BS-181 HCl | BS-181 (hydrochloride) | CDK Inhibitor | AmBeed-信号通路专用抑制剂

BS-181 HCl {[allProObj[0].p_purity_real_show]}

货号：A750865 同义名： BS-181 (hydrochloride); BS-181 hydrochloride

BS-181 HCl是一种选择性的 CDK7 抑制剂，IC50 为 21 nM。

BS-181 HCl 化学结构
CAS号：1397219-81-6

BS-181 HCl 3D分子结构
CAS号：1397219-81-6

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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											SGK,ERK	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/CyclinA, IC50: 70 nM CDK2/CyclinE, IC50: 35 nM		+ CDK4/CyclinD1, IC50: 850 nM								99%+
SCH900776				++ CDK2, IC50: 0.16 μM										99%+
AUZ 454				++++ CDK2(C118L), Kd: 18.6 nM CDK2(A144C), Kd: 9.7 nM										99%+
A-674563 HCl				++ CDK2, Ki: 46 nM									PKA	99%
JNJ-7706621		++++ CDK1/CyclinB, IC50: 9 nM		++++ CDK2/CyclinA, IC50: 4 nM CDK2/CyclinE, IC50: 3 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/CyclinA, IC50: 8 nM CDK2/CyclinE, 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/CyclinA, IC50: 45 nM CDK2/CyclinE, IC50: 363 nM		++ CDK4/CyclinD1, IC50: 160 nM	+ CDK5/p35, IC50: 265 nM		++ CDK7/CyclinH, IC50: 150 nM					99%+
Kenpaullone		+ CDK1/CyclinB, IC50: 0.4μM		+ CDK2/CyclinA, IC50: 0.68μM CDK2/CyclinE, IC50: 7.5μM			+ CDK5/p35, IC50: 0.85μM							98%
SNS-032				+++ CDK2/CyclinA, IC50: 38 nM CDK2/CyclinE, IC50: 48 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/CyclinA, IC50: 0.7 μM CDK2/CyclinE, 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/CyclinA, IC50: 224 nM CDK2/CyclinE, IC50: 2.54 μM		++ 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												+++ mCLK4, IC50: 15 nM mCLK1, IC50: 200 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。

BS-181 HCl 生物活性

靶点

CDK7

CDK7, IC50:21 nM

描述

Cyclin-dependent kinases (CDKs) are a large group of serine/threonine protein kinases that have central roles in the cell cycle signaling pathway^[3]. CDK7, a member of the CDK family, can regulate transcription as part of the TFIIH basal transcription factor. BS-181 HCl inhibits cancer cell growth by inhibiting phosphorylation of CDK7 substrates, Ser5 in the RNA polymeraseII CTD. In vitro , the luciferase assay results showed that BS-181 inhibited CDK7 activity with an IC50 of 21 nM^[4]. The IC50s of BS-181 HCl in MKN28, SGC-7901, AGS and BGC823 cell lines were 17-22 μM, and the IC50 in RGM-1 cell line was 6.5μM^[5]. In vivo assay, tumor growth was significantly inhibited by BS-181 HCl in a dose-dependent manner. After intraperitoneal injection of BS-181 HCl to mice at the dose of 5mg / kg or 10mg / kg twice a day, the growth of tumor decreased by 25% and 50% respectively over a period of 14 days ^[4].

作用机制

BS-181 HCl is a highly selective CDK7 inhibitor by inhibiting phosphorylation of CDK7 substrates.

