SGC-CBP30 | CBP/p300 Inhibitor | AmBeed-信号通路专用抑制剂

SGC-CBP30 {[allProObj[0].p_purity_real_show]}

货号：A636668

SGC-CBP30是一种强效的CREBBP/EP300溴结构域抑制剂，对CREBBP和EP300溴结构域的IC50分别为21-69 nM和38 nM。

SGC-CBP30 化学结构
CAS号：1613695-14-9

SGC-CBP30 3D分子结构
CAS号：1613695-14-9

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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	+++ 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	+ 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	++++ BRD9, IC50: 19 nM BRD7, IC50: 117 nM						97%
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	++ 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	++++ Brd3(BD2), Kd: 13 nM Brd2(BD2), Kd: 62 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		+ L3MBTL4, IC50: 6 μM L3MBTL3, IC50: 35 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		++ PRC2, Kd: 114 nM EED, Kd: 82 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			++++ BRPF1, IC50: 48 nM BRPF3, IC50: 260 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,NF-κB,Nrf2	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。

SGC-CBP30 生物活性

靶点

p300/CBP

CREBBP, IC50:21 nM

EP300, IC50:38 nM

描述

CREBBP/EP300, two highly homologous transcriptional co-activators, are characterized by several zinc finger domains, a bromodomain, a plant homology domain, a HAT domain and a CREB binding domain. They bind to multiple partner proteins, mainly transcription factors and other co-activators and play essential roles in histone acetylation, mainly at histone H3 positions K18 and K27. SGC-CBP30, also called as CBP30, is a potent CREBBP/EP300 inhibitor with IC50 values of 69nM and 38nM for CREBBP (measured by Alphascreen assay) and EP300 (measured by ITC assay), respectively^[1]. Treatment with 2μM SGC-CBP30 for 24h in Th17 cells can inhibit the binding of p300 and ac-H3K56, a known CBP/p300 mark, to the IL17A gene locus in CHIP experiment. SGC-CBP30 showed a broad anti-inflammatory activity in a panel of 12 stimulated primary human cell types treated with SGC-CBP30 (<10uM), shown as the down-regulation of the cytokines IL-17, TNFα, IL-8, IL-2, IL-6, IL-1α, and IL-10, VCAM-1 and MCP1. 2μM CBP30 inhibited IL-17A production by AS CD4 T cells by 77%, and an average reduced the secretion of IL-17A by 66.3% in cells from patients with AS and PSA and from HCs^[2].

作用机制

SGC-CBP30 preferentially binds to the CBP/p300 Bromodomain and inhibited binding of p300 and of acetylated histone H3K56.^[2]

