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HS-173 {[allProObj[0].p_purity_real_show]}

货号:A336342 Ambeed 开学季,买赠积分,赢豪礼

HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM.

HS-173 化学结构 CAS号:1276110-06-5
HS-173 化学结构
CAS号:1276110-06-5
HS-173 3D分子结构
CAS号:1276110-06-5
HS-173 化学结构 CAS号:1276110-06-5
HS-173 3D分子结构 CAS号:1276110-06-5
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HS-173 纯度/质量文件 产品仅供科研

货号:A336342 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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产品名称 C2β p110α p110β p110γ p110δ PI3K Vps34 其他靶点 纯度
A66 +

C2β, IC50: 462 nM

++

p110α, IC50: 32 nM

{[allProObj[0].p_purity_real_show]}
Taselisib +

C2β, IC50: 292 nM

++++

PI3Kα, Ki: 0.29 nM

+++

PI3Kβ, Ki: 9.1 nM

++++

PI3Kγ, Ki: 0.97 nM

++++

PI3Kδ, Ki: 0.12 nM

+

hVps34, IC50: 374 nM

{[allProObj[0].p_purity_real_show]}
Gedatolisib ++++

PI3Kα, IC50: 0.4 nM

+++

PI3Kγ, IC50: 5.4 nM

mTOR {[allProObj[0].p_purity_real_show]}
HS-173 ++++

PI3Kα , IC50: 0.8 nM

{[allProObj[0].p_purity_real_show]}
Serabelisib +++

PI3Kα, IC50: 21 nM

{[allProObj[0].p_purity_real_show]}
GNE-477 ++++

PI3Kα, IC50: 4 nM

mTOR {[allProObj[0].p_purity_real_show]}
YM-201636 +

p110α, IC50: 3.3 μM

PIKfyve {[allProObj[0].p_purity_real_show]}
AS-252424 +

PI3Kα, IC50: 935 nM

++

PI3Kγ, IC50: 33 nM

{[allProObj[0].p_purity_real_show]}
Alpelisib +++

PI3Kα, IC50: 5 nM

{[allProObj[0].p_purity_real_show]}
AS-604850 +

PI3Kα, IC50: 4.5 μM

+

PI3Kγ, IC50: 0.25 μM

{[allProObj[0].p_purity_real_show]}
SF2523 ++

PI3Kα, IC50: 34 nM

++

PI3Kγ, IC50: 158 nM

DNA-PK,mTOR {[allProObj[0].p_purity_real_show]}
Inavolisib ++++

PI3K alpha, IC50: 0.038 nM

{[allProObj[0].p_purity_real_show]}
Bimiralisib ++++

PI3Kα, Kd: 1.5 nM

+++

PI3Kβ, Kd: 11 nM

++

PI3Kγ, Kd: 25 nM

++

PI3Kδ, Kd: 25 nM

mTOR {[allProObj[0].p_purity_real_show]}
GSK1059615 ++++

PI3Kα, IC50: 0.4 nM

++++

PI3Kβ, IC50: 0.6 nM

+++

PI3Kγ, IC50: 5 nM

++++

PI3Kδ, IC50: 2 nM

mTOR {[allProObj[0].p_purity_real_show]}
GSK2636771 {[allProObj[0].p_purity_real_show]}
Fimepinostat +++

