GSK2801 | BAZ2A/B Inhibitor | AmBeed-信号通路专用抑制剂

GSK2801 {[allProObj[0].p_purity_real_show]}

货号：A884058

GSK2801抑制BAZ2家族的溴结构域蛋白，包括BAZ2A（Kd = 260 nM）和BAZ2B（Kd= 140 nM，IC50 = 9-350 nM）。

GSK2801 化学结构
CAS号：1619994-68-1

GSK2801 3D分子结构
CAS号：1619994-68-1

规格	价格	会员价	库存	数量
{[ item.pr_size ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]}	现货	1周咨询	- +

购物车0 收藏询单

sales@ambeed.cn tech@ambeed.cn 400-920-2911 产品手册产品订购技术咨询
快速发货顺丰冷链运输，1-2 天到达

品质保证

技术支持

免费溶解

表观遗传阅读框亚型比较

产品名称	BET ↓ ↑	bromodomain ↓ ↑	BRPF ↓ ↑	CBP/beta-catenin ↓ ↑	p300/CBP ↓ ↑	其他靶点	纯度
MS436	++ BRD4 (2), Ki: 0.34 μM BRD4 (1), Ki: <0.085 μM						99%+
CPI-203	+++ BRD4, IC50: 37 nM						98+%
GSK1324726A	+++ BRD4, IC50: 22 nM BRD2, IC50: 31 nM						99%+
PFI-1	++ BRD4, IC50: 0.22 μM BRD2, IC50: 98 nM						98%
Apabetalone	+ BD2, IC50: 0.51 μM						99%
(+)-JQ1	+++ BRD4 (1), IC50: 77 nM BRD4 (2), IC50: 33 nM						98%
I-BET151	+ BRD4, IC50: 0.5 μM BRD3, IC50: 0.25 μM						98%
Molibresib	+++ BET proteins, IC50: 35 nM						99%+
I-BRD9	+++ BRD4, pIC50: 5.3 BRD9, pIC50: 7.3						99%+
BI-7273	++++ BRD7, IC50: 117 nM BRD9, IC50: 19 nM						97%
Pelabresib	+++ BRD4-BD1, IC50: 39 nM						98%
ARV-825	+++ BRD4 BD2, Kd: 28 nM BRD4 BD1, Kd: 90 nM						99%+
Birabresib							99%+
BI 2536	+++ BRD4, Kd: 37 nM					c-Myc	99%+
Bromosporine	++ BRD9, IC50: 0.122 μM BRD2, IC50: 0.29 μM	++++ CECR2, IC50: 17 nM					99%+
XMD8-92	++ BRD4 (1), Kd: 170 nM						99%+
Mivebresib	✔						99%+
BI-9564	++++ BRD9, Kd: 5.9 nM BRD7, Kd: 73 nM	++ CECR2, Kd: 77 nM					98%
AZD5153 6-Hydroxy-2-naphthoic acid	++++ FL-BRD4, IC50: 5 nM						99%+
PLX51107	++++ BRD4 BD2, Kd: 1.7 nM BRD3 BD1, Kd: 2.1 nM						99%+
FL-411	+ BRD4(1), IC50: 0.43 μM						99%+
ABBV-744	✔						99%+
dBET6	++++ BRD4, IC50: 14 nM						99%+
dBET1	++++ BRD4, IC50: 20 nM						99%+
MZ1	++++ Brd2(BD2), Kd: 62 nM Brd3(BD2), Kd: 13 nM						99%+
dBET57	+ BRD4_BD1, DC50: 500 nM						99%+
SF2523	+ BRD4, IC50: 241 nM					DNA-PK	99%+
INCB054329	++++ BRD4-BD1, IC50: 119 nM BRD3-BD1, IC50: 9 nM						99%
INCB-057643	✔						99%+
(E/Z)-ZL0420	+++ BRD4 BD1, IC50: 27 nM BRD4 BD2, IC50: 32 nM						99%+