SGC-CBP30 细胞实验

Cell Line Myofibroblasts from Dupuytren's disease patients XG1LenRes cells Cardiac progenitor cells Panc1 cells MiaPaCa2 cells ASPC1 cells JJN3 cells KMS11LenRes cells HiBEC and NHC Intestinal epithelial cells (IECs)	Concentration	Treated Time	Description	References
Myofibroblasts from Dupuytren's disease patients	2.5 µM	3 days	To evaluate the effect of SGC-CBP30 on the expression of key profibrotic genes (ACTA2, COL1A1, COL3A1, TGFB1) in myofibroblasts. Results showed that SGC-CBP30 significantly inhibited the expression of these genes.	Proc Natl Acad Sci U S A. 2020 Aug 25;117(34):20753-20763.
XG1LenRes cells	0.2 µM and 0.4 µM	3 days	Co-treatment with SGC-CBP30 and lenalidomide significantly reduced the viability of XG1LenRes cells and downregulated IRF4 and MYC expression.	Blood Cancer J. 2019 Feb 11;9(2):19.
Cardiac progenitor cells	2 mM	48 hours	To explore the histone acetylation function of P300 that is responsible for modulation of gata4 transcription; CBP30 suppressed GATA4 mRNA.	Genes Dis. 2018 Oct 15;6(3):318-325.
Panc1 cells	1 µM	48 hours	To evaluate the effect of SGC-CBP30 on Panc1 cell growth, results showed that SGC-CBP30 alone had a marginal effect on cell growth, but its combination with JQ-1 significantly enhanced the suppression of cell growth.	Proc Natl Acad Sci U S A. 2022 Jan 25;119(4):e2116764119.
MiaPaCa2 cells	1 µM	48 hours	To evaluate the effect of SGC-CBP30 on MiaPaCa2 cell viability, results showed that the combination of SGC-CBP30 with JQ-1 significantly reduced cell viability.	Proc Natl Acad Sci U S A. 2022 Jan 25;119(4):e2116764119.
ASPC1 cells	1 µM	48 hours	To evaluate the effect of SGC-CBP30 on ASPC1 cell viability, results showed that the combination of SGC-CBP30 with JQ-1 significantly reduced cell viability.	Proc Natl Acad Sci U S A. 2022 Jan 25;119(4):e2116764119.
JJN3 cells	2.5 µM and 5 µM	5 days	Co-treatment with SGC-CBP30 and lenalidomide significantly reduced the viability of JJN3 cells.	Blood Cancer J. 2019 Feb 11;9(2):19.
KMS11LenRes cells	0.3 µM and 1 µM	5 days	Co-treatment with SGC-CBP30 and lenalidomide significantly reduced the viability of KMS11LenRes cells and downregulated IKZF1/IKZF3, IRF4, and MYC expression.	Blood Cancer J. 2019 Feb 11;9(2):19.
HiBEC and NHC	10 µM		Depletion of ACTA2-AS1 reduced expression of proliferative/fibrogenic markers, reduced LPS-induced cholangiocyte proliferation, and impaired organoid formation	J Hepatol. 2022 Apr;76(4):921-933.
Intestinal epithelial cells (IECs)	50 mg/kg		To test the hepatoprotective and enteroprotective effect of Ep300 inhibitor	Cell Discov. 2023 Jul 25;9(1):77.

Cell Line

Concentration

Treated Time

Description

References

Myofibroblasts from Dupuytren's disease patients

2.5 µM

3 days

To evaluate the effect of SGC-CBP30 on the expression of key profibrotic genes (ACTA2, COL1A1, COL3A1, TGFB1) in myofibroblasts. Results showed that SGC-CBP30 significantly inhibited the expression of these genes.

Proc Natl Acad Sci U S A. 2020 Aug 25;117(34):20753-20763.

XG1LenRes cells

0.2 µM and 0.4 µM

3 days

Co-treatment with SGC-CBP30 and lenalidomide significantly reduced the viability of XG1LenRes cells and downregulated IRF4 and MYC expression.

Blood Cancer J. 2019 Feb 11;9(2):19.

Cardiac progenitor cells

2 mM

48 hours

To explore the histone acetylation function of P300 that is responsible for modulation of gata4 transcription; CBP30 suppressed GATA4 mRNA.

Genes Dis. 2018 Oct 15;6(3):318-325.

Panc1 cells

1 µM

48 hours

To evaluate the effect of SGC-CBP30 on Panc1 cell growth, results showed that SGC-CBP30 alone had a marginal effect on cell growth, but its combination with JQ-1 significantly enhanced the suppression of cell growth.

Proc Natl Acad Sci U S A. 2022 Jan 25;119(4):e2116764119.

MiaPaCa2 cells

1 µM

48 hours

To evaluate the effect of SGC-CBP30 on MiaPaCa2 cell viability, results showed that the combination of SGC-CBP30 with JQ-1 significantly reduced cell viability.

Proc Natl Acad Sci U S A. 2022 Jan 25;119(4):e2116764119.

ASPC1 cells

1 µM

48 hours

To evaluate the effect of SGC-CBP30 on ASPC1 cell viability, results showed that the combination of SGC-CBP30 with JQ-1 significantly reduced cell viability.

Proc Natl Acad Sci U S A. 2022 Jan 25;119(4):e2116764119.

JJN3 cells

2.5 µM and 5 µM

5 days

Co-treatment with SGC-CBP30 and lenalidomide significantly reduced the viability of JJN3 cells.

Blood Cancer J. 2019 Feb 11;9(2):19.

KMS11LenRes cells

0.3 µM and 1 µM

5 days

Co-treatment with SGC-CBP30 and lenalidomide significantly reduced the viability of KMS11LenRes cells and downregulated IKZF1/IKZF3, IRF4, and MYC expression.

Blood Cancer J. 2019 Feb 11;9(2):19.