PI3Kα, IC50: 19 nM

++

PI3Kβ, IC50: 54 nM

++

PI3Kδ, IC50: 39 nM

{[allProObj[0].p_purity_real_show]}
VS-5584 ++++

PI3Kα, IC50: 2.6 nM

+++

PI3Kβ, IC50: 21 nM

++++

PI3Kγ, IC50: 3.0 nM

++++

PI3Kδ, IC50: 2.7 nM

mTOR {[allProObj[0].p_purity_real_show]}
Dactolisib ++++

p110α1, IC50: 4 nM

++

p110β, IC50: 75 nM

+++

p110γ, IC50: 5 nM

+++

p110δ, IC50: 7 nM

{[allProObj[0].p_purity_real_show]}
PI-103 ++++

p110α, IC50: 2 nM

++++

p110β, IC50: 3 nM

+++

p110γ, IC50: 15 nM

++++

p110δ, IC50: 3 nM

DNA-PK,mTOR {[allProObj[0].p_purity_real_show]}
PI-3065 +

p110β, IC50: 1078 nM

+++

p110δ, IC50: 15 nM

{[allProObj[0].p_purity_real_show]}
Voxtalisib ++

PI3Kα, IC50: 39 nM

++

PI3Kβ, IC50: 113 nM

+++

PI3Kγ, IC50: 9 nM

++

PI3Kδ, IC50: 43 nM

DNA-PK,mTOR {[allProObj[0].p_purity_real_show]}
AZD-8835 +++

PI3Kα, IC50: 6.2 nM

+

PI3Kβ, IC50: 431 nM

++

PI3Kγ, IC50: 90 nM

+++

PI3Kδ, IC50: 5.7 nM

{[allProObj[0].p_purity_real_show]}
Pilaralisib analogue ++

PI3Kα, IC50: 39 nM

++

PI3Kβ, IC50: 36 nM

+++

PI3Kγ, IC50: 23 nM

++

PI3Kδ, IC50: 36 nM

{[allProObj[0].p_purity_real_show]}
ZSTK474 +++

PI3Kα, IC50: 16 nM

++

PI3Kβ, IC50: 44 nM

++

PI3Kγ, IC50: 49 nM

+++

PI3Kδ, IC50: 4.6 nM

++

PI3K, IC50: 37 nM

{[allProObj[0].p_purity_real_show]}
AS-605240 ++

PI3Kα, IC50: 60 nM

+

PI3Kβ, IC50: 270 nM

+++

PI3Kγ, IC50: 8 nM

+

PI3Kδ, IC50: 300 nM

{[allProObj[0].p_purity_real_show]}
TGX-221 +++

p110β, IC50: 5 nM

++

p110δ, IC50: 0.1 μM

{[allProObj[0].p_purity_real_show]}
PF-04691502 ++++

PI3Kα, Ki: 1.8 nM

++++

PI3Kβ, Ki: 2.1 nM

++++

PI3Kγ, Ki: 1.9 nM

++++

PI3Kδ, Ki: 1.6 nM

mTOR {[allProObj[0].p_purity_real_show]}
GDC-0084 ++++

PI3Kα, Ki app: 2 nM

++

PI3Kβ, Ki app: 46 nM

+++

PI3Kγ, Ki app: 10 nM

++++

PI3Kδ, Ki app: 3 nM

mTOR {[allProObj[0].p_purity_real_show]}
Buparlisib ++

p110α, IC50: 52 nM

+

p110β, IC50: 166 nM

+

p110γ, IC50: 262 nM

++

p110δ, IC50: 116 nM

+

Vps34, IC50: 2.4 μM

mTOR {[allProObj[0].p_purity_real_show]}
LY294002 +

p110α, IC50: 0.5 μM

+

p110β, IC50: 0.97 μM

+

p110δ, IC50: 0.57 μM

DNA-PK {[allProObj[0].p_purity_real_show]}
AZD 6482 +

PI3Kα, IC50: 870 nM

+++

PI3Kβ, IC50: 10 nM

++

PI3Kδ, IC50: 80 nM

DNA-PK {[allProObj[0].p_purity_real_show]}
Pictilisib ++++

p110α, IC50: 3 nM

++

p110β, IC50: 33 nM

++

p110γ, IC50: 75 nM

++++

p110δ, IC50: 3 nM

mTOR {[allProObj[0].p_purity_real_show]}
PKI-402 ++++

PI3Kα, IC50: 2 nM

+++

PI3Kβ, IC50: 7 nM

+++

PI3Kγ, IC50: 16 nM

+++

PI3Kδ, IC50: 14 nM

mTOR {[allProObj[0].p_purity_real_show]}
Copanlisib ++++

PI3Kα, IC50: 0.5 nM

++++

PI3Kβ, IC50: 3.7 nM

