hSMG-1 inhibitor 11j | hSMG-1 Inhibitor | AmBeed-信号通路专用抑制剂

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hSMG-1 inhibitor 11j {[allProObj[0].p_purity_real_show]}

货号：A922737

hSMG-1 inhibitor 11j是一种嘧啶衍生物，能够有效选择性地抑制 hSMG-1，IC₅₀ 值为 0.11 nM。与 mTOR (IC₅₀=50 nM)、PI3Kα/γ (IC₅₀=92/60 nM) 和 CDK1/CDK2 (IC₅₀=32/7.1 μM) 相比，该抑制剂对 hSMG-1 具有 455 倍以上的选择性，可用于癌症相关的研究。

hSMG-1 inhibitor 11j 化学结构
CAS号：1402452-15-6

hSMG-1 inhibitor 11j 3D分子结构
CAS号：1402452-15-6

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hSMG-1 inhibitor 11j 纯度/质量文件产品仅供科研

货号：A922737 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JACS Au, 2024. Ambeed. [ A148168 ]; • JMC, 2024. Ambeed. [ A187643 ]; • JMC, 2024. Ambeed. [ A341145 , A633512 , A607865 , A167774 ]; • Biomacromolecules, 2024. Ambeed. [ A110759 ]; • Biomacromolecules, 2024. Ambeed. [ A203543 ]; 更多 >

PI3K 亚型比较
mTOR 亚型比较
GSK-3 亚型比较
CDK 亚型比较

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				mTOR,DNA-PK	{[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			mTOR,DNA-PK	{[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			mTOR,DNA-PK	{[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			mTOR,DNA-PK	{[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			PKC,Src,Sirtuin	{[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						✔		Akt,PTEN	{[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,CDK,ATM/ATR	{[allProObj[0].p_purity_real_show]}
Resibufogenin						✔		ROS	{[allProObj[0].p_purity_real_show]}
KU-57788						+ PI3K, IC50: 5 μM		mTOR,DNA-PK	{[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。