HiBEC and NHC

10 µM

Depletion of ACTA2-AS1 reduced expression of proliferative/fibrogenic markers, reduced LPS-induced cholangiocyte proliferation, and impaired organoid formation

J Hepatol. 2022 Apr;76(4):921-933.

Intestinal epithelial cells (IECs)

50 mg/kg

To test the hepatoprotective and enteroprotective effect of Ep300 inhibitor

Cell Discov. 2023 Jul 25;9(1):77.

SGC-CBP30 动物实验

Species Mice Mice Mice Mice	Animal Model Murine cholangiopathy model H1975 and H1299 cell lines KPC model D-GALN/LPS-induced acute liver failure model	Administration	Dosage	Frequency	Description	References
Mice	Murine cholangiopathy model	Intraperitoneal injection	10 μg/g	Three times per week for 8 weeks	Confirmed the protective role of p300 inhibition in terms of DR and hepatic fibrosis	J Hepatol. 2022 Apr;76(4):921-933.
Mice	H1975 and H1299 cell lines	Intraperitoneal injection	250 mg/kg/d	Every other day for a duration of 21 days	The study investigated the role of UPP1 in regulating tumor growth and sensitivity to glycolytic inhibitors in a nude mouse model.	Aging Dis. 2022 Oct 1;13(5):1488-1503
Mice	KPC model	Intraperitoneal injection	5 mg/kg	Daily for 6 months	To evaluate the effect of XP-524 on survival and tumor growth in the KPC model, results showed that XP-524 significantly extended survival and reduced tumor burden and fibrosis.	Proc Natl Acad Sci U S A. 2022 Jan 25;119(4):e2116764119.
Mice	D-GALN/LPS-induced acute liver failure model	Intraperitoneal injection	50 mg/kg	One time 1 h before D/L treatment	To investigate the therapeutic potential of Ep300 inhibition in intestinal and liver protection	Cell Discov. 2023 Jul 25;9(1):77.

Species

Mice Mice Mice Mice

Animal Model

Murine cholangiopathy model H1975 and H1299 cell lines KPC model D-GALN/LPS-induced acute liver failure model

Administration

Dosage

Frequency

Description

References

Mice

Murine cholangiopathy model

Intraperitoneal injection

10 μg/g

Three times per week for 8 weeks

Confirmed the protective role of p300 inhibition in terms of DR and hepatic fibrosis

J Hepatol. 2022 Apr;76(4):921-933.

Mice

H1975 and H1299 cell lines

Intraperitoneal injection

250 mg/kg/d

Every other day for a duration of 21 days

The study investigated the role of UPP1 in regulating tumor growth and sensitivity to glycolytic inhibitors in a nude mouse model.

Aging Dis. 2022 Oct 1;13(5):1488-1503

Mice

KPC model

Intraperitoneal injection

5 mg/kg

Daily for 6 months

To evaluate the effect of XP-524 on survival and tumor growth in the KPC model, results showed that XP-524 significantly extended survival and reduced tumor burden and fibrosis.

Proc Natl Acad Sci U S A. 2022 Jan 25;119(4):e2116764119.

Mice

D-GALN/LPS-induced acute liver failure model

Intraperitoneal injection

50 mg/kg

One time 1 h before D/L treatment

To investigate the therapeutic potential of Ep300 inhibition in intestinal and liver protection

Cell Discov. 2023 Jul 25;9(1):77.

SGC-CBP30 参考文献

SGC-CBP30 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.96mL

0.39mL

0.20mL

9.82mL

1.96mL

0.98mL

19.64mL

3.93mL

1.96mL

SGC-CBP30 技术信息

CAS号	1613695-14-9
分子式	C₂₈H₃₃ClN₄O₃
分子量	509.04
SMILES Code	C[C@H](N1CCOCC1)CN2C(CCC3=CC=C(OC)C(Cl)=C3)=NC4=CC(C5=C(C)ON=C5C)=CC=C24
MDL No.	MFCD26792586

别名
运输	蓝冰
InChI Key	GEPYBHCJBORHCE-SFHVURJKSA-N
Pubchem ID	72201027

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: 65 mg/mL(127.69 mM)，配合低频超声，并水浴加热至45℃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

SGC-CBP30 {[allProObj[0].p_purity_real_show]}

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