CPI-637 | CBP/EP300 Inhibitor | AmBeed-信号通路专用抑制剂

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CPI-637 {[allProObj[0].p_purity_real_show]}

货号：A788310

CPI-637是一种有效的CBP/EP300溴域抑制剂，IC50为0.03 ± 0.01 μM。

CPI-637 化学结构
CAS号：1884712-47-3

CPI-637 3D分子结构
CAS号：1884712-47-3

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CPI-637 纯度/质量文件产品仅供科研

货号：A788310 标准纯度： {[allProObj[0].p_purity_real_show]} 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: • Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]; • Cell, 2025. Ambeed. [ A122167 ]; • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]; • Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]; 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 (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	+++ 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	++ 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	++++ 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	++++ BRD3-BD1, IC50: 9 nM BRD4-BD1, IC50: 119 nM						99%
INCB-057643	✔						99%+
(E/Z)-ZL0420	+++ BRD4 BD2, IC50: 32 nM BRD4 BD1, IC50: 27 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	+++ BRD2-BD1, IC50: 75nM BRD4-BD1, IC50: 143 nM						97%
SRX3207	+ BRD42, IC50: 3070 nM BRD41, 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		++ BAZ2A, Kd: 257 nM BAZ2B, Kd: 136 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					++ 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					++++ EP300, IC50: 38 nM CREBBP, IC50: 21 nM		99%+
Nordihydroguaiaretic acid					✔	IGF-1R,HER2	99%+
Curcumin					+ p300, IC50: ~25 μM	Ferroptosis,NF-κB,Nrf2	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。

CPI-637 生物活性

靶点	p300/CBP EP300, IC50:0.051 μM CBP, IC50:0.03 μM
描述	Mutations in the CBP/EP300 bromodomain are linked to the onset of neurological disorders and lymphomas. CPI-637 is a selective and cell-active CBP/EP300 bromodomain inhibitor with IC50 values of 0.03±0.01, 0.051±0.004, 11.0±0.6μM for CBP, EP300, and BRD4 BD-1, respectively. The EC₅₀ value of CPI-637 for CBP is 0.3±0.1μM. CPI-637 inhibited the expression of MYC, a transcription factor in human cancers, with an EC₅₀ value of 0.60μM^[2]. In mice inoculated with Q165P-mutant prostate cancer cells, combined treatment with CPI-637 (30mg/kg) and JQ1 (50mg/kg) five days a week for three consecutive weeks significantly reduced tumor volume and suppressed the phosphorylation of AKT, the expression of androgen receptor and its downstream target genes^[3].
作用机制	CPI-637 is a selective benzodiazepinone CBP/EP300 bromodomain inhibitor. The benzodiazepinone core of CPI-637 recapitulated the key hydrogen bonding interactions with the indazole substituents filling space above Pro1110 and the Pro/Arg cleft^[2].

CPI-637 细胞实验

Cell Line HL cell lines (L1236, KMH2) ALCL cell lines (DEL, Karpas299, MAC1) TZM-bl cells ACH2 cells J-Lat 10.6 cells J-Lat A2 cells	Concentration	Treated Time	Description	References
HL cell lines (L1236, KMH2)	10μM	24 h	To evaluate the effect of CPI-637 on HL cell proliferation and CD30 surface expression. Results showed that CPI-637 significantly inhibited cell proliferation and reduced CD30 expression.	Leukemia. 2023 Feb;37(2):396-407.
ALCL cell lines (DEL, Karpas299, MAC1)	10μM	24 h	To evaluate the effect of CPI-637 on ALCL and HL cell proliferation and CD30 surface expression. Results showed that CPI-637 significantly inhibited cell proliferation and reduced CD30 expression.	Leukemia. 2023 Feb;37(2):396-407.
TZM-bl cells	20 µM	48 h	CPI-637 increased LTR-driven luciferase activity, indicating its ability to activate HIV-1 transcription	Front Cell Infect Microbiol. 2021 Jul 19;11:686035.
ACH2 cells	20 µM	48 h	CPI-637 significantly increased the expression of HIV-1 p24 antigen, indicating its ability to reverse HIV-1 latent infection	Front Cell Infect Microbiol. 2021 Jul 19;11:686035.
J-Lat 10.6 cells	20 µM	48 h	CPI-637 significantly increased the percentage of GFP-positive cells, indicating its ability to reverse HIV-1 latent infection	Front Cell Infect Microbiol. 2021 Jul 19;11:686035.
J-Lat A2 cells	20 µM	48 h	CPI-637 significantly increased the percentage of GFP-positive cells, indicating its ability to reverse HIV-1 latent infection	Front Cell Infect Microbiol. 2021 Jul 19;11:686035.

CPI-637 动物实验

Species NSG mice	Animal Model ALCL and HL xenograft models	Administration	Dosage	Frequency	Description	References
NSG mice	ALCL and HL xenograft models	Oral	50 mg/kg	Daily administration until the endpoint	To evaluate the effect of CPI-637 on tumor growth in ALCL and HL xenograft models. Results showed that CPI-637 significantly slowed tumor growth and reduced the expression of MYC, IRF4, BATF3, and IL10.	Leukemia. 2023 Feb;37(2):396-407.

CPI-637 参考文献

[1]aylor AM, Côte A, et al. Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor(CPI-637). ACS Med Chem Lett. 2016 Mar 15;7(5):531-6.

[2]Taylor AM, Côté A, Hewitt MC, et al. Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637). ACS Med Chem Lett. 2016;7(5):531-536. Published 2016 Mar 15. doi:10.1021/acsmedchemlett.6b00075

[3]Yan Y, Ma J, Wang D, et al. The novel BET-CBP/p300 dual inhibitor NEO2734 is active in SPOP mutant and wild-type prostate cancer. EMBO Mol Med. 2019;11(11):e10659. doi:10.15252/emmm.201910659

CPI-637 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.59mL

0.52mL

0.26mL

12.94mL

2.59mL

1.29mL

25.88mL

5.18mL

2.59mL

CPI-637 技术信息

CAS号	1884712-47-3
分子式	C₂₂H₂₂N₆O
分子量	386.45
SMILES Code	O=C1C[C@@H](C)NC2=C(C3=CC4=C(N(C)N=C4C5=CN(C)N=C5)C=C3)C=CC=C2N1
MDL No.	MFCD30489741

别名
运输	蓝冰
InChI Key	BFTKDWYIRJGJCA-CYBMUJFWSA-N
Pubchem ID	121271792

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, store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 9 mg/mL(23.29 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

CPI-637 {[allProObj[0].p_purity_real_show]}

CPI-637 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

CPI-637 质控信息

CPI-637 生物活性

CPI-637 细胞实验

CPI-637 动物实验

CPI-637 参考文献

CPI-637 实验方案

CPI-637 技术信息

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CPI-637 {[allProObj[0].p_purity_real_show]}

CPI-637 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

CPI-637 质控信息

CPI-637 生物活性

CPI-637 细胞实验

CPI-637 动物实验

CPI-637 参考文献

CPI-637 实验方案

CPI-637 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

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临床研究

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