产品名称	mTOR ↓ ↑	mTORC1 ↓ ↑	mTORC2 ↓ ↑	其他靶点	纯度
AZD-8055	++++ mTOR (full length), IC50: 0.8 nM mTOR (truncated), IC50: 0.13 nM				{[allProObj[0].p_purity_real_show]}
Gedatolisib	++++ mTOR, IC50: 1.6 nM				{[allProObj[0].p_purity_real_show]}
GSK1059615	++ mTOR, IC50: 12 nM				{[allProObj[0].p_purity_real_show]}
Vistusertib	+++ mTOR, IC50: 2.8 nM				{[allProObj[0].p_purity_real_show]}
Torin 1	+++ mTOR, IC50: 4.32 nM	+++ mTORC1, IC50: 2 nM	++ mTORC2, IC50: 10 nM	DNA-PK	{[allProObj[0].p_purity_real_show]}
Dactolisib	+++ mTOR (p70S6K), IC50: 6 nM				{[allProObj[0].p_purity_real_show]}
PI-103	+ mTOR, IC50: 30 nM				{[allProObj[0].p_purity_real_show]}
WAY-600	++ mTOR, IC50: 9 nM				{[allProObj[0].p_purity_real_show]}
Voxtalisib	+ mTOR, IC50: 157 nM				{[allProObj[0].p_purity_real_show]}
PF-04691502	++ mTOR, Ki: 16 nM				{[allProObj[0].p_purity_real_show]}
Onatasertib	++ mTOR, IC50: 16 nM			DNA-PK	{[allProObj[0].p_purity_real_show]}
Chrysophanol	✔			EGFR	{[allProObj[0].p_purity_real_show]}
Samotolisib	✔			DNA-PK	{[allProObj[0].p_purity_real_show]}
Torkinib	+++ mTOR, IC50: 8 nM			PDGFR,DNA-PK	{[allProObj[0].p_purity_real_show]}
Everolimus					{[allProObj[0].p_purity_real_show]}
WYE-354	+++ mTOR, IC50: 5 nM				{[allProObj[0].p_purity_real_show]}
Tacrolimus	✔				{[allProObj[0].p_purity_real_show]}
PP121	++ mTOR, IC50: 13 nM			PDGFR,VEGFR	{[allProObj[0].p_purity_real_show]}
Torin 2	++++ mTOR, IC50: 0.25 nM			DNA-PK	{[allProObj[0].p_purity_real_show]}
Rapamycin	++++ mTOR, IC50: ~0.1 nM				{[allProObj[0].p_purity_real_show]}
GDC-0349	+++ mTOR, Ki: 3.8 nM				{[allProObj[0].p_purity_real_show]}
XL388	++ mTOR, IC50: 9.9 nM	+++ mTORC1, IC50: 8 nM	+ mTORC2, IC50: 166 nM		{[allProObj[0].p_purity_real_show]}
WYE-687	+++ mTOR, IC50: 7 nM				{[allProObj[0].p_purity_real_show]}
Apitolisib	+ mTOR, Ki app: 17 nM				{[allProObj[0].p_purity_real_show]}
WYE-132	++++ mTOR, IC50: 0.19 nM				{[allProObj[0].p_purity_real_show]}
Sapanisertib	++++ mTOR, Ki: 1.4 nM				{[allProObj[0].p_purity_real_show]}
BGT226 maleate	✔				{[allProObj[0].p_purity_real_show]}
ETP-46464	++++ mTOR, IC50: 0.6 nM			DNA-PK	{[allProObj[0].p_purity_real_show]}
PI3K-IN-1	+ mTOR, IC50: 157 nM				{[allProObj[0].p_purity_real_show]}
Zotarolimus	+++ FKBP-12, IC50: 2.8 nM				{[allProObj[0].p_purity_real_show]}
OSI-027	+++ mTOR, IC50: 4 nM	+ mTORC1, IC50: 22 nM	+ mTORC2, IC50: 65 nM		{[allProObj[0].p_purity_real_show]}
Ridaforolimus	++++ mTOR, IC50: 0.2 nM				{[allProObj[0].p_purity_real_show]}
Temsirolimus	+ mTOR, IC50: 1.76 μM				{[allProObj[0].p_purity_real_show]}
CZ415	++ mTOR, pIC50: 8.07				{[allProObj[0].p_purity_real_show]}
SF2523	+ mTOR, IC50: 280 nM			DNA-PK	{[allProObj[0].p_purity_real_show]}
KU-0063794		++ mTORC1, IC50: ~10 nM	++ mTORC2, IC50: ~10 nM		{[allProObj[0].p_purity_real_show]}
Omipalisib		++++ mTORC1, Ki: 0.18 nM	++++ mTORC2, Ki: 0.3 nM		{[allProObj[0].p_purity_real_show]}
Palomid 529		✔			{[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。