BS-181 HCl 细胞实验

Cell Line BGC823 Jurkat A3 Jurkat JT/Neo Jurkat JT/BCL-2 MCF-7 MCF-7 MH7A cells FLS cells HeLa cells A549 cells	Concentration	Treated Time	Description	References
BGC823	0 µM, 1 µM, 10 µM, 20 µM	12 hours, 24 hours, 48 hours, 72 hours	BS-181 significantly reduced the activity of CDK7 with downregulation of cyclin D1 and XIAP, inducing cell cycle arrest and apoptosis.	Drug Des Devel Ther. 2016 Mar 16;10:1181-9.
Jurkat A3	5, 10, 15, 20 µM	20 hours	BS-181 caused cytotoxicity and several apoptotic events, including TRAIL/DR4/DR5 upregulation, c-FLIP down-regulation, BID cleavage, BAK activation, ΔΨm loss, caspase-8/9/3 activation, and PARP cleavage.	Cancers (Basel). 2020 Dec 19;12(12):3845.
Jurkat JT/Neo	10, 15 µM	24 hours	BS-181 induced BAK activation and ΔΨm loss, with significant increases in BAK activation rates and ΔΨm loss in JT/Neo cells.	Cancers (Basel). 2020 Dec 19;12(12):3845.
Jurkat JT/BCL-2	10, 15 µM	24 hours	BS-181-induced BAK activation and ΔΨm loss were abrogated in JT/BCL-2 cells.	Cancers (Basel). 2020 Dec 19;12(12):3845.
MCF-7	25 µM	24 hours	BS-181 treatment led to an increase in G1 phase cells and induced apoptosis.	Cancer Res. 2009 Aug 1;69(15):6208-15.
MCF-7	50 µM	24 hours	BS-181 treatment led to an increase in G1 phase cells and induced apoptosis.	Cancer Res. 2009 Aug 1;69(15):6208-15.
MH7A cells	80 nM	24 hours	BS-181 significantly down-regulated the mRNA levels of IL-1β, IL-6, IL-8 and RANKL, suggesting inhibition of CDK7 by BS-181 effectively suppressed LPS-induced MH7A inflammation.	J Cell Mol Med. 2018 Feb;22(2):1292-1301.
FLS cells	80 nM	24 hours	BS-181 significantly down-regulated transcript levels of IL-1β, IL-6, IL-8 and RANKL in LPS-induced FLS cells, suggesting BS-181 effectively suppressed LPS-induced FLS cell inflammation.	J Cell Mol Med. 2018 Feb;22(2):1292-1301.
HeLa cells	1 µM, 3 µM, 5 µM, 10 µM, 20 µM	30 minutes	To test the effect of CDK7 inhibitors on in vitro transcription, results showed that compound 140 significantly inhibited transcription at low concentrations	Mol Cell Biol. 2014 Oct 1;34(19):3675-88.
A549 cells	0.05 µM, 0.1 µM, 0.3 µM, 0.5 µM, 1 µM	30 minutes	To test the effect of CDK7 inhibitors on in vitro transcription, results showed that compound 297 significantly inhibited transcription at low concentrations	Mol Cell Biol. 2014 Oct 1;34(19):3675-88.

Cell Line

Concentration

Treated Time

Description

References

BGC823

0 µM, 1 µM, 10 µM, 20 µM

12 hours, 24 hours, 48 hours, 72 hours

BS-181 significantly reduced the activity of CDK7 with downregulation of cyclin D1 and XIAP, inducing cell cycle arrest and apoptosis.

Drug Des Devel Ther. 2016 Mar 16;10:1181-9.

Jurkat A3

5, 10, 15, 20 µM

20 hours

BS-181 caused cytotoxicity and several apoptotic events, including TRAIL/DR4/DR5 upregulation, c-FLIP down-regulation, BID cleavage, BAK activation, ΔΨm loss, caspase-8/9/3 activation, and PARP cleavage.

Cancers (Basel). 2020 Dec 19;12(12):3845.

Jurkat JT/Neo

10, 15 µM

24 hours

BS-181 induced BAK activation and ΔΨm loss, with significant increases in BAK activation rates and ΔΨm loss in JT/Neo cells.

Cancers (Basel). 2020 Dec 19;12(12):3845.

Jurkat JT/BCL-2

10, 15 µM

24 hours

BS-181-induced BAK activation and ΔΨm loss were abrogated in JT/BCL-2 cells.

Cancers (Basel). 2020 Dec 19;12(12):3845.

MCF-7

25 µM

24 hours

BS-181 treatment led to an increase in G1 phase cells and induced apoptosis.

Cancer Res. 2009 Aug 1;69(15):6208-15.

