazoline compound. WO2022017519A1.

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GRK6-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。

GRK6-IN-1 

GRK6-IN-1 (compound 18) 是 G 蛋白偶联受体激酶 6 (GRK6) 的有效抑制剂,IC50 为 120 nM。GRK6 是多发性骨髓瘤 (MM) 细胞存活所需的关键激酶。GRK6-IN-1 具有研究多发性骨髓瘤的潜力。

GRK6-IN-1

GRK6-IN-1 Chemical Structure

CAS No. : 2677786-61-5

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生物活性

GRK6-IN-1 (compound 18) is a potent inhibitor of G protein-coupled receptor kinase 6 (GRK6) with an IC50 of 120 nM. GRK6 is a critical kinase required for the survival of multiple myeloma (MM) cells. GRK6-IN-1 has the potential for the research of multiple myeloma[1].

分子量

438.91

Formula

C22H23ClN6O2

CAS 号

2677786-61-5

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]. Uehling DE, et al. Design, Synthesis, and Characterization of 4-Aminoquinazolines as Potent Inhibitors of the G Protein-Coupled Receptor Kinase 6 (GRK6) for the Treatment of Multiple Myeloma [published correction appears in J Med Chem. 2022 Jan 13;65(1):886-887]. J Med Chem. 2021;64(15):11129-11147.

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ARUK3001185

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。

ARUK3001185 

ARUK3001185 (Compound 8l) 是一种有效的、选择性的、具有口服活性的、能通过大脑屏障的 Notum 抑制剂,IC50 值为 6.7 nM。

ARUK3001185

ARUK3001185 Chemical Structure

CAS No. : 2411969-39-4

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生物活性

ARUK3001185 (Compound 8l) is a potent, selective, orally active and brain-penetrant inhibitor of Notum activity with an IC50 of 6.7 nM[1].

IC50 & Target

IC50: 6.7 nM (Notum)[1]

分子量

282.05

Formula

C9H4Cl2F3N3

CAS 号

2411969-39-4

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]. Willis NJ, et al. Design of a Potent, Selective, and Brain-Penetrant Inhibitor of Wnt-Deactivating Enzyme Notum by Optimization of a Crystallographic Fragment Hit. J Med Chem. 2022 May 26;65(10):7212-7230.

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Immune initiator-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。

Immune initiator-1 

Immune initiator-1 (Compound 1a) 是一种氨基酸修饰的近红外 Aza-BODIPY 光敏剂,可作为免疫诱导剂用于有效光动力治疗黑色素瘤。

Immune initiator-1

Immune initiator-1 Chemical Structure

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生物活性

Immune initiator-1 (Compound 1a) is an amino acid-modified near-infrared Aza-BODIPY photosensitizer, acts as an immune initiator for potent photodynamic therapy in melanoma[1].

分子量

868.43

Formula

C41H32BF2IN4O7

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]. Zhiliang Yu, et al. Discovery of an Amino Acid-Modified Near-Infrared Aza-BODIPY Photosensitizer as an Immune Initiator for Potent Photodynamic Therapy in Melanoma. J Med Chem. 2022 Feb 24;65(4):3616-3631.

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SOS1-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。

SOS1-IN-9 

SOS1-IN-9 是一种有效的 SOS1 抑制剂,对 KRAS G12C-SOS1 的IC50 为 116.5 nM。

SOS1-IN-9

SOS1-IN-9 Chemical Structure

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生物活性

SOS1-IN-9 is a potent SOS1 inhibitor with an IC50 of 116.5 nM for SOS1-KRAS G12C (WO2022028506A1, compound 302)[1].

IC50 & Target[1]

KRAS G12C-SOS1

116.5 nM (IC50)

分子量

435.49

Formula

C22H28F3N5O

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]. Sos1 inhibitor, pharmaceutical composition containing same, and use therefor. WO2022028506A1.