+++

PI3Kγ, IC50: 6.4 nM

++++

PI3Kδ, IC50: 0.7 nM

{[allProObj[0].p_purity_real_show]}
Omipalisib ++++

p110α, Ki: 0.019 nM

++++

p110β, Ki: 0.13 nM

++++

p110γ, Ki: 0.06 nM

++++

p110δ, Ki: 0.024 nM

{[allProObj[0].p_purity_real_show]}
Izorlisib +++

PI3Kα, IC50: 14 nM

++

PI3Kβ, IC50: 0.12 μM

++

PI3Kγ, IC50: 36 nM

+

PI3Kδ, IC50: 0.50 μM

{[allProObj[0].p_purity_real_show]}
AZD8186 ++

PI3Kα, IC50: 35 nM

++++

PI3Kβ, IC50: 4 nM

+++

PI3Kδ, IC50: 12 nM

{[allProObj[0].p_purity_real_show]}
KU-0060648 ++++

PI3Kα, IC50: 4 nM

++++

PI3Kβ, IC50: 0.5 nM

+

PI3Kγ, IC50: 0.59 μM

++++

PI3Kδ, IC50: 0.1 nM

DNA-PK {[allProObj[0].p_purity_real_show]}
Apitolisib +++

p110α, IC50: 5 nM

++

p110β, IC50: 27 nM

+++

p110γ, IC50: 14 nM

+++

p110δ, IC50: 7 nM

mTOR {[allProObj[0].p_purity_real_show]}
CZC24832 +

PI3Kβ, IC50: 1.1 μM

++

PI3Kγ, IC50: 27 nM

{[allProObj[0].p_purity_real_show]}
BGT226 maleate ++++

PI3Kα, IC50: 4 nM

++

PI3Kβ, IC50: 63 nM

++

PI3Kγ, IC50: 38 nM

mTOR {[allProObj[0].p_purity_real_show]}
TG 100713 ++

PI3Kα, IC50: 165 nM

+

PI3Kβ, IC50: 215 nM

++

PI3Kγ, IC50: 50 nM

+++

PI3Kδ, IC50: 24 nM

{[allProObj[0].p_purity_real_show]}
PI3K-IN-1 ++

PI3Kα, IC50: 39 nM

++

PI3Kβ, IC50: 113 nM

+++

PI3Kγ, IC50: 9 nM

++

PI3Kδ, IC50: 43 nM

DNA-PK,mTOR {[allProObj[0].p_purity_real_show]}
TG100-115 +

PI3Kα, IC50: 1.3 μM

+

PI3Kβ, IC50: 1.2 μM

++

PI3Kγ, IC50: 83 nM

+

PI3Kδ, IC50: 235 nM

{[allProObj[0].p_purity_real_show]}
PIK-90 +++

PI3Kα, IC50: 11 nM

+

PI3Kβ, IC50: 350 nM

+++

PI3Kγ, IC50: 18 nM

++

PI3Kδ, IC50: 58 nM

{[allProObj[0].p_purity_real_show]}
PIK-294 +

p110β, IC50: 490 nM

++

p110γ, IC50: 160 nM

+++

p110δ, IC50: 10 nM

{[allProObj[0].p_purity_real_show]}
Duvelisib ++++

PI3Kβ, Ki: 1564 pM

++

PI3Kγ, Ki: 243 pM

++++

PI3Kδ, Ki: 23 pM

{[allProObj[0].p_purity_real_show]}
GDC-0326 ++++

PI3Kα, Ki: 0.2 nM

++

PI3Kβ, Ki: 26.6 nM

+++

PI3Kγ, Ki: 10.2 nM

++++

PI3Kδ, Ki: 4 nM

{[allProObj[0].p_purity_real_show]}
Quercetin Dihydrate +

PI3Kβ, IC50: 5.4 μM

+

PI3Kγ, IC50: 2.4 μM

+

PI3Kδ, IC50: 3.0 μM

{[allProObj[0].p_purity_real_show]}
Quercetin +

PI3Kβ, IC50: 5.4 μM

+

PI3Kγ, IC50: 2.4 μM

+

PI3Kδ, IC50: 3.0 μM

Sirtuin,PKC,Src {[allProObj[0].p_purity_real_show]}
Leniolisib +

PI3Kα, IC50: 0.244 μM

+

PI3Kβ, IC50: 0.424 μM

+

PI3Kγ, IC50: 2.23 μM

+++

PI3Kδ, IC50: 0.011 μM

DNA-PK {[allProObj[0].p_purity_real_show]}
PIK-108 {[allProObj[0].p_purity_real_show]}
Eganelisib +++

PI3Kγ, IC50: 16 nM

{[allProObj[0].p_purity_real_show]}
CAY10505 {[allProObj[0].p_purity_real_show]}
IPI-3063 ++++

