91高清自产国产拍,无码免费A级毛片大全,日本 欧美 国产中文字幕,99re热视频这里只有精品视频首页

INK 128 (MLN0128),mTOR抑制剂

规格或纯度: ≥98%
有货

库存信息

关闭

库存信息

关闭

库存信息

关闭
货号 (SKU) 包装规格 是否现货 价格 数量
I128086-5mg 5mg 现货 Stock Image
I128086-25mg 25mg 现货 Stock Image
I128086-100mg 100mg 现货 Stock Image

基本描述

规格或纯度 ≥98%
英文名称 INK 128 (MLN0128)
别名 INK-128;MLN0128
英文别名 Sapanisertib; MLN0128; 3-(2-amino-5-benzoxazolyl)-1-(1-methylethyl)-1h-pyrazolo(3,4-d)pyrimidin-4-amine;3-(2-aminobenzo[d]oxazol-5-yl)-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine
生化机理 INK 128 exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases [1]. As TORC1/2 inhibitor, INK 128 inhibits both the phosphorylation of S6 and 4EBP1, the downstream substrates of TORC1, and selectively inhibits AKT phosphorylation at Ser473, the downstream substrate of TORC2. Furthermore, INK 128 also shows potent inhibition effects on cell lines resistant to rapamycin and pan-PI3K inhibitors
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 5mg卖完停产,不再备货
产品介绍

INK 128是高活性mTOR抑制剂,IC50为1 nM,比对其它I型PI3K亚型的抑制性高200倍。A potent and selective TORC1/2 inhibitor

INK 128 (MLN0128) is a potent and selective mTOR inhibitor with IC50 of 1 nM in cell-free assays; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin).
A potent and selective TORC1/2 inhibitor

名称和标识符

IUPAC Name 5-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1,3-benzoxazol-2-amine
INCHI InChI=1S/C15H15N7O/c1-7(2)22-14-11(13(16)18-6-19-14)12(21-22)8-3-4-10-9(5-8)20-15(17)23-10/h3-7H,1-2H3,(H2,17,20)(H2,16,18,19)
InChi Key GYLDXIAOMVERTK-UHFFFAOYSA-N
Canonical SMILES CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(C=C3)OC(=N4)N)N
分子式

