I-BET151 | GSK1210151A | BRD2/3/4 Inhibitor | AmBeed-信号通路专用抑制剂

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I-BET151 98%

货号：A111934 同义名： GSK1210151A

I-BET-151 is a selective BET inhibitor for BRD2, BRD3 and BRD4 with IC50 of 0.5 μM, 0.25 μM, and 0.79 μM in cell-free assays, respectively.

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I-BET151 化学结构
CAS号：1300031-49-5

I-BET151 3D分子结构
CAS号：1300031-49-5

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I-BET151 纯度/质量文件产品仅供科研

货号：A111934 标准纯度： 98% 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: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

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						99+%
GSK1324726A	+++ BRD2, IC50: 31 nM BRD4, IC50: 22 nM						99%+
PFI-1	++ BRD2, IC50: 98 nM BRD4, IC50: 0.22 μM						98%
Apabetalone	+ BD2, IC50: 0.51 μM						99%
(+)-JQ1	+++ BRD4 (1), IC50: 77 nM BRD4 (2), IC50: 33 nM						98%
I-BET151	+ BRD3, IC50: 0.25 μM BRD4, IC50: 0.5 μM						98%
Molibresib	+++ BET proteins, IC50: 35 nM						99%+
I-BRD9	+++ BRD9, pIC50: 7.3 BRD4, pIC50: 5.3						99%+
BI-7273	++++ BRD7, IC50: 117 nM BRD9, IC50: 19 nM						99+%
Pelabresib	+++ BRD4-BD1, IC50: 39 nM						98%
ARV-825	+++ BRD4 BD1, Kd: 90 nM BRD4 BD2, Kd: 28 nM						99%+
Birabresib							99%+
BI 2536	+++ BRD4, Kd: 37 nM					c-Myc	99%+
Bromosporine	++ BRD2, IC50: 0.29 μM BRD9, IC50: 0.122 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	++++ BRD3 BD1, Kd: 2.1 nM BRD4 BD2, Kd: 1.7 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-BD1, IC50: 5 nM BRD4-BD2, IC50: 41 nM						97%
A1874	✔						99%+
Y06036	++ BRD4 (1), Kd: 82 nM						99%+
Alobresib	✔					NF-κB	98%
ODM-207	✔						99%
GSK778	+++ BRD2-BD1, IC50: 75nM BRD4-BD1, IC50: 143 nM						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%
Thalidomide-NH-C4-NH-Boc	✔						98%
Trotabresib	✔						99%
NHWD-870	✔						98%
CFT8634	++++ BRD9, DC50: 3 nM						98%
GSK2801		++ BAZ2A, Kd: 257 nM BAZ2B, Kd: 136 nM					99%+
KG-501		✔					99%+
UNC 669		+ L3MBTL4, IC50: 6 μM L3MBTL3, IC50: 35 μM					98%
PFI-3		+++ SMARCA2A, Kd: 72 nM SMARCA4, Kd: 55 nM					99%+
UNC1215		+++ L3MBTL3- D274A, IC50: 3.5 μM L3MBTL3, IC50: 120 nM					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			++ BRPF2, Kd: 500 nM BRPF1B, Kd: 100 nM				99%+
GSK-5959			++ BRPF3, pIC50: 7.1 BRPF2, pIC50: 5.2				99%
GSK6853			++++ BRPF1, pIC50: 8.1				99%+
NI-42			++++ BRPF1, IC50: 48 nM BRPF3, IC50: 260 nM				99%+
E-7386				+++ CBP/beta-catenin, IC50: 0.0484 μM			97%
I-CBP112					++ CBP, Kd: 151 nM p300, Kd: 167 nM		98+%
Histone Acetyltransferase Inhibitor II					+ p300, IC50: 5 μM		98%
C646					+ p300/CBP, Ki: 400 nM		99%+
Anacardic Acid					+ PCAF, IC50: 5 μM p300/CBP, IC50: 8.5 μM		99%+
SGC-CBP30					++++ EP300, IC50: 38 nM CREBBP, IC50: 21 nM		99%+
Nordihydroguaiaretic acid					✔	HER2,IGF-1R	99%+
Curcumin					+ p300, IC50: ~25 μM	Nrf2,Ferroptosis,NF-κB	98%
PF-CBP1 HCl					++ p300/CBP, IC50: 363nM CREBBP, IC50: 125nM		97%
CPI-637					+++ CBP, IC50: 0.03 μM EP300, IC50: 0.051 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		98%
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。