BMS-986158	✔						99%
BRD4 Inhibitor-10	++++ BRD4-BD2, IC50: 41 nM BRD4-BD1, IC50: 5 nM						97%
A1874	✔						99%+
Y06036	++ BRD4 (1), Kd: 82 nM						99%+
Alobresib	✔					NF-κB	95%
ODM-207	✔						98%
GSK778	+++ BRD4-BD1, IC50: 143 nM BRD2-BD1, IC50: 75nM						97%
SRX3207	+ BRD41, IC50: 3070 nM BRD42, IC50: 3070 nM					Syk	98%
GSK046	+++ BRD4_BD2, IC50: 214 nM BRD3_BD2, IC50: 98 nM						98%
GSK620	✔						97%
Trotabresib	✔						99%
NHWD-870	✔						98%
CFT8634	++++ BRD9, DC50: 3 nM						98%
GSK2801		++ BAZ2B, Kd: 136 nM BAZ2A, Kd: 257 nM					99%+
KG-501		✔					99%+
UNC 669		+ L3MBTL3, IC50: 35 μM L3MBTL4, IC50: 6 μM					99%
PFI-3		+++ SMARCA2A, Kd: 72 nM SMARCA4, Kd: 55 nM					99%+
UNC1215		+++ L3MBTL3, IC50: 120 nM L3MBTL3- D274A, IC50: 3.5 μM					99%+
EED226		++ EED, Kd: 82 nM PRC2, Kd: 114 nM					99%+
BRD9539		✔					98%
UNC926		+ L3MBTL1, Kd: 3.9 μM					99%
666-15		++ CREB, IC50: 81 nM					99%+
UNC6852		+ EED, IC50: 247 nM					98%
BAZ1A-IN-1		+ BAZ1A, Kd: 0.52 μM					99%+
PFI-4			++ BRPF2, IC50: 7.9 μM BRPF1, IC50: 80 nM				99%+
OF-1			++ BRPF1B, Kd: 100 nM BRPF2, Kd: 500 nM				99%+
GSK-5959			++ BRPF3, pIC50: 7.1 BRPF2, pIC50: 5.2				99%
GSK6853			++++ BRPF1, pIC50: 8.1				99%+
NI-42			++++ BRPF3, IC50: 260 nM BRPF1, IC50: 48 nM				99%+
E-7386				+++ CBP/beta-catenin, IC50: 0.0484 μM			99%
I-CBP112					++ p300, Kd: 167 nM CBP, Kd: 151 nM		98+%
Histone Acetyltransferase Inhibitor II					+ p300, IC50: 5 μM		98%
C646					+ p300/CBP, Ki: 400 nM		99%+
Anacardic Acid					+ p300/CBP, IC50: 8.5 μM PCAF, IC50: 5 μM		99%+
SGC-CBP30					++++ CREBBP, IC50: 21 nM EP300, IC50: 38 nM		99%+
Nordihydroguaiaretic acid					✔	IGF-1R,HER2	99%+
Curcumin					+ p300, IC50: ~25 μM	Ferroptosis,Nrf2,NF-κB	98%
CPI-637					+++ EP300, IC50: 0.051 μM CBP, IC50: 0.03 μM		99%+
Foscenvivint					✔	β-catenin	99%+
A-485					++ p300 HAT, IC50: 0.06 μM		99%+
GNE-781	+ BRD4(1), IC50: 5100 nM				++++ CBP, IC50: 0.94 nM		99%
NEO2734	+++ BET, IC50: <30 nM				+++ p300/CBP, IC50: <30 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。

