NU6027 | CDK/ATR Inhibitor | AmBeed-信号通路专用抑制剂

NU6027 {[allProObj[0].p_purity_real_show]}

货号：A488693

NU6027是一种有效的 ATR/CDK 抑制剂，可抑制 CDK1/2、ATR 和 DNA-PK，其 Ki 分别为 2.5 μM/1.3 μM、0.4 μM 和 2.2 μM，并比基于 6-氨基嘌呤的抑制剂更易进入细胞。

NU6027 化学结构
CAS号：220036-08-8

NU6027 3D分子结构
CAS号：220036-08-8

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CDK 亚型比较

产品名称	Cdc ↓ ↑	CDK1 ↓ ↑	CDK19 ↓ ↑	CDK2 ↓ ↑	CDK3 ↓ ↑	CDK4 ↓ ↑	CDK5 ↓ ↑	CDK6 ↓ ↑	CDK7 ↓ ↑	CDK8 ↓ ↑	CDK9 ↓ ↑	CLK ↓ ↑	其他靶点	纯度
XL413 HCl	++++ Cdc7, IC50: 3.4 nM													99%+
SU9516		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 22 nM		++ CDK4, IC50: 200 nM								99%+
RO-3306		+++ CDK1, Ki: 20 nM											ERK,SGK	98%
R547		++++ CDK1/CyclinB, Ki: 2 nM		++++ CDK2/CyclinE, Ki: 3 nM		++++ CDK4/CyclinD1, Ki: 1 nM								99%+
BMS-265246		++++ CDK1/CyclinB, IC50: 6 nM		++++ CDK2/CyclinE, IC50: 9 nM		+ CDK4/CyclinD, IC50: 230 nM								99%+
NU6027		+ CDK1, Ki: 2.5 μM		+ CDK2, Ki: 1.3 μM									DNA-PK	98%
Purvalanol A	++++ Cdc2/CyclinB, IC50: 4 nM			+++ CDK2/CyclinE, IC50: 35 nM CDK2/CyclinA, IC50: 70 nM		+ CDK4/CyclinD1, IC50: 850 nM								99%+
SCH900776				++ CDK2, IC50: 0.16 μM										99%+
AUZ 454				++++ CDK2(A144C), Kd: 9.7 nM CDK2(C118L), Kd: 18.6 nM										99%+
A-674563 HCl				++ CDK2, Ki: 46 nM									PKA	99%
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						99%+
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			98+%
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			99%+
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					99%+
Kenpaullone		+ CDK1/CyclinB, IC50: 0.4μM		+ CDK2/CyclinE, IC50: 7.5μM CDK2/CyclinA, IC50: 0.68μM			+ CDK5/p35, IC50: 0.85μM							98%
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			99%+
Dinaciclib		++++ CDK1, IC50: 3 nM		++++ CDK2, IC50: 1 nM			++++ CDK5, IC50: 1 nM				++++ CDK9, IC50: 4 nM			99%+
PHA-767491 HCl	++++ Cdc7, IC50: 10 nM	+ CDK1, IC50: 250 nM		+ CDK2, IC50: 240 nM			+ CDK5, IC50: 460 nM				+++ CDK9, IC50: 34 nM		MK2	99%
(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							99%+
Narazaciclib						++++ CDK4/CyclinD1, IC50: 3.87 nM		++++ CDK6/CyclinD1, IC50: 9.82 nM					RET	99%+
Palbociclib						++++ CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%
Abemaciclib						++++ CDK4, IC50: 2 nM		++++ CDK6, IC50: 10 nM						99%
Ribociclib						++++ CDK4, IC50: 10 nM		+++ CDK6, IC50: 39 nM						98%
Palbociclib isethionate						++++ CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%+
BS-181 HCl									+++ CDK7, IC50: 21 nM					99%+
(E/Z)-THZ1 2HCl									++++ CDK7, IC50: 3.2 nM					99%+
LDC4297									++++ CDK7, IC50: 0.13 nM					99%+
Senexin A			+ CDK19, Kd: 0.31 μM							+ CDK8, Kd: 0.83 μM				99%
MSC2530818										++++ CDK8, IC50: 2.6 nM				99%+
Wogonin											✔			99%+
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			98%
LDC000067				+ CDK2, IC50: 2.441 μM							++ CDK9, IC50: 44 nM			98%
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			99%+
LY2857785									+ CDK7, IC50: 0.246 μM	+++ CDK8, IC50: 0.016 μM	+++ CDK9, IC50: 0.011 μM			99%+
AZD-5438		+++ CDK1, IC50: 16 nM		++++ CDK2, IC50: 6 nM							+++ CDK9, IC50: 20 nM			99%+
ML167												++ CLK4, IC50: 136 nM Dyrk1B , IC50: 1648 nM		99%+
(E/Z)-TG003												+++ mCLK1, IC50: 200 nM mCLK4, IC50: 15 nM		99%+
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。