C15H15N7O

PubChem CID 45375953
分子量 309.33

化学和物理性质

溶解性 DMSO

靶标

Target ID 2109
名称 mechanistic target of rapamycin kinase
缩写名 mTOR
家族 FRAP subfamily
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 2549 1p36.22 MTOR mechanistic target of rapamycin kinase
Mouse 2 2549 4 78.76 cM Mtor mechanistic target of rapamycin kinase
Rat 2 2549 5q36 Mtor mechanistic target of rapamycin kinase
Ensembl Gene ENSG00000198793 (Hs) , ENSMUSG00000028991 (Mm) , ENSRNOG00000009615 (Rn)
Entrez Gene 2475 (Hs) , 56717 (Mm) , 56718 (Rn)
OMIM 601231 (Hs)
UniProtKB P42345 (Hs) , P42346 (Rn) , Q9JLN9 (Mm)
RefSeq Nucleotide NM_004958 (Hs) , NM_019906 (Rn) , NM_020009 (Mm)
RefSeq Protein NP_004949 (Hs) , NP_063971 (Rn) , NP_064393 (Mm)
Protein GI 4826730 (Hs) , 227330586 (Mm) , 9845251 (Rn)
DrugBank Target P42345 (Hs)
CATH/Gene3D 1.10.1070.11 (N/A) , 1.20.120.150 (N/A) , 1.25.10.10 (N/A)
ChEMBL Target CHEMBL1075134 (Rn) , CHEMBL1255165 (Mm) , CHEMBL2842 (Hs)
Target ID 2153
名称 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha
缩写名 PI3Kα
家族 Phosphatidylinositol-4,5-bisphosphate 3-kinase family
别名 Thyroid-Stimulating Hormone Receptor
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 1068 3q26.32 PIK3CA phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha
Mouse 2 1068 3 15.7 cM Pik3ca phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha
Rat 2 1068 2 q25 Pik3ca phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit alpha
Ensembl Gene ENSG00000121879 (Hs) , ENSMUSG00000027665 (Mm) , ENSRNOG00000056371 (Rn)
Entrez Gene 5290 (Hs) , 18706 (Mm) , 170911 (Rn)
OMIM 171834 (Hs)
UniProtKB P42336 (Hs) , P42337 (Mm)
RefSeq Nucleotide NM_006218 (Hs) , NM_008839 (Mm) , NM_133399 (Rn)
RefSeq Protein NP_006209 (Hs) , NP_032865 (Mm) , NP_596890 (Rn)
Orphanet 117820 (Hs)
Protein GI 54792082 (Hs) , 254540080 (Mm) , 282158067 (Rn)
CATH/Gene3D 1.10.1070.11 (N/A) , 2.60.40.150 (N/A)
ChEMBL Target CHEMBL4005 (Hs) , CHEMBL2499 (Mm)
Target ID 2155
名称 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta
缩写名 PI3Kδ
家族 Phosphatidylinositol-4,5-bisphosphate 3-kinase family
别名 Thyroid-Stimulating Hormone Receptor
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 1044 1p36.22 PIK3CD phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta
Mouse 2 1043 4 E2 Pik3cd phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta
Rat 2 944 5q36 Pik3cd phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit delta
Ensembl Gene ENSG00000171608 (Hs) , ENSMUSG00000039936 (Mm) , ENSRNOG00000016846 (Rn)
Entrez Gene 5293 (Hs) , 18707 (Mm) , 366508 (Rn)
OMIM 602839 (Hs)
UniProtKB O00329 (Hs) , O35904 (Mm)
RefSeq Nucleotide NM_001029837 (Mm) , NM_001108978 (Rn) , NM_005026 (Hs)
RefSeq Protein NP_001025008 (Mm) , NP_001102448 (Rn) , NP_005017 (Hs)
Protein GI 156564405 (Hs) , 255708437 (Mm) , 157822959 (Rn)
CATH/Gene3D 1.10.1070.11 (N/A) , 2.60.40.150 (N/A)
ChEMBL Target CHEMBL3130 (Hs) , CHEMBL2216745 (Mm)
Target ID 2156
名称 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma
缩写名 PI3Kγ
家族 Phosphatidylinositol-4,5-bisphosphate 3-kinase family
别名 Thyroid-Stimulating Hormone Receptor
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 1102 7q22.3 PIK3CG phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma
Mouse 2 1102 12 A3 Pik3cg phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma
Rat 2 1102 6 q16 Pik3cg phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit gamma
Ensembl Gene ENSG00000105851 (Hs) , ENSMUSG00000020573 (Mm) , ENSRNOG00000009385 (Rn)
Entrez Gene 5294 (Hs) , 30955 (Mm) , 298947 (Rn)
OMIM 601232 (Hs)
UniProtKB P48736 (Hs) , Q9JHG7 (Mm)
RefSeq Nucleotide NM_001146200 (Mm) , NM_002649 (Hs) , XM_003750140 (Rn)
RefSeq Protein NP_001139672 (Mm) , NP_002640 (Hs) , XP_003750188 (Rn)
Protein GI 21237725 (Hs) , 226246569 (Mm) , 392348758 (Rn)
CATH/Gene3D 1.10.1070.11 (N/A) , 2.60.40.150 (N/A)
ChEMBL Target CHEMBL2189158 (Mm) , CHEMBL3267 (Hs)

关联配体

Ligand ID 7933
名称 sapanisertib
别名 MLN0128
类别 Synthetic organic
学名 5-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1,3-benzoxazol-2-amine
生物活性评价 The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价 Sapanisertib (INK128) is an ATP-competitive inhibitor of mTOR in mTORC1 and mTORC2 complexes, that exhibits potent anti-tumour activity .

The compound also has antimalarial activity. The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY.
配体家族 Antimalarial ligands

参考文献

1. Liu Q, Thoreen C, Wang J, Sabatini D, Gray NS.  (2009)  mTOR Mediated Anti-Cancer Drug Discovery..  Drug Discov Today Ther Strateg,  (2):  (47-55).  [PMID:20622997]
2. Schenone S, Brullo C, Musumeci F, Radi M, Botta M.  (2011)  ATP-competitive inhibitors of mTOR: an update..  Curr Med Chem,  18  (20):  (2995-3014).  [PMID:21651476]
3. Hsieh AC, Liu Y, Edlind MP, Ingolia NT, Janes MR, Sher A, Shi EY, Stumpf CR, Christensen C, Bonham MJ et al..  (2012)  The translational landscape of mTOR signalling steers cancer initiation and metastasis..  Nature,  485  (7396):  (55-61).  [PMID:22367541]
4. Arendse LB, Murithi JM, Qahash T, Pasaje CFA, Godoy LC, Dey S, Gibhard L, Ghidelli-Disse S, Drewes G, Bantscheff M et al..  (2022)  The anticancer human mTOR inhibitor sapanisertib potently inhibits multiple Plasmodium kinases and life cycle stages..  Sci Transl Med,  14  (667):  (eabo7219).  [PMID:36260689]

相关文档

质检报告COA

请输入批号:


产品问答

产品问答

登录提交问题 Hover me 请先登录再提交问题
您提交该产品问题后,我们会在1-2个工作日内给您答复,您可以登录"我的账号",然后点击"我的产品问答"查看答案

91高清自产国产拍,无码免费A级毛片大全,日本 欧美 国产中文字幕,99re热视频这里只有精品视频首页

品牌简介

{转码主词}