p110δ, IC50: 2.5 nM

{[allProObj[0].p_purity_real_show]}
Nemiralisib ++++

PI3Kδ, pKi: 9.9

{[allProObj[0].p_purity_real_show]}
PF-4989216 ++++

p110α, IC50: 2 nM

++

p110γ, IC50: 65 nM

++++

p110δ, IC50: 1 nM

{[allProObj[0].p_purity_real_show]}
PIK-75 HCl +++

p110α, IC50: 5.8 nM

++

p110γ, IC50: 76 nM

+

p110δ, IC50: 0.51 μM

DNA-PK {[allProObj[0].p_purity_real_show]}
Tenalisib ++

PI3Kγ, IC50: 33.2 nM

++

PI3Kδ, IC50: 24.5 nM

{[allProObj[0].p_purity_real_show]}
Acalisib +++

p110δ, IC50: 14 nM

{[allProObj[0].p_purity_real_show]}
Umbralisib +++

PI3Kδ, IC50: 22.2 nM

{[allProObj[0].p_purity_real_show]}
AMG319 +

PI3Kγ, IC50: 850 nM

+++

PI3Kδ, IC50: 18 nM

{[allProObj[0].p_purity_real_show]}
IC-87114 +

PI3Kγ, IC50: 29 μM

+

PI3Kδ, IC50: 0.5 μM

{[allProObj[0].p_purity_real_show]}
Idelalisib ++

p110γ, IC50: 89 nM

++++

p110δ, IC50: 2.5 nM

{[allProObj[0].p_purity_real_show]}
PIK-293 +

p110γ, IC50: 10 μM

+

p110δ, IC50: 0.24 μM

{[allProObj[0].p_purity_real_show]}
Vps34-PIK-III +

PI3Kδ, IC50: 1.2μM

+++

Vps34, IC50: 0.018μM

{[allProObj[0].p_purity_real_show]}
GSK2292767 {[allProObj[0].p_purity_real_show]}
Seletalisib +

PI3Kγ, IC50: 282 nM

+++

PI3Kδ, IC50: 12 nM

{[allProObj[0].p_purity_real_show]}
P110δ-IN-1 ++++

P110δ, IC50: 0.6 nM

{[allProObj[0].p_purity_real_show]}
PI3Kδ-IN-5 ++++

PI3Kδ, IC50: 0.9 nM

{[allProObj[0].p_purity_real_show]}
SRX3207 +

PI3K alpha, IC50: 244 nM

+

PI3K gamma, IC50: 9790 nM

+

PI3K delta, IC50: 388 nM

Syk {[allProObj[0].p_purity_real_show]}
Parsaclisib HCl ++++

PI3Kδ, IC50: 1 nM

{[allProObj[0].p_purity_real_show]}
IHMT-PI3Kδ-372 +++

PI3Kδ, IC50: 14 nM

{[allProObj[0].p_purity_real_show]}
Trigonelline Akt {[allProObj[0].p_purity_real_show]}
Wortmannin ++++

PI3K, IC50: 3 nM

MLCK,DNA-PK {[allProObj[0].p_purity_real_show]}
Samotolisib DNA-PK {[allProObj[0].p_purity_real_show]}
GNE-317 {[allProObj[0].p_purity_real_show]}
Oroxin B PTEN,Akt {[allProObj[0].p_purity_real_show]}
NU 7026 +

PI3K, IC50: 13 μM

DNA-PK {[allProObj[0].p_purity_real_show]}
Deguelin Akt {[allProObj[0].p_purity_real_show]}
Ailanthone Akt,ATM/ATR,CDK {[allProObj[0].p_purity_real_show]}
Resibufogenin ROS {[allProObj[0].p_purity_real_show]}
KU-57788 +

PI3K, IC50: 5 μM

DNA-PK,mTOR {[allProObj[0].p_purity_real_show]}
Cinobufagine Akt {[allProObj[0].p_purity_real_show]}
α-Linolenic acid {[allProObj[0].p_purity_real_show]}
MTX-211 EGFR {[allProObj[0].p_purity_real_show]}
PI3K/mTOR Inhibitor-2 ++++

PI3K, IC50: 3.4 nM

mTOR {[allProObj[0].p_purity_real_show]}
SPP-86 {[allProObj[0].p_purity_real_show]}
(E)-Akt inhibitor-IV {[allProObj[0].p_purity_real_show]}
Vps34-IN-1 ++