NU6027 生物活性

靶点

CDK2

CDK2, Ki:1.3 μM
CDK1

CDK1, Ki:2.5 μM

描述

Cyclin-dependent kinases (CDKs) are the catalytic subunits of a family of mammalian heterodimeric serine/threonine kinases that have been implicated in the control of cell-cycle progression, transcription and neuronal function^[3]. NU6027 is a potent and ATP-competitive inhibitor of both CDK1 and CDK2, with Kis of 2.5 µM and 1.3 µM, respectively. NU6027 is also a potent inhibitor of ATR and enhances hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner^[4]. NU6027 attenuated G2/M arrest following DNA damage, inhibited RAD51 focus formation and increased the cytotoxicity of the major classes of DNA-damaging anticancer cytotoxic therapy but not the antimitotic, paclitaxel. NU6027 was synthetically lethal when DNA single-strand break repair is impaired either through poly(ADP-ribose) polymerase (PARP) inhibition or defects in XRCC1^[5]. NU6027 prevented the Trovafloxacin-mediated increases in LPS-induced TNF mRNA and protein release, Trovafloxacin prolonged TNF mRNA stability, and this effect was largely attenuated by NU6027^[6]. NU-6027 inhibits Mycobacterium bovis BCG growth in vitro and also displayed cross-reactivity with Mycobacterium tuberculosis protein kinase D (PknD) and protein kinase G (PknG)^[7].

NU6027 细胞实验

Cell Line RAW 264.7 murine macrophages CP70-B1 and CP70-A2 cells A2780 cells MCF7 cells GM847KD cells Mouse cortical neurons THP-1 macrophages M. bovis BCG HEK293 cells	Concentration	Treated Time	Description	References
RAW 264.7 murine macrophages	10 µM	1 hour	NU6027 inhibited ATR signaling and prevented TVX-mediated increases in LPS-induced TNF mRNA and protein release	J Pharmacol Exp Ther. 2014 Jul;350(1):164-70.
CP70-B1 and CP70-A2 cells	4 µM and 10 µM	24 hours	NU6027 enhanced temozolomide cytotoxicity, with greater effects in MMR-proficient CP70-B1 cells	Br J Cancer. 2011 Jul 26;105(3):372-81.
A2780 cells	4 µM and 10 µM	24 hours	NU6027 significantly enhanced cisplatin cytotoxicity, with greater effects in p53 wild-type cells	Br J Cancer. 2011 Jul 26;105(3):372-81.
MCF7 cells	6.7 µM (IC50 )	24 hours	NU6027 inhibits ATR activity with an IC50 of 6.7 μM	Br J Cancer. 2011 Jul 26;105(3):372-81.
GM847KD cells	2.8 µM (IC50 )	24 hours	NU6027 inhibits ATR activity with an IC50 of 2.8 μM	Br J Cancer. 2011 Jul 26;105(3):372-81.
Mouse cortical neurons	1 µM	24 hours	NU6027 significantly reduced H2O2-induced neuronal death, confirmed by LDH release and PI staining.	Mol Neurobiol. 2019 Apr;56(4):2822-2835.
THP-1 macrophages	25 µM	4 days	NU-6027 inhibits growth of M. bovis BCG and M. tuberculosis in macrophages	Antimicrob Agents Chemother. 2019 Aug 23;63(9):e00996-19.
M. bovis BCG	1.56 µM (IC99 )	7 days	NU-6027 inhibits M. bovis BCG growth in a dose- and time-dependent manner	Antimicrob Agents Chemother. 2019 Aug 23;63(9):e00996-19.
HEK293 cells	1 µM		NU6027 inhibited TRPC5-mediated currents, indicating a direct action on TRPC5 channels.	Mol Neurobiol. 2019 Apr;56(4):2822-2835.

Cell Line

RAW 264.7 murine macrophages CP70-B1 and CP70-A2 cells A2780 cells MCF7 cells GM847KD cells Mouse cortical neurons THP-1 macrophages M. bovis BCG HEK293 cells

Concentration

Treated Time

Description

References

RAW 264.7 murine macrophages

10 µM

1 hour

NU6027 inhibited ATR signaling and prevented TVX-mediated increases in LPS-induced TNF mRNA and protein release

J Pharmacol Exp Ther. 2014 Jul;350(1):164-70.

CP70-B1 and CP70-A2 cells

4 µM and 10 µM

24 hours

NU6027 enhanced temozolomide cytotoxicity, with greater effects in MMR-proficient CP70-B1 cells

Br J Cancer. 2011 Jul 26;105(3):372-81.