产品名称	GSK-3 ↓ ↑	GSK-3α ↓ ↑	GSK-3β ↓ ↑	纯度
AZD2858	+ GSK-3, IC50: 68 nM			{[allProObj[0].p_purity_real_show]}
Bikinin	✔			{[allProObj[0].p_purity_real_show]}
GSK 3 Inhibitor IX	++++ GSK-3, IC50: 5 nM			{[allProObj[0].p_purity_real_show]}
AZD1080		+++ GSK-3α, IC50: 6.9 nM	++ GSK-3β, IC50: 31 nM	{[allProObj[0].p_purity_real_show]}
BIO-acetoxime		+++ GSK-3α, IC50: 10 nM	+++ GSK-3β, IC50: 10 nM	{[allProObj[0].p_purity_real_show]}
SB-216763		++ GSK-3α, IC50: 34.3 nM	++ GSK-3β, IC50: ~34.3 nM	{[allProObj[0].p_purity_real_show]}
SB 415286		+ GSK-3α, IC50: 78 nM	+ GSK-3β, IC50: ~78 nM	{[allProObj[0].p_purity_real_show]}
CHIR-98014		++++ GSK-3α, IC50: 0.65 nM	++++ GSK-3β, IC50: 0.58 nM	{[allProObj[0].p_purity_real_show]}
LY2090314		++++ GSK-3α, IC50: 1.5 nM	++++ GSK-3β, IC50: 0.9 nM	{[allProObj[0].p_purity_real_show]}
CHIR 99021		+++ GSK-3α, IC50: 10 nM	++++ GSK-3β, IC50: 6.7 nM	{[allProObj[0].p_purity_real_show]}
TDZD-8			+ GSK-3β, IC50: 2 μM	{[allProObj[0].p_purity_real_show]}
Indirubin			+ GSK-3β, IC50: 0.6 μM	{[allProObj[0].p_purity_real_show]}
IM-12			++ GSK-3β, IC50: 53 nM	{[allProObj[0].p_purity_real_show]}
TWS119			++ GSK-3β, IC50: 30 nM	{[allProObj[0].p_purity_real_show]}
1-Azakenpaullone			+++ GSK-3β, IC50: 18 nM	{[allProObj[0].p_purity_real_show]}
AR-A014418			++ GSK-3β, Ki: 38 nM	{[allProObj[0].p_purity_real_show]}
Tideglusib			+ GSK-3β, IC50: 60 nM	{[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。