I-BET151 生物活性

靶点	BET BRD3, IC50:0.25 μM BRD4, IC50:0.5 μM
描述	The Bromodomain and Extra-Terminal Domain BET (Bromodomain and Extra-Terminal Domain) family is characterized by the presence of two tandem bromodomains and an extra-terminal domain. BET proteins can govern the assembly of histone acetylation-dependent chromatin complexes, thus regulating gene expression. I-BET-151 is a potent BET protein inhibitor with IC50 values of 0.5, 0.25 and 0.79 μM for BRD2, BRD3 and BRD4 (measure by FP ligand displacement assay), respectively. I-BET-151 shows more potential and selective effect on growth inhibition of MLL-fusion leukemic cell lines with IC50 values of 15 - 192 nM for MV4-11, RS4-11, MOLM13 and NOMO1 cell lines. Treatment with I-BET-151 for 72h cause a marked induction of apoptosis and a prominent G0/G1 arrest in MOLM13 and MV4-11 cells. This may due to the ability of I-BET-151 to inhibit the transcription of MLL targeted gene such as BCL2, CDK6 or MYC, which regulated by aberrantly co-opted SEC and PAFc in MLL fusions. Treatment with I-BET-151 at dose of 30mg/kg, i.p., daily, for 21 days can provide excellent control of MLL leukemia progression in xenotransplanted model of disseminated human MLL–AF4 leukemia and syngeneic model of murine MLL–AF9 leukemia. Compared with I-BET-762 or JQ1, I-BET-151 showed enhanced in vivo pharmacokinetics and terminal half-life to enable prolonged in vivo studies^[1]. I-BET151 has anti-tumor activity in hematological malignancies, including myeloma^[2], acute myeloid leukemia^[3], lymphoma^[4] and myeloproliferative neoplasms^[5]. Similar with I-BET-762, I-BET-151 can effectively inhibit IL-6 production in LPS-stimulated PMBCs^[6], as well as osteoclast genesis and inflammatory bone resorption^[7].
作用机制	I-BET-151 can bind to the acetylated-lysine (AcK) recognition pocket of the BET protein and inhibit the transcription activity of key gene through the displacement of BRD3/4, PAFc and SEC components from chromatin^[1].

I-BET151 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
A172	~10 μM	Function assay		reduces cellular ATP with IC50 of 1.28 μM	24496381
A2	~10 μM	Function assay		reactivates latent HIV-1	23255218
A72	~10 μM	Function assay		reactivates latent HIV-1	23255218
BC1	~1 μM	Growth inhibitory assay		IC50=220 nM	23792448

I-BET151 动物研究

Dose

Rat^[8] (p.o.): 2 mg/kg, 10 mg/kg, mice^[8] (p.o.): 50 mg/kg

Administration

p.o.

Pharmacokinetics

Animal	Mice^[1]	Rats^[1]	Dogs^[1]
Dose	i.v. p.o.	i.v. p.o.	i.v. p.o.
Administration	3 mg/kg 3 mg/kg	1 mg/kg 2 mg/kg	1 mg/kg 3 mg/kg
C_max	3.87 ± 1.03 μM (p.o.)	0.72 ± 0.24 μM (p.o.)	0.09 ± <0.1 μM (p.o.)
T_1/2	1.8 ± 0.3 h (i.v.) 2.6 ± 0.3 h (p.o.)	1.7 ± 0.3 h (i.v.) 2.1 ± 0.3 h (p.o.)	1.2 ± 0.1 h (i.v.) 4.7 h, 2.2 h (p.o.)
F	1	66 ± 26%	16 ± 3%
AUC_last	15.0 ± 1.5 μM/h (i.v.) 18.2 ± 4.9 μM/h (p.o.)	2.3 ± 0.5 μM/h (i.v.) 2.8 ± 1.1 μM/h (p.o.)	1.1 ± 0.3 μM/h (i.v.) 0.5 ± 0.2 μM/h (p.o.)
T_max	1.02 h (p.o.)	0.75 h (p.o.)	2 h (p.o.)
Vss	1.2 ± 0.1 l/kg (i.v.)	2.1 ± 0.1 l/kg (i.v.)	3.0 ± 0.6 l/kg (i.v.)
AUC_∞	15.3 ± 2.3 μM/h (i.v.) 19.1 ± 4.8 μM/h (p.o.)	2.4 ± 0.6 μM/h (i.v.) 2.9 ± 1.2 μM/h (p.o.)	1.2 ± 0.3 μM/h (i.v.) 0.8, 0.3 μM/h (p.o.)
CL	8 ± 1 ml/min/kg (i.v.)	18 ± 5 ml/min/kg (i.v.)	38 ± 10 ml/min/kg (i.v.)
MRT	2.5 ± 0.2 h (i.v.)	2.1 ± 0.5 h (i.v.)	1.3 ± 0.1 h (i.v.)

