Y11

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。

Y11 

Y11 通过阻断 Y397 的磷酸化来抑制 FAK1的自身磷酸化,并抑制肿瘤生长。

Y11

Y11 Chemical Structure

CAS No. : 1086639-59-9

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

* Please select Quantity before adding items.

生物活性

Y11 inhibits FAK1 autophosphorylation by blocking phosphorylation of Y397 and decreases tumor growth[1].

分子量

265.15

Formula

C8H17BrN4O

CAS 号

1086639-59-9

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]. Golubovskaya VM, et al. A small molecule inhibitor, 1,2,4,5-benzenetetraamine tetrahydrochloride, targeting the y397 site of focal adhesion kinase decreases tumor growth. J Med Chem. 2008 Dec 11;51(23):7405-16.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Mycestericin C

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。

Mycestericin C 

Mycestericin C 是从Mycelia sterilia ATCC 20349 的培养液中分离得到的化合物。Mycestericin C 在小鼠同种异体混合淋巴细胞反应中抑制淋巴细胞的增殖。

Mycestericin C

Mycestericin C Chemical Structure

CAS No. : 37817-99-5

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

* Please select Quantity before adding items.

生物活性

Mycestericin C is a compound isolated from the culture broth of Mycelia sterilia ATCC 20349. Mycestericin C suppresses the proliferation of lymphocytes in the mouse allogeneic mixed lymphocyte reaction[1].

分子量

403.55

Formula

C21H41NO6

CAS 号

37817-99-5

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]. Sasaki S, et al. Fungal metabolites. Part 14. Novel potent immunosuppressants, mycestericins, produced by Mycelia sterilia. J Antibiot (Tokyo). 1994;47(4):420-433.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

D942

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。

D942 

D942 是一种可透过细胞的 AMPK 激动剂,部分抑制线粒体复合物 I。在多发性骨髓瘤细胞中,D942 抑制细胞生长。

D942

D942 Chemical Structure

CAS No. : 849727-81-7

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

* Please select Quantity before adding items.

生物活性

D942 is a cell penetrant AMPK activator and partially inhibits the mitochondrial complex I. In multiple myeloma cells, D942 inhibits cell growth[1].

分子量

368.40

Formula

C22H21FO4

CAS 号

849727-81-7

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]. Baumann P, et al. Activation of adenosine monophosphate activated protein kinase inhibits growth of multiple myeloma cells. Exp Cell Res. 2007 Oct 1;313(16):3592-603.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

TD-802

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。

TD-802 

TD-802 (Compound 33c) 是一种雄激素受体 (androgen receptor) PROTAC 降解剂。TD-802 具有良好的体内抗肿瘤效果,能被用于转移性去势抵抗性前列腺癌的研究。

TD-802

TD-802 Chemical Structure

CAS No. : 2760703-21-5

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

* Please select Quantity before adding items.

生物活性

TD-802 (Compound 33c) is an androgen receptor (AR) PROTAC degrader with good microsomal stability. TD-802 has good antitumor efficacy in vivo and can be used for metastatic castration-resistant prostate cancer research[1].

分子量

957.56

Formula

C52H61ClN10O6

CAS 号

2760703-21-5

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]. Takwale AD, et al. Design and characterization of cereblon-mediated androgen receptor proteolysis-targeting chimeras. Eur J Med Chem. 2020 Dec 15;208:112769.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

NSC12

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。

NSC12 

NSC12 是 FGF2 的细胞外陷阱,与 FGF2 结合并干扰其与 FGFR1 的相互作用。NSC12 在体外和体内均能抑制 FGF 依赖性不同肿瘤细胞的增殖,且无全身毒性作用。

NSC12

NSC12 Chemical Structure

CAS No. : 102586-30-1

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

* Please select Quantity before adding items.

生物活性

NSC 12 is an extracellular trap of fibroblast growth factor 2 (FGF2) that binds FGF2 and interferes with its interaction with FGFR1. NSC12 inhibits the proliferation of different FGF-dependent tumour cells both in vitro and in vivo with no systemic toxic effects[1].

分子量

484.52

Formula

C24H34F6O3

CAS 号

102586-30-1

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]. Ronca R, et al. Long-Pentraxin 3 Derivative as a Small-Molecule FGF Trap for Cancer Therapy. Cancer Cell. 2015 Aug 10;28(2):225-39.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

(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

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

* Please select Quantity before adding items.

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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

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

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

* Please select Quantity before adding items.

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].

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: 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]

Shanghai Jinpan Biotech Co Ltd 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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

UK-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。

UK-1 

UK-1 是链霉菌 517-02 的细胞毒性代谢产物,具有广泛的抗肿瘤活性。UK-1 还可抑制HCV复制。

UK-1

UK-1 Chemical Structure

CAS No. : 151271-53-3

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

* Please select Quantity before adding items.

生物活性

UK-1 is a cytotoxic metabolite from Streptomyces sp. 517-02 and exerts a wide spectrum of potent anticancer activities[1]. UK-1 also inhibits HCV replication[2].

分子量

386.36

Formula

C22H14N2O5

CAS 号

151271-53-3

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]. Ueki M, et al. UK-1, a novel cytotoxic metabolite from Streptomyces sp. 517-02. I. Taxonomy, fermentation, isolation, physico-chemical and biological properties. J Antibiot (Tokyo). 1993 Jul;46(7):1089-94.

    [2]. Ward DN, et al. UK-1 and structural analogs are potent inhibitors of hepatitis C virus replication. Bioorg Med Chem Lett. 2014 Jan 15;24(2):609-12.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

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

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

* Please select Quantity before adding items.

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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

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

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

* Please select Quantity before adding items.

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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Y11

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。

Y11 

Y11 通过阻断 Y397 的磷酸化来抑制 FAK1的自身磷酸化,并抑制肿瘤生长。

Y11

Y11 Chemical Structure

CAS No. : 1086639-59-9

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

* Please select Quantity before adding items.

生物活性

Y11 inhibits FAK1 autophosphorylation by blocking phosphorylation of Y397 and decreases tumor growth[1].

分子量

265.15

Formula

C8H17BrN4O

CAS 号

1086639-59-9

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]. Golubovskaya VM, et al. A small molecule inhibitor, 1,2,4,5-benzenetetraamine tetrahydrochloride, targeting the y397 site of focal adhesion kinase decreases tumor growth. J Med Chem. 2008 Dec 11;51(23):7405-16.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

D942

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。

D942 

D942 是一种可透过细胞的 AMPK 激动剂,部分抑制线粒体复合物 I。在多发性骨髓瘤细胞中,D942 抑制细胞生长。

D942

D942 Chemical Structure

CAS No. : 849727-81-7

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

* Please select Quantity before adding items.

生物活性

D942 is a cell penetrant AMPK activator and partially inhibits the mitochondrial complex I. In multiple myeloma cells, D942 inhibits cell growth[1].

分子量

368.40

Formula

C22H21FO4

CAS 号

849727-81-7

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]. Baumann P, et al. Activation of adenosine monophosphate activated protein kinase inhibits growth of multiple myeloma cells. Exp Cell Res. 2007 Oct 1;313(16):3592-603.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

(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

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

* Please select Quantity before adding items.

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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

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

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

* Please select Quantity before adding items.

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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

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

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

* Please select Quantity before adding items.

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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

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

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

* Please select Quantity before adding items.

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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

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

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

* Please select Quantity before adding items.

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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

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

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

* Please select Quantity before adding items.

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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

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

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

* Please select Quantity before adding items.

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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

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

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

* Please select Quantity before adding items.

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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务