A2780 cells

4 µM and 10 µM

24 hours

NU6027 significantly enhanced cisplatin cytotoxicity, with greater effects in p53 wild-type cells

Br J Cancer. 2011 Jul 26;105(3):372-81.

MCF7 cells

6.7 µM (IC50 )

24 hours

NU6027 inhibits ATR activity with an IC50 of 6.7 μM

Br J Cancer. 2011 Jul 26;105(3):372-81.

GM847KD cells

2.8 µM (IC50 )

24 hours

NU6027 inhibits ATR activity with an IC50 of 2.8 μM

Br J Cancer. 2011 Jul 26;105(3):372-81.

Mouse cortical neurons

1 µM

24 hours

NU6027 significantly reduced H2O2-induced neuronal death, confirmed by LDH release and PI staining.

Mol Neurobiol. 2019 Apr;56(4):2822-2835.

THP-1 macrophages

25 µM

4 days

NU-6027 inhibits growth of M. bovis BCG and M. tuberculosis in macrophages

Antimicrob Agents Chemother. 2019 Aug 23;63(9):e00996-19.

M. bovis BCG

1.56 µM (IC99 )

7 days

NU-6027 inhibits M. bovis BCG growth in a dose- and time-dependent manner

Antimicrob Agents Chemother. 2019 Aug 23;63(9):e00996-19.

HEK293 cells

1 µM

NU6027 inhibited TRPC5-mediated currents, indicating a direct action on TRPC5 channels.

Mol Neurobiol. 2019 Apr;56(4):2822-2835.

NU6027 动物实验

Species Sprague-Dawley rats BALB/c mice Sprague-Dawley rats	Animal Model Traumatic brain injury (TBI) model Tuberculosis infection model KA-induced seizure model	Administration	Dosage	Frequency	Description	References
Sprague-Dawley rats	Traumatic brain injury (TBI) model	Intraperitoneal injection	1 mg/kg	Immediately injected once, continued for one week	NU6027 reduces TBI-induced neuronal death, zinc accumulation, oxidative stress, and glial activation by inhibiting TRPC5 channels and improves cognitive function	Int J Mol Sci. 2020 Nov 4;21(21):8256
BALB/c mice	Tuberculosis infection model	Oral	100 mg/kg	5 days a week for 4 weeks	NU-6027 inhibits M. tuberculosis growth in Mice tissues	Antimicrob Agents Chemother. 2019 Aug 23;63(9):e00996-19.
Sprague-Dawley rats	KA-induced seizure model	Intraperitoneal injection	100 μg/kg	Single dose, observed for 24 hours	NU6027 significantly reduced mortality and neuronal death in KA-induced epileptic rats.	Mol Neurobiol. 2019 Apr;56(4):2822-2835.

Species

Sprague-Dawley rats BALB/c mice Sprague-Dawley rats

Animal Model

Traumatic brain injury (TBI) model Tuberculosis infection model KA-induced seizure model

Administration

Dosage

Frequency

Description

References

Sprague-Dawley rats

Traumatic brain injury (TBI) model

Intraperitoneal injection

1 mg/kg

Immediately injected once, continued for one week

NU6027 reduces TBI-induced neuronal death, zinc accumulation, oxidative stress, and glial activation by inhibiting TRPC5 channels and improves cognitive function

Int J Mol Sci. 2020 Nov 4;21(21):8256

BALB/c mice

Tuberculosis infection model

Oral

100 mg/kg

5 days a week for 4 weeks

NU-6027 inhibits M. tuberculosis growth in Mice tissues

Antimicrob Agents Chemother. 2019 Aug 23;63(9):e00996-19.

Sprague-Dawley rats

KA-induced seizure model

Intraperitoneal injection

100 μg/kg

Single dose, observed for 24 hours

NU6027 significantly reduced mortality and neuronal death in KA-induced epileptic rats.

Mol Neurobiol. 2019 Apr;56(4):2822-2835.

NU6027 参考文献

NU6027 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.98mL

0.80mL

0.40mL

19.90mL

3.98mL

1.99mL

39.79mL

7.96mL

3.98mL

NU6027 技术信息

CAS号	220036-08-8
分子式	C₁₁H₁₇N₅O₂
分子量	251.29
SMILES Code	NC1=NC(OCC2CCCCC2)=C(N=O)C(N)=N1
MDL No.	MFCD05664735

别名
运输	蓝冰
InChI Key	DGWXOLHKVGDQLN-UHFFFAOYSA-N
Pubchem ID	398148

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 12 mg/mL(47.75 mM)，配合低频超声，并水浴加热至45℃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：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

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