I-BET151 参考文献

[1]Dawson MA, Prinjha RK, et al. Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. Nature. 2011 Oct 2;478(7370):529-33.

[2]Chaidos A, Caputo V, et al. Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762. Blood. 2014 Jan 30;123(5):697-705.

[3]Dawson MA, Gudgin EJ, et al. Recurrent mutations, including NPM1c, activate a BRD4-dependent core transcriptional program in acute myeloid leukemia. Leukemia. 2014 Feb;28(2):311-20.

[4]Tolani B, Gopalakrishnan R, et al. Targeting Myc in KSHV-associated primary effusion lymphoma with BET bromodomain inhibitors. Oncogene. 2014 May 29;33(22):2928-37.

[5]Wyspiańska BS, Bannister AJ, et al. BET protein inhibition shows efficacy against JAK2V617F-driven neoplasms. Leukemia. 2014 Jan;28(1):88-97.

[6]Seal J, Lamotte Y, et al. Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A). Bioorg Med Chem Lett. 2012 Apr 15;22(8):2968-72.

[7]Park-Min KH, Lim E, et al. Inhibition of osteoclastogenesis and inflammatory bone resorption by targeting BET proteins and epigenetic regulation. Nat Commun. 2014 Nov 13;5:5418.

[8]Piquereau J, Boet A, et al. The BET Bromodomain Inhibitor I-BET-151 Induces Structural and Functional Alterations of the Heart Mitochondria in Healthy Male Mice and Rats. Int J Mol Sci. 2019 Mar 27;20(7). pii: E1527.

I-BET151 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.41mL

0.48mL

0.24mL

12.04mL

2.41mL

1.20mL

24.07mL

4.81mL

2.41mL

I-BET151 技术信息

CAS号	1300031-49-5
分子式	C₂₃H₂₁N₅O₃
分子量	415.445

别名	GSK1210151A
运输	蓝冰

存储条件

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(252.74 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