MCF-7

50 µM

24 hours

BS-181 treatment led to an increase in G1 phase cells and induced apoptosis.

Cancer Res. 2009 Aug 1;69(15):6208-15.

MH7A cells

80 nM

24 hours

BS-181 significantly down-regulated the mRNA levels of IL-1β, IL-6, IL-8 and RANKL, suggesting inhibition of CDK7 by BS-181 effectively suppressed LPS-induced MH7A inflammation.

J Cell Mol Med. 2018 Feb;22(2):1292-1301.

FLS cells

80 nM

24 hours

BS-181 significantly down-regulated transcript levels of IL-1β, IL-6, IL-8 and RANKL in LPS-induced FLS cells, suggesting BS-181 effectively suppressed LPS-induced FLS cell inflammation.

J Cell Mol Med. 2018 Feb;22(2):1292-1301.

HeLa cells

1 µM, 3 µM, 5 µM, 10 µM, 20 µM

30 minutes

To test the effect of CDK7 inhibitors on in vitro transcription, results showed that compound 140 significantly inhibited transcription at low concentrations

Mol Cell Biol. 2014 Oct 1;34(19):3675-88.

A549 cells

0.05 µM, 0.1 µM, 0.3 µM, 0.5 µM, 1 µM

30 minutes

To test the effect of CDK7 inhibitors on in vitro transcription, results showed that compound 297 significantly inhibited transcription at low concentrations

Mol Cell Biol. 2014 Oct 1;34(19):3675-88.

BS-181 HCl 动物实验

Species BALB/c-nu mice Nude mice	Animal Model Human gastric cancer xenograft model MCF-7 human xenograft model	Administration	Dosage	Frequency	Description	References
BALB/c-nu mice	Human gastric cancer xenograft model	Intraperitoneal injection	10 mg/kg/d, 20 mg/kg/d	Twice daily for 14 days	BS-181 significantly inhibited tumor growth and increased survival rate.	Drug Des Devel Ther. 2016 Mar 16;10:1181-9.
Nude mice	MCF-7 human xenograft model	Intraperitoneal injection	10 mg/kg/day and 20 mg/kg/day	Twice daily for 14 days	BS-181 significantly inhibited the growth of MCF-7 tumors with no apparent toxicity.	Cancer Res. 2009 Aug 1;69(15):6208-15.

Species

BALB/c-nu mice Nude mice

Animal Model

Human gastric cancer xenograft model MCF-7 human xenograft model

Administration

Dosage

Frequency

Description

References

BALB/c-nu mice

Human gastric cancer xenograft model

Intraperitoneal injection

10 mg/kg/d, 20 mg/kg/d

Twice daily for 14 days

BS-181 significantly inhibited tumor growth and increased survival rate.

Drug Des Devel Ther. 2016 Mar 16;10:1181-9.

Nude mice

MCF-7 human xenograft model

Intraperitoneal injection

10 mg/kg/day and 20 mg/kg/day

Twice daily for 14 days

BS-181 significantly inhibited the growth of MCF-7 tumors with no apparent toxicity.

Cancer Res. 2009 Aug 1;69(15):6208-15.

BS-181 HCl 参考文献

BS-181 HCl 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.40mL

0.48mL

0.24mL

11.99mL

2.40mL

1.20mL

23.98mL

4.80mL

2.40mL

BS-181 HCl 技术信息

CAS号	1397219-81-6
分子式	C₂₂H₃₃ClN₆
分子量	416.99
SMILES Code	CC(C1=C2N=C(NCCCCCCN)C=C(NCC3=CC=CC=C3)N2N=C1)C.[H]Cl
MDL No.	MFCD18384975

别名	BS-181 (hydrochloride); BS-181 hydrochloride
运输	蓝冰
InChI Key	NVIJWMOQODWNFN-UHFFFAOYSA-N
Pubchem ID	49867928

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案

细胞实验：

DMSO: 50 mg/mL(119.91 mM)，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

H₂O: 100 mg/mL(239.81 mM)，配合低频超声助溶

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

方案三

配制的工作液建议现用现配，短期内尽快用完。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

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