Vps34, IC50: 25 nM

{[allProObj[0].p_purity_real_show]}
SAR405 ++++

Vps34, IC50: 1.2 nM

{[allProObj[0].p_purity_real_show]}
3-Methyladenine +

PI3Kγ, IC50: 60 μM

+

Vps34, IC50: 25 μM

Autophagy {[allProObj[0].p_purity_real_show]}
Vps34-IN-4 +++

VPS34, IC50: 15 nM

{[allProObj[0].p_purity_real_show]}
Autophinib +++

Vps34, IC50: 19 nM

Autophagy {[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

HS-173 生物活性

靶点
  • p110α

    PI3Kα , IC50:0.8 nM

描述 HS-173, at concentrations ranging from 0.1 to 10 μM, diminishes cell viability in a manner that is both concentration and time-dependent. It effectively curbs the growth of colonies in pancreatic cancer cells as the dosage increases. Moreover, HS-173 blocks cell migration and invasion triggered by TGF-β in pancreatic cancer cells and prevents TGF-β-induced epithelial-mesenchymal transition (EMT)[1]. In experiments with two hepatic stellate cell lines, HS-173 application leads to a reduction in cell viability, influenced by the dosage and duration of treatment. It prompts a halt in the cell cycle at the G2/M phase. The compound elevates levels of cleaved caspase-3 and reduces those of Bcl-2 in HSC-T6 cells. Furthermore, HS-173 curtails the expression of pro-fibrotic mediators and modulators of extracellular matrix (ECM) degradation in hepatic stellate cells (HSCs)[2]. The co-administration of Sorafenib and HS-173 acts synergistically to halt cell proliferation in pancreatic cancer cell lines, affecting crucial enzymes within the RAF/MAPK and PI3K/AKT signaling pathways[3].
体内研究

Administered intraperitoneally at 10 mg/kg, HS-173 significantly upregulates TUNEL and cleaved caspase-3 expression while downregulating PCNA expression in tumor tissues. It also diminishes the levels of phosphorylated AKT and Smad2 in these tissues. Doses of 10 and 30 mg/kg of HS-173 markedly reduce metastatic spread to the lungs and liver[1].

At doses of 10 and 20 mg/kg, HS-173 tackles ECM accumulation and the PI3K/Akt pathway in a mouse model of liver fibrosis induced by CCl4. It notably lowers the levels of phosphorylated Akt and p-P70S6K, alongside reducing collagen I and vimentin expression in the liver fibrosis model[2].

体外研究

HS-173, at concentrations ranging from 0.1 to 10 μM, diminishes cell viability in a manner that is both concentration and time-dependent. It effectively curbs the growth of colonies in pancreatic cancer cells as the dosage increases. Moreover, HS-173 blocks cell migration and invasion triggered by TGF-β in pancreatic cancer cells and prevents TGF-β-induced epithelial-mesenchymal transition (EMT)[1].

In experiments with two hepatic stellate cell lines, HS-173 application leads to a reduction in cell viability, influenced by the dosage and duration of treatment. It prompts a halt in the cell cycle at the G2/M phase. The compound elevates levels of cleaved caspase-3 and reduces those of Bcl-2 in HSC-T6 cells. Furthermore, HS-173 curtails the expression of pro-fibrotic mediators and modulators of extracellular matrix (ECM) degradation in hepatic stellate cells (HSCs)[2].

The co-administration of Sorafenib and HS-173 acts synergistically to halt cell proliferation in pancreatic cancer cell lines, affecting crucial enzymes within the RAF/MAPK and PI3K/AKT signaling pathways[3].

HS-173 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
MCF7 cells Cytotoxicity assay 48 h Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=7.8 μM 21388141
SK-BR-3 cells Cytotoxicity assay 48 h Cytotoxicity against human SK-BR-3 cells after 48 hrs by MTT assay, IC50=1.5 μM 21388141
T47D cells Cytotoxicity assay 48 h Cytotoxicity against human T47D cells after 48 hrs by MTT assay, IC50=0.6 μM 21388141

HS-173 参考文献

[1]Rumman M, et al. HS-173, a novel PI3K inhibitor suppresses EMT and metastasis in pancreatic cancer. Oncotarget. 2016 Oct 25

[2]Son MK, et al. HS-173, a novel PI3K inhibitor, attenuates the activation of hepatic stellate cells in liver fibrosis. Sci Rep. 2013 Dec 11;3:3470

[3]Yun SM, et al. Synergistic anticancer activity of HS-173, a novel PI3K inhibitor in combination with Sorafenib against pancreatic cancer cells. Cancer Lett. 2013 May 1;331(2):250-61

HS-173 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.37mL

0.47mL

0.24mL

11.84mL

2.37mL

1.18mL

23.67mL

4.73mL

2.37mL

HS-173 技术信息

CAS号1276110-06-5
分子式C21H18N4O4S
分子量 422.457
别名
运输蓝冰
存储条件

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 50 mg/mL(118.36 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方

IP 2% DMSO+2% Tween80+30% PEG300+water 4 mg/mL clear

PO 0.5% CMC-Na 34 mg/mL suspension

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