产品名称	Cdc ↓ ↑	CDK1 ↓ ↑	CDK19 ↓ ↑	CDK2 ↓ ↑	CDK3 ↓ ↑	CDK4 ↓ ↑	CDK5 ↓ ↑	CDK6 ↓ ↑	CDK7 ↓ ↑	CDK8 ↓ ↑	CDK9 ↓ ↑	CLK ↓ ↑	其他靶点	纯度
XL413 hydrochloride	++++ Cdc7, IC50: 3.4 nM													{[allProObj[0].p_purity_real_show]}
SU9516		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 22 nM		++ CDK4, IC50: 200 nM								{[allProObj[0].p_purity_real_show]}
RO-3306		+++ CDK1, Ki: 20 nM											ERK,SGK	{[allProObj[0].p_purity_real_show]}
R547		++++ CDK1/CyclinB, Ki: 2 nM		++++ CDK2/CyclinE, Ki: 3 nM		++++ CDK4/CyclinD1, Ki: 1 nM								{[allProObj[0].p_purity_real_show]}
BMS-265246		++++ CDK1/CyclinB, IC50: 6 nM		++++ CDK2/CyclinE, IC50: 9 nM		+ CDK4/CyclinD, IC50: 230 nM								{[allProObj[0].p_purity_real_show]}
NU6027		+ CDK1, Ki: 2.5 μM		+ CDK2, Ki: 1.3 μM									DNA-PK	{[allProObj[0].p_purity_real_show]}
Purvalanol A	++++ Cdc2/CyclinB, IC50: 4 nM			+++ CDK2/CyclinE, IC50: 35 nM CDK2/CyclinA, IC50: 70 nM		+ CDK4/CyclinD1, IC50: 850 nM								{[allProObj[0].p_purity_real_show]}
SCH900776				++ CDK2, IC50: 0.16 μM										{[allProObj[0].p_purity_real_show]}
AUZ 454				++++ CDK2(C118L), Kd: 18.6 nM CDK2(A144C), Kd: 9.7 nM										{[allProObj[0].p_purity_real_show]}
A-674563 HCl				++ CDK2, Ki: 46 nM									PKA	{[allProObj[0].p_purity_real_show]}
JNJ-7706621		++++ CDK1/CyclinB, IC50: 9 nM		++++ CDK2/CyclinE, IC50: 3 nM CDK2/CyclinA, IC50: 4 nM	++ CDK3/CyclinE, IC50: 58 nM	+ CDK4/CyclinD1, IC50: 253 nM		++ CDK6/CyclinD1, IC50: 175 nM						{[allProObj[0].p_purity_real_show]}
AT7519		++ CDK1/CyclinB, IC50: 210 nM		++ CDK2/CyclinA, IC50: 47 nM	+ CDK3/CyclinE, IC50: 360 nM	++ CDK4/CyclinD1, IC50: 100 nM	+++ CDK5/p35, IC50: 13 nM	++ CDK6/CyclinD3, IC50: 170 nM			++++ CDK9/CyclinT, IC50: <10 nM			{[allProObj[0].p_purity_real_show]}
PHA-793887		++ CDK1/CyclinB, IC50: 60 nM		++++ CDK2/CyclinE, IC50: 8 nM CDK2/CyclinA, IC50: 8 nM		++ CDK4/CyclinD1, IC50: 62 nM	++++ CDK5/p25, IC50: 5 nM		++++ CDK7/CyclinH, IC50: 10 nM		++ CDK9/CyclinT1, IC50: 138 nM			{[allProObj[0].p_purity_real_show]}
Milciclib		+ CDK1/CyclinB, IC50: 398 nM		++ CDK2/CyclinE, IC50: 363 nM CDK2/CyclinA, IC50: 45 nM		++ CDK4/CyclinD1, IC50: 160 nM	+ CDK5/p35, IC50: 265 nM		++ CDK7/CyclinH, IC50: 150 nM					{[allProObj[0].p_purity_real_show]}
Kenpaullone		+ CDK1/CyclinB, IC50: 0.4μM		+ CDK2/CyclinE, IC50: 7.5μM CDK2/CyclinA, IC50: 0.68μM			+ CDK5/p35, IC50: 0.85μM							{[allProObj[0].p_purity_real_show]}
SNS-032				+++ CDK2/CyclinE, IC50: 48 nM CDK2/CyclinA, IC50: 38 nM			+ CDK5/p35, IC50: 340 nM		++ CDK7/CyclinH, IC50: 62 nM		++++ CDK9/CyclinT, IC50: 4 nM			{[allProObj[0].p_purity_real_show]}
Dinaciclib		++++ CDK1, IC50: 3 nM		++++ CDK2, IC50: 1 nM			++++ CDK5, IC50: 1 nM				++++ CDK9, IC50: 4 nM			{[allProObj[0].p_purity_real_show]}
PHA-767491 hydrochloride	++++ Cdc7, IC50: 10 nM	+ CDK1, IC50: 250 nM		+ CDK2, IC50: 240 nM			+ CDK5, IC50: 460 nM				+++ CDK9, IC50: 34 nM		MK2	{[allProObj[0].p_purity_real_show]}
(R)-Roscovitine	+ Cdc2/CyclinB, IC50: 0.65 μM			+ CDK2/CyclinE, IC50: 0.7 μM CDK2/CyclinA, IC50: 0.7 μM			++ CDK5/p35, IC50: 0.16 μM							{[allProObj[0].p_purity_real_show]}
Narazaciclib						++++ CDK4/CyclinD1, IC50: 3.87 nM		++++ CDK6/CyclinD1, IC50: 9.82 nM					RET	{[allProObj[0].p_purity_real_show]}
Palbociclib						++++ CDK4/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 nM		+++ CDK6/CyclinD2, IC50: 15 nM						{[allProObj[0].p_purity_real_show]}
Abemaciclib						++++ CDK4, IC50: 2 nM		++++ CDK6, IC50: 10 nM						{[allProObj[0].p_purity_real_show]}
Ribociclib						++++ CDK4, IC50: 10 nM		+++ CDK6, IC50: 39 nM						{[allProObj[0].p_purity_real_show]}
Palbociclib isethionate						++++ CDK4/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 nM		+++ CDK6/CyclinD2, IC50: 15 nM						{[allProObj[0].p_purity_real_show]}
BS-181 HCl									+++ CDK7, IC50: 21 nM					{[allProObj[0].p_purity_real_show]}
(E/Z)-THZ1 dihydrochloride									++++ CDK7, IC50: 3.2 nM					{[allProObj[0].p_purity_real_show]}
LDC4297									++++ CDK7, IC50: 0.13 nM					{[allProObj[0].p_purity_real_show]}
Senexin A			+ CDK19, Kd: 0.31 μM							+ CDK8, Kd: 0.83 μM				{[allProObj[0].p_purity_real_show]}
MSC2530818										++++ CDK8, IC50: 2.6 nM				{[allProObj[0].p_purity_real_show]}
Wogonin											✔			{[allProObj[0].p_purity_real_show]}
Riviciclib HCl		++ CDK1/CyclinB, IC50: 79 nM		+ CDK2/CyclinE, IC50: 2.54 μM CDK2/CyclinA, IC50: 224 nM		++ CDK4/CyclinD1, IC50: 63 nM		+ CDK6/CyclinD3, IC50: 396 nM	+ CDK7/CyclinH, IC50: 2.87 μM		+++ CDK9/CyclinT1, IC50: 20 nM			{[allProObj[0].p_purity_real_show]}
LDC000067				+ CDK2, IC50: 2.441 μM							++ CDK9, IC50: 44 nM			{[allProObj[0].p_purity_real_show]}
Flavopiridol		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 40 nM		+++ CDK4, IC50: 40 nM		+++ CDK6, IC50: 40 nM	+ CDK7, IC50: 300 nM		+++ CDK9, IC50: 20 nM			{[allProObj[0].p_purity_real_show]}
LY2857785									+ CDK7, IC50: 0.246 μM	+++ CDK8, IC50: 0.016 μM	+++ CDK9, IC50: 0.011 μM			{[allProObj[0].p_purity_real_show]}
AZD-5438		+++ CDK1, IC50: 16 nM		++++ CDK2, IC50: 6 nM							+++ CDK9, IC50: 20 nM			{[allProObj[0].p_purity_real_show]}
ML167												++ Dyrk1B , IC50: 1648 nM CLK4, IC50: 136 nM		{[allProObj[0].p_purity_real_show]}
(E/Z)-TG003												+++ mCLK4, IC50: 15 nM mCLK1, IC50: 200 nM		{[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。