动物实验配方

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

A172	~10 μM	Function assay	reduces cellular ATP with IC50 of 1.28 μM	24496381
A2	~10 μM	Function assay	reactivates latent HIV-1	23255218
A72	~10 μM	Function assay	reactivates latent HIV-1	23255218
BC1	~1 μM	Growth inhibitory assay	IC50=220 nM	23792448
BC1	500 nM	Function assay	induces cell-cycle arrest	23792448
BC1	800 nM	Function assay	reduces c-Myc protein levels	23792448
BC3	~1 μM	Growth inhibitory assay	IC50=460 nM	23792448
BC3	500 nM	Function assay	induces cell-cycle arrest	23792448
BC3	800 nM	Function assay	reduces c-Myc protein levels	23792448
BCBL1	~1 μM	Growth inhibitory assay	IC50=330 nM	23792448
BJAB	~1 μM	Growth inhibitory assay	IC50=970 nM	23792448
H929	~1 μM	Function assay	induces cell cycle arrest	24335499
H929	~1 μM	Apoptosis assay	induces cell apoptosis	24335499
HEL	~100 μM	cytotoxicity assay	IC50=1 μM	21964340
HL60	~100 μM	cytotoxicity assay	IC50=890 nM	21964340
Jurkat	~1 μM	Growth inhibitory assay	IC50=1220 nM	23792448
K562	~100 μM	cytotoxicity assay	IC50>100 μM	21964340
KMS11	~1 μM	Function assay	induces cell cycle arrest	24335499
KMS11	~1 μM	Apoptosis assay	induces cell apoptosis	24335499
KMS12BM	~1 μM	Function assay	induces cell cycle arrest	24335499
KMS12BM	~1 μM	Apoptosis assay	induces cell apoptosis	24335499
KMS12PE	~1 μM	Function assay	induces cell cycle arrest	24335499
KMS12PE	~1 μM	Apoptosis assay	induces cell apoptosis	24335499
KMS18	~1 μM	Function assay	induces cell cycle arrest	24335499
KMS18	~1 μM	Apoptosis assay	induces cell apoptosis	24335499
Me007	~100 μM	Growth inhibitory assay	inhibits the growth	24906137
Me007	~100 μM	Apoptosis assay	induces apoptosis	24906137
Me007	10 μM	Function assay	induces cell cycle arrest by upregulation of p21	24906137
Me007	10 μM	Function assay	upregulates proapoptotic and cell cycle arrest genes	24906137
MEG01	~100 μM	cytotoxicity assay	IC50=25 μM	21964340
Mel-JD	~100 μM	Growth inhibitory assay	inhibits the growth	24906137
Mel-JD	~100 μM	Apoptosis assay	induces apoptosis	24906137
Mel-JD	10 μM	Function assay	induces cell cycle arrest by upregulation of p21	24906137
Mel-JD	10 μM	Function assay	upregulates proapoptotic and cell cycle arrest genes	24906137
Mel-RM	~100 μM	Growth inhibitory assay	inhibits the growth	24906137
Mel-RM	~100 μM	Apoptosis assay	induces apoptosis	24906137
Mel-RM	10 μM	Function assay	induces cell cycle arrest by upregulation of p21	24906137
Mel-RM	10 μM	Function assay	upregulates proapoptotic and cell cycle arrest genes	24906137
Mel-RMU	~100 μM	Growth inhibitory assay	inhibits the growth	24906137
Mel-RMU	~100 μM	Apoptosis assay	induces apoptosis	24906137
Mel-RMU	10 μM	Function assay	induces cell cycle arrest by upregulation of p21	24906137
Mel-RMU	10 μM	Function assay	upregulates proapoptotic and cell cycle arrest genes	24906137
MM1S	~1 μM	Growth inhibitory assay	IC50=760 nM	23792448
MOLM13	~100 μM	cytotoxicity assay	IC50=120 nM	21964340
MOLM13	~100 μM	Apoptosis assay	induces apoptosis	21964340
MV4;11	~100 μM	cytotoxicity assay	IC50=26 nM	21964340
MV4;11	~100 μM	Apoptosis assay	induces apoptosis	21964340
MV4;11		Function assay	decreases the recruitment of BRD3/4 and impaired recruitment of CDK9 and PAF1 to the transcriptional start site	21964340
Namalwa	~1 μM	Growth inhibitory assay	IC50=970 nM	23792448
NOMO1	~100 μM	cytotoxicity assay	IC50=15 nM	21964340
PBMC		Function assay	inhibits IL-6 with pIC50 of 6.7	22437115
RAW267.4	1 μM	Function assay	reduces IL-6 production induced by LPS	24859008
RAW267.4	1 μM	Function assay	reduces the association between BRD4 and acetylated p65	24859008
RPMI8226	~1 μM	Function assay	induces cell cycle arrest	24335499
RPMI8226	~1 μM	Apoptosis assay	induces cell apoptosis	24335499
RS4;11	~100 μM	cytotoxicity assay	IC50=192 nM	21964340
SK-Mel-28	~100 μM	Growth inhibitory assay	inhibits the growth	24906137
SK-Mel-28	~100 μM	Apoptosis assay	induces apoptosis	24906137
SK-Mel-28	10 μM	Function assay	induces cell cycle arrest by upregulation of p21	24906137
SK-Mel-28	10 μM	Function assay	upregulates proapoptotic and cell cycle arrest genes	24906137
SW1783	~10 μM	Function assay	reduces cellular ATP with IC50 of 2.68 μM	24496381
U266	~1 μM	Growth inhibitory assay	IC50=950 nM	23792448
U87MG	~10 μM	Function assay	reduces U87MG cellular ATP with IC50 of 1.05 μM	24496381
U87MG	~10 μM	Function assay	increases proportion of cells in the G1/S transition	24496381
UM-PEL-1	~1 μM	Growth inhibitory assay	IC50=210 nM	23792448
UM-PEL-3	~1 μM	Growth inhibitory assay	IC50=180 nM	23792448

I-BET151 98%

I-BET151 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

I-BET151 质控信息

I-BET151 生物活性

I-BET151 细胞研究

I-BET151 动物研究

I-BET151 参考文献

I-BET151 实验方案

I-BET151 技术信息

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I-BET151 98%

I-BET151 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

I-BET151 质控信息

I-BET151 生物活性

I-BET151 细胞研究

I-BET151 动物研究

I-BET151 参考文献

I-BET151 实验方案

I-BET151 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

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I-BET151 纯度/质量文件产品仅供科研