I-BRD9 | GSK602 | Chemical Probe | AmBeed-信号通路专用抑制剂

I-BRD9 {[allProObj[0].p_purity_real_show]}

货号：A178532 同义名： GSK602

I-BRD9是一种BRD9溴结构域抑制剂，pIC50值为7.3，pKd为8.7。BRD9作为SWI/SNF复合物的一部分，参与染色质重塑。

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I-BRD9 化学结构
CAS号：1714146-59-4

I-BRD9 3D分子结构
CAS号：1714146-59-4

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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 (1), Ki: <0.085 μM BRD4 (2), Ki: 0.34 μM						99%+
CPI-203	+++ BRD4, IC50: 37 nM						98+%
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 (2), IC50: 33 nM BRD4 (1), IC50: 77 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						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	++++ BRD7, Kd: 73 nM BRD9, Kd: 5.9 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	95%
ODM-207	✔						98%
GSK778	+++ BRD2-BD1, IC50: 75nM BRD4-BD1, IC50: 143 nM						97%
SRX3207	+ BRD41, IC50: 3070 nM BRD42, IC50: 3070 nM					Syk	98%
GSK046	+++ BRD3_BD2, IC50: 98 nM BRD4_BD2, IC50: 214 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- 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			++ BRPF1, IC50: 80 nM BRPF2, IC50: 7.9 μM				99%+
OF-1			++ BRPF2, Kd: 500 nM BRPF1B, Kd: 100 nM				99%+
GSK-5959			++ BRPF2, pIC50: 5.2 BRPF3, pIC50: 7.1				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					++ 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					+ p300/CBP, IC50: 8.5 μM PCAF, IC50: 5 μM		99%+
SGC-CBP30					++++ CREBBP, IC50: 21 nM EP300, IC50: 38 nM		99%+
Nordihydroguaiaretic acid					✔	HER2,IGF-1R	99%+
Curcumin					+ p300, IC50: ~25 μM	Ferroptosis,Nrf2,NF-κB	98%
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		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。

I-BRD9 生物活性

靶点

BET

BRD9, pIC50:7.3

BRD4, pIC50:5.3

描述

BRD9 (Bromodomain Containing 9) plays a role in chromatin remodeling and regulation of transcription. It acts as a chromatin reader that recognizes and binds acylated histones. BRD9 is also component of SWI/SNF chromatin remodeling subcomplex GBAF that carries out key enzymatic activities, changing chromatin structure by altering DNA-histone contacts within a nucleosome in an ATP-dependent manner^[2]. I-BRD9 is a selective BRD9 inhibitor. According to data obtained by TR-FRET assays, the pIC50s of I-BRD9 against BRD9 and BRD4 were 7.3 and 5.3, respectively, suggesting 100-fold selectivity for BRD9. A nanoBRET assay revealed that the pIC50 of I-BRD9 agianst BRD9 was 6.8. In a BROMOscan profiling against 34 bromodomains, the pKd of I-BRD9 binding BRD9 was 8.7 and good selectivity over other bromodomians was revealed^[3]. According data obtained by MTT cytotoxicity assays, the inhibitory IC50s of I-BRD9 against cell proliferation of Rhabdoid tumor cell lines BT12, BT16, Chla266, G401 and KD were 21.2 μM, 11.2 μM, 13.3 μM, 13.4 μM and 8.1 μM, respectively^[4]. Kasumi-1 cells were treated by 10 μM I-BRD9 for 6h and results obtained by qPCR assays suggested that I-BRD9 suppressed the genes of CLEC1, DUSP6, FES and SAMSN1^[3].

I-BRD9 细胞实验

Cell Line KD G401 Chla266 BT16 BT12 U2OS OVCAR8 Kasumi-1 cells UTSM cells HuLM cells Leishmania donovani promastigotes	Concentration	Treated Time	Description	References
KD	8.1 µM, 7.1 µM	72h and 144h	Evaluate the effect of I-BRD9 on KD cell proliferation, IC50 values decreased over time	Int J Mol Sci. 2017 Jul 16;18(7):1537.
G401	13.4 µM, 6.1 µM	72h and 144h	Evaluate the effect of I-BRD9 on G401 cell proliferation, IC50 values decreased over time	Int J Mol Sci. 2017 Jul 16;18(7):1537.
Chla266	13.3 µM, 24.7 µM	72h and 144h	Evaluate the effect of I-BRD9 on Chla266 cell proliferation, IC50 values varied over time	Int J Mol Sci. 2017 Jul 16;18(7):1537.
BT16	11.2 µM	72h	Evaluate the effect of I-BRD9 on BT16 cell proliferation, IC50 value was 11.2 µM	Int J Mol Sci. 2017 Jul 16;18(7):1537.
BT12	21.2 µM, 8.2 µM	72h and 144h	Evaluate the effect of I-BRD9 on BT12 cell proliferation, showing decreased IC50 over time	Int J Mol Sci. 2017 Jul 16;18(7):1537.
U2OS	10 or 20 µM	36 h	To evaluate the effect of I-BRD9 on HR activity. Results showed that I-BRD9 significantly inhibited HR activity.	Nat Commun. 2020 May 26;11(1):2639.
OVCAR8	10 or 20 µM	36 h	To evaluate the effect of I-BRD9 on HR and NHEJ activity. Results showed that I-BRD9 significantly inhibited HR activity but had no significant effect on NHEJ activity.	Nat Commun. 2020 May 26;11(1):2639.
Kasumi-1 cells	10 μM	6 h	Identify genes selectively regulated by BRD9 bromodomain inhibition, involved in oncology and immune response pathways	J Med Chem. 2016 Feb 25;59(4):1425-39.
UTSM cells	5-25 µM	48 h	Evaluate the effect of I-BRD9 on UTSM cell proliferation, showing dose-dependent inhibition of cell proliferation	Int J Mol Sci. 2024 Jan 11;25(2):905.
HuLM cells	1-25 µM	48 h	Evaluate the effect of I-BRD9 on HuLM cell proliferation, showing dose-dependent inhibition of cell proliferation	Int J Mol Sci. 2024 Jan 11;25(2):905.
Leishmania donovani promastigotes	0-30 μM	5 days	To evaluate the effect of I-BRD9 on the cell viability of Leishmania donovani promastigotes. Results showed that I-BRD9 had minimal inhibitory activity on promastigote growth at concentrations up to 30 μM.	ACS Infect Dis. 2023 Nov 10;9(11):2340-2357.

Cell Line

Concentration

Treated Time

Description

References

8.1 µM, 7.1 µM

72h and 144h

Evaluate the effect of I-BRD9 on KD cell proliferation, IC50 values decreased over time