GSK2801 生物活性

靶点

bromodomain

BAZ2B, Kd:136 nM

BAZ2A, Kd:257 nM

描述

BAZ2A and BAZ2B are bromodomain-containing proteins that constitute the central scaffolding protein of the nucleolar remodeling complex (NoRC). GSK2801 is a potent, selective, cell-active inhibitor of BAZ2A and BAZ2B bromodomains. It binds to the BAZ2 bromodomains of BAZ2A and BAZ2B with K_D values of 257 and 136nM, respectively. GSK2801 at a concentration of 10μM led to a temperature shift of 4.1 and 2.7°C for BAZ2A and BAZ2B, respectively. An isothermal titration calorimetry binding experiment showed that GSK2801 bound to TAF1L(2) with a binding enthalpy change ΔH of −8.6(±0.02)kcal/mol and a K_D value of 3.2μM. A chemoproteomic competition binding assay showed that GSK2801 bound to endogenous BAZ2 proteins with a pK_d value of 5.5. In male CD1 mice, GSK2801 exhibited reasonable in vivo exposure, modest clearance, and reasonable plasma stability after an oral dosing of 30mg/kg (T_max=1.0h; C_max=435ng/mL; Terminal _t1/2=1.5h)^[2].

GSK2801 细胞实验

Cell Line HepaRG cells Huh7 cells Prostate cancer cell 22Rv1 Prostate cancer cell PC3 WHIM12 SUM-159 MDA-MB-231 HCC1806 8505C-PTX SW1736-PTX SUM-159 HCC-1806 MDA-MB-231	Concentration	Treated Time	Description	References
HepaRG cells	10 µM	8 days	Inhibition of HDV replication	Nat Commun. 2020 Jan 21;11(1):419.
Huh7 cells	10 µM		Inhibition of HDV replication	Nat Commun. 2020 Jan 21;11(1):419.
Prostate cancer cell 22Rv1	≥5μM		GSK2801 significantly reduced growth rate of 22Rv1 cells at the highest concentrations tested without affecting viability	Protein Sci. 2023 Sep;32(9):e4752.
Prostate cancer cell PC3	≥5μM		GSK2801 significantly reduced growth rate of PC3 cells at the highest concentrations tested without affecting viability	Protein Sci. 2023 Sep;32(9):e4752.
WHIM12	10 μM	96 hours	Evaluate the synergistic anti-proliferative effect of GSK2801 with BET inhibitor JQ1	Mol Cancer Res. 2019 Jul;17(7):1503-1518.
SUM-159	10 μM	96 hours	Evaluate the synergistic anti-proliferative effect of GSK2801 with BET inhibitor JQ1	Mol Cancer Res. 2019 Jul;17(7):1503-1518.
MDA-MB-231	10 μM	96 hours	Evaluate the synergistic anti-proliferative effect of GSK2801 with BET inhibitor JQ1	Mol Cancer Res. 2019 Jul;17(7):1503-1518.
HCC1806	10 μM	96 hours	Evaluate the synergistic anti-proliferative effect of GSK2801 with BET inhibitor JQ1	Mol Cancer Res. 2019 Jul;17(7):1503-1518.
8505C-PTX	20 μM	72 hours	Evaluate the effect of GSK2801 on cell viability, showing limited effect when used alone but significant decrease in cell viability when combined with paclitaxel	Int J Mol Sci. 2023 Mar 22;24(6):5993.
SW1736-PTX	20 μM	72 hours	Evaluate the effect of GSK2801 on cell viability, showing limited effect when used alone but significant decrease in cell viability when combined with paclitaxel	Int J Mol Sci. 2023 Mar 22;24(6):5993.
SUM-159	10 µM	72 hours	To evaluate the anti-proliferative activity of GSK2801 on SUM-159 cells, results showed limited efficacy when used alone but synergistic effects when combined with JQ1.	BMC Cancer. 2022 Jun 8;22(1):627.
HCC-1806	10 µM	72 hours	To evaluate the anti-proliferative activity of GSK2801 on HCC-1806 cells, results showed limited efficacy when used alone but synergistic effects when combined with JQ1.	BMC Cancer. 2022 Jun 8;22(1):627.
MDA-MB-231	10 µM	72 hours	To evaluate the anti-proliferative activity of GSK2801 on MDA-MB-231 cells, results showed limited efficacy when used alone but synergistic effects when combined with JQ1.	BMC Cancer. 2022 Jun 8;22(1):627.

Cell Line

Concentration

Treated Time

Description

References

HepaRG cells

10 µM

8 days

Inhibition of HDV replication

Nat Commun. 2020 Jan 21;11(1):419.

Huh7 cells

10 µM

Inhibition of HDV replication

Nat Commun. 2020 Jan 21;11(1):419.

Prostate cancer cell 22Rv1

≥5μM

GSK2801 significantly reduced growth rate of 22Rv1 cells at the highest concentrations tested without affecting viability

Protein Sci. 2023 Sep;32(9):e4752.

Prostate cancer cell PC3

≥5μM

GSK2801 significantly reduced growth rate of PC3 cells at the highest concentrations tested without affecting viability

Protein Sci. 2023 Sep;32(9):e4752.