hSMG-1 inhibitor 11j 生物活性

描述

The pyrimidine derivative hSMG-1 inhibitor 11j is a potent and selective inhibitor of hSMG-1, with an IC50 of 0.11 nM. It demonstrates >455-fold selectivity for hSMG-1 over mTOR (IC50=50 nM), PI3Kα/γ (IC50=92/60 nM), and CDK1/CDK2 (IC50=32/7.1 μM). This inhibitor can be utilized for cancer research ^[1].

体外研究

In MDA 361 cells, treatment with hSMG-1 inhibitor 11j (0.3-3 μM; 6 h) markedly decreases UPF1 phosphorylation at 0.3 μM and abolishes it at 1 μM ^[1].

HSMG-1 inhibitor 11j suppresses the proliferation of MDA468 cells, with an IC50 of 75 nM ^[1].

hSMG-1 inhibitor 11j 参考文献

[1]Gopalsamy A, et, al. Identification of pyrimidine derivatives as hSMG-1 inhibitors. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6636-41.

hSMG-1 inhibitor 11j 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.77mL

0.35mL

0.18mL

8.83mL

1.77mL

0.88mL

17.67mL

3.53mL

1.77mL

hSMG-1 inhibitor 11j 技术信息

CAS号	1402452-15-6
分子式	C₂₇H₂₈ClN₇O₃S
分子量	566.074

别名
运输	蓝冰

存储条件

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 85 mg/mL(150.16 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

hSMG-1 inhibitor 11j {[allProObj[0].p_purity_real_show]}

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hSMG-1 inhibitor 11j 技术信息

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