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HDACs/mTOR Inhibitor 1

COA COA
    级别和纯度:
  • ≥98%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
H647174-5mg
 5mg 期货 Stock Image
H647174-10mg
 10mg 期货 Stock Image
H647174-50mg
 50mg 期货 Stock Image
H647174-100mg
 100mg 期货 Stock Image
大包装询价 收藏夹 比较  SDS下载  DATASHEET  质量标准
查看相关系列
Apoptosis (7108) Cell Cycle (7376) Cell Cycle/DNA Damage (2603) HDAC (161) Histone Modification (3105) MTOR (146) PI3K/Akt/mTOR (764) 表观遗传学 (1497)
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基本描述

别名 HDAC/mTOR 抑制剂 1
规格或纯度 ≥98%
英文名称 HDACs/mTOR Inhibitor 1
生化机理 HDACs/mTOR 抑制剂 1 是一种 HDACs 和 mTOR 双重抑制剂，对 HDAC1、HDAC6 和 mTOR 的 IC 50 s 分别为 0.19 nM、1.8 nM 和 1.2 nM。HDACs/mTOR 抑制剂 1 能刺激细胞周期停滞在 G0/G1 期，并诱导肿瘤细胞凋亡，毒性较低。
储存温度 -20°C储存
运输条件 超低温冰袋运输
作用类型 抑制剂
产品介绍


HDACs/mTOR Inhibitor 1 is a dual HDACs and mTOR inhibitor, with IC 50 s of 0.19 nM, 1.8 nM, 1.2 nM for HDAC1 , HDAC6 , mTOR , respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induces tumor cell apoptosis with low toxicity in vivo . HDACs/mTOR Inhibitor 1 can be used in the research of hematologic malignancies

In Vitro

HDACs/mTOR Inhibitor 1 (Compound 12l) inhibits leukemia cells proliferation with IC 50 s of 4.05, 9.01, 9.98 μM for MV4-11, OCI-AML2, OCI-AML3 cells. HDACs/mTOR Inhibitor 1 (0-10 μM, 6 h or 24 h) downregulates p-ERK and increases Ac-H3 in MV4-11 cells. HDACs/mTOR Inhibitor 1 (10 to 1000 nM, 48 h) reduces S-phase cells and increases the percentage of cells in G0/G1 phase in MV4-11 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: MV4-11 cells Concentration: 0.01, 0.1, 1, 10 μM Incubation Time: 6 h or 24 h Result: Downregulated p-ERK (24 h) and increased of the Ac-H3 (6 h) in a dose-dependent manner.

In Vivo

HDACs/mTOR Inhibitor 1 (Compound 12l) (10 or 20 mg/kg, i.v.) inhibits tumor growth without significant toxicity in MV4-11 and MM1S xenograft NOD/SCID mouse model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: MV4-11 xenograft NOD/SCID mouse model Dosage: 10 mg/kg Administration: Intravenous injection (i.v.), every two days (Q2D)×6 Result: The TGI (tumor growth inhibitory rate) was 53.1%.

Form:Solid

IC50& Target:HDAC1 0.19 nM (IC 50 ) HDAC6 1.8 nM (IC 50 ) mTOR 1.2 nM (IC 50 )
纯度 ≥98%

关联靶点（人）

HDAC6 Tclin 组蛋白去乙酰化酶6(Histone deacetylase 6) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HDAC1 Tclin 组蛋白去乙酰化酶1(Histone deacetylase 1) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HDAC2 Tclin 组蛋白去乙酰化酶2(Histone deacetylase 2) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HDAC10 Tclin 组蛋白去乙酰化酶10(Histone deacetylase 10) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HDAC8 Tclin 组蛋白去乙酰化酶8(Histone deacetylase 8) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HDAC3 Tclin 组蛋白去乙酰化酶3(Histone deacetylase 3) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
MTOR Tclin 丝氨酸/苏氨酸蛋白激酶 mTOR(Serine/threonine-protein kinase mTOR) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HDAC8 Tclin Histone deacetylase 8 (4516 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HDAC10 Tclin Histone deacetylase 10 (801 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HDAC2 Tclin Histone deacetylase 2 (3971 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HDAC3 Tclin Histone deacetylase 3 (3654 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HDAC4 Tclin Histone deacetylase 4 (2328 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MTOR Tclin Serine/threonine-protein kinase mTOR (13850 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HDAC9 Tclin Histone deacetylase 9 (708 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HDAC11 Tclin Histone deacetylase 11 (967 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HDAC7 Tclin Histone deacetylase 7 (1047 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Raji (5516 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HCT-116 (91556 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MV4-11 (7307 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PIK3R1 Tchem PI3-kinase p110-alpha/p85-alpha (2589 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
FKBP1A Tclin FKBP12A/mTOR (12 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OCI-AML2 (350 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HDAC1 Tclin Histone deacetylase 1/2/3 (160 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MM1.S (1111 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

关联靶点（其它种属）

Hdac1 Histone deacetylase 1 (93 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Hdac5 Histone deacetylase 5 (5 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

分子类型 未知
IIUPAC Name (2R)-N-[4-[1-[7-(hydroxyamino)-7-oxoheptyl]-4-morpholin-4-ylpyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-2-methylmorpholine-4-carboxamide
INCHI 1S/C28H38N8O5/c1-20-19-35(14-17-41-20)28(38)30-22-9-7-21(8-10-22)25-31-26(34-12-15-40-16-13-34)23-18-29-36(27(23)32-25)11-5-3-2-4-6-24(37)33-39/h7-10,18,20,39H,2-6,11-17,19H2,1H3,(H,30,38)(H,33,37)/t20-/m1/s1
InChi Key YPXRCUVTZDXVHY-HXUWFJFHSA-N
Smiles CC1CN(CCO1)C(=O)NC2=CC=C(C=C2)C3=NC4=C(C=NN4CCCCCCC(=O)NO)C(=N3)N5CCOCC5
Isomeric SMILES C[C@@H]1CN(CCO1)C(=O)NC2=CC=C(C=C2)C3=NC4=C(C=NN4CCCCCCC(=O)NO)C(=N3)N5CCOCC5
PubChem CID 137628684
分子量 566.65

化学和物理性质

溶解性 DMSO : 32.5 mg/mL (57.35 mM; Need ultrasonic)

质检证书（CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器

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