WHIM12

10 μM

96 hours

Evaluate the synergistic anti-proliferative effect of GSK2801 with BET inhibitor JQ1

Mol Cancer Res. 2019 Jul;17(7):1503-1518.

SUM-159

10 μM

96 hours

Evaluate the synergistic anti-proliferative effect of GSK2801 with BET inhibitor JQ1

Mol Cancer Res. 2019 Jul;17(7):1503-1518.

MDA-MB-231

10 μM

96 hours

Evaluate the synergistic anti-proliferative effect of GSK2801 with BET inhibitor JQ1

Mol Cancer Res. 2019 Jul;17(7):1503-1518.

HCC1806

10 μM

96 hours

Evaluate the synergistic anti-proliferative effect of GSK2801 with BET inhibitor JQ1

Mol Cancer Res. 2019 Jul;17(7):1503-1518.

8505C-PTX

20 μM

72 hours

Evaluate the effect of GSK2801 on cell viability, showing limited effect when used alone but significant decrease in cell viability when combined with paclitaxel

Int J Mol Sci. 2023 Mar 22;24(6):5993.

SW1736-PTX

20 μM

72 hours

Evaluate the effect of GSK2801 on cell viability, showing limited effect when used alone but significant decrease in cell viability when combined with paclitaxel

Int J Mol Sci. 2023 Mar 22;24(6):5993.

SUM-159

10 µM

72 hours

To evaluate the anti-proliferative activity of GSK2801 on SUM-159 cells, results showed limited efficacy when used alone but synergistic effects when combined with JQ1.

BMC Cancer. 2022 Jun 8;22(1):627.

HCC-1806

10 µM

72 hours

To evaluate the anti-proliferative activity of GSK2801 on HCC-1806 cells, results showed limited efficacy when used alone but synergistic effects when combined with JQ1.

BMC Cancer. 2022 Jun 8;22(1):627.

MDA-MB-231

10 µM

72 hours

To evaluate the anti-proliferative activity of GSK2801 on MDA-MB-231 cells, results showed limited efficacy when used alone but synergistic effects when combined with JQ1.

BMC Cancer. 2022 Jun 8;22(1):627.

GSK2801 动物实验

Species CD1 mice	Animal Model	Administration	Dosage	Frequency	Description	References
CD1 mice		Oral and intraperitoneal	30 mg/kg		Assessed the pharmacokinetic properties of GSK2801 in mice. Results showed that GSK2801 had reasonable in vivo exposure after oral dosing, with modest clearance and reasonable plasma stability.	J Med Chem. 2016 Feb 25;59(4):1410-24

Species

CD1 mice

Animal Model

Administration

Dosage

Frequency

Description

References

CD1 mice

Oral and intraperitoneal

30 mg/kg

Assessed the pharmacokinetic properties of GSK2801 in mice. Results showed that GSK2801 had reasonable in vivo exposure after oral dosing, with modest clearance and reasonable plasma stability.

J Med Chem. 2016 Feb 25;59(4):1410-24

GSK2801 参考文献

GSK2801 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.69mL

0.54mL

0.27mL

13.46mL

2.69mL

1.35mL

26.92mL

5.38mL

2.69mL

GSK2801 技术信息

CAS号	1619994-68-1
分子式	C₂₀H₂₁NO₄S
分子量	371.45
SMILES Code	O=C(C)C1=CC(C2=C(S(=O)(C)=O)C=CC=C2)=C3N1C=CC(OCCC)=C3
MDL No.	MFCD26142953

别名
运输	蓝冰
InChI Key	KHWCPNJRJCNVRI-UHFFFAOYSA-N
Pubchem ID	73010930

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

细胞实验：

DMSO: 50 mg/mL(134.61 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：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

GSK2801 {[allProObj[0].p_purity_real_show]}

GSK2801 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

GSK2801 质控信息

GSK2801 生物活性

GSK2801 细胞实验

GSK2801 动物实验

GSK2801 参考文献

GSK2801 实验方案

GSK2801 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

GSK2801 {[allProObj[0].p_purity_real_show]}

GSK2801 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

GSK2801 质控信息

GSK2801 生物活性

GSK2801 细胞实验

GSK2801 动物实验

GSK2801 参考文献

GSK2801 实验方案

GSK2801 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

请登录您的专属账户

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

GSK2801 纯度/质量文件产品仅供科研