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Pyruvate Carboxylase-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。

Pyruvate Carboxylase-IN-1 

Pyruvate Carboxylase-IN-1 (compound 37) 是一种有效的丙酮酸羧化酶(pyruvate carboxylase) 抑制剂,在基于细胞裂解物和基于细胞的 PC 活性中,IC50s 分别为 0.204 和 0.104 μM。Pyruvate Carboxylase-IN-1 是毛兰素的天然类似物。Pyruvate Carboxylase-IN-1 抑制 PC 的酶活性,介导人肝细胞癌 (HCC) 的抗癌作用。

Pyruvate Carboxylase-IN-1

Pyruvate Carboxylase-IN-1 Chemical Structure

CAS No. : 70205-50-4

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生物活性

Pyruvate Carboxylase-IN-1 (compound 37) is a potent inhibitor of pyruvate carboxylase (PC) with IC50s of 0.204 and 0.104 μM in cell lysate-based and cell-based PC activity, respectively. Pyruvate Carboxylase-IN-1 is a natural analog of erianin. Pyruvate Carboxylase-IN-1 inhibites the enzymatic activity of PC, mediating the anticancer effect in human hepatocellular carcinoma (HCC)[1].

分子量

242.27

Formula

C15H14O3

CAS 号

70205-50-4

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]. Sheng Y, et al. Identification of Pyruvate Carboxylase as the Cellular Target of Natural Bibenzyls with Potent Anticancer Activity against Hepatocellular Carcinoma via Metabolic Reprogramming. J Med Chem. 2022;65(1):460-484.

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BDP-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。

BDP-4 

BDP-4 是一种氨基酸修饰的近红外 Aza-BODIPY 光敏剂,可作为免疫诱导剂用于有效光动力治疗黑色素瘤。

BDP-4

BDP-4 Chemical Structure

CAS No. : 2566625-99-6

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生物活性

BDP-4 is an amino acid-modified near-infrared Aza-BODIPY photosensitizer, acts as an immune initiator for potent photodynamic therapy in melanoma[1].

分子量

683.29

Formula

C34H25BF2IN3O2

CAS 号

2566625-99-6

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]. Zhiliang Yu, et al. Discovery of an Amino Acid-Modified Near-Infrared Aza-BODIPY Photosensitizer as an Immune Initiator for Potent Photodynamic Therapy in Melanoma. J Med Chem. 2022 Feb 24;65(4):3616-3631.

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RMS5

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。

RMS5 

RMS5 是一种汉防己碱类似物,是一种有效的 P-糖蛋白 (P-gp) 抑制剂。RMS5 对癌细胞具有显着的抗增殖和细胞毒作用。RMS5 略微降低抗凋亡 Bcl-2 家族蛋白 Bcl-XL 和 Mcl-1 的表达。RMS3 导致 PARP 裂解,这是细胞凋亡的标志物。RMS5 具有强抗癌特性。

RMS5

RMS5 Chemical Structure

CAS No. : 2497686-68-5

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生物活性

RMS5, a tetrandrine analogue, is a potent P-glycoprotein (P-gp) inhibitor. RMS5 has markedly antiproliferative and cytotoxic effects on cancer cells. RMS5 slightly diminishes the expression of the anti-apoptotic Bcl-2 family proteins Bcl-XL and Mcl-1. RMS3 causes PARP cleavage, a marker for cells undergoing apoptosis. RMS5 has strong anticancer property[1].

分子量

598.75

Formula

C35H38N2O5S

CAS 号

2497686-68-5

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]. RamonaSchütz, et al. Synthesis, biological evaluation and toxicity of novel tetrandrine analogues. Eur J Med Chem. 2020 Dec 1;207:112810.

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RET-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。

RET-IN-9 

RET-IN-9 是一种有效的 RET 抑制剂。RET 激酶是一种单通道跨膜受体酪氨酸激酶,在肾脏和肠神经系统的发育以及维持神经、内分泌、造血和男性生殖系统的体内平衡中起重要作用。RET-IN-9 具有研究 RET 相关疾病的潜力,包括非小细胞肺癌和甲状腺髓样癌 (信息提取自专利 WO2021115457A1, 化合物 29)。

RET-IN-9

RET-IN-9 Chemical Structure

CAS No. : 2649418-11-9

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生物活性

RET-IN-9 is a potent inhibitor of RET. RET kinase is a single-pass transmembrane receptor tyrosine kinase that plays an important role in the development of the kidney and enteric nervous system, and the maintenance of homeostasis in the nervous, endocrine, hematopoietic, and male reproductive systems. RET-IN-9 has the potential for the research of RET-related disease including non-small cell lung cancer and medullary thyroid cancer (extracted from patent WO2021115457A1, compound 29)[1].

分子量

481.55

Formula

C26H27N9O

CAS 号

2649418-11-9

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]. Huimin Chen, et al. Pyrazolo[1,5-a]pyridine compounds and preparation method and application thereof. Patent WO2021115457A1.

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