PFI-1 | Epigenetic Reader Domain Inhibitor | AmBeed-信号通路专用抑制剂

PFI-1 {[allProObj[0].p_purity_real_show]}

货号：A280183 同义名： PF-06405761; PF-6405761

PFI-1是一种高度选择性的 BET（溴结构域含蛋白）抑制剂，对于 BRD4 的 IC50 为 0.22 μM，对于 BRD2 的 IC50 为 98 nM。

PFI-1 化学结构
CAS号：1403764-72-6

PFI-1 3D分子结构
CAS号：1403764-72-6

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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	+ BRD4, IC50: 0.5 μM BRD3, IC50: 0.25 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	++++ 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 BD2, IC50: 32 nM BRD4 BD1, IC50: 27 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	+++ BRD4-BD1, IC50: 143 nM BRD2-BD1, IC50: 75nM						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		++ BAZ2B, Kd: 136 nM BAZ2A, Kd: 257 nM					99%+
KG-501		✔					99%+
UNC 669		+ L3MBTL4, IC50: 6 μM L3MBTL3, IC50: 35 μM					99%
PFI-3		+++ SMARCA4, Kd: 55 nM SMARCA2A, Kd: 72 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			++ BRPF1, IC50: 80 nM BRPF2, IC50: 7.9 μM				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			++++ 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					+ 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,NF-κB,Ferroptosis	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。

PFI-1 生物活性

靶点

BET

BRD2, IC50:98 nM

BRD4, IC50:0.22 μM

描述

PFI-1 is a potent and selective BET inhibitor with IC50 value of 0.22μM for BRD4(1). PFI-1 exhibited inhibitory effect on IL6 production from human blood mononuclear cells stimulated by LPS with EC50 value of 1.89μM^[3]. PFI-1 has antiproliferative effects on leukemic cell lines and efficiently abrogates their clonogenic growth with GI50 values ranging in 0.8-11μM. Exposure of sensitive cell lines with PFI-1 resulted in G1 cell cycle arrest, downregulation of MYC expression in MV4;11 cells, as well as induction of apoptosis and induced differentiation of primary leukemic blasts. Cells exposed to PFI-1 showed significant downregulation of Aurora B kinase, thus attenuating phosphorylation of the Aurora substrate H3S10^[4].

作用机制

PFI-1 could bind to BET protein through the key interaction with Asn140. And the urea carbonyl also makes a water-bridged hydrogenbond interaction with the phenolic OH of Tyr97^[3]. PFI-1 efficiently blocks the interaction of BET BRDs with acetylated histone tails. It acts as an acetyl-lysine (Kac) mimetic inhibitor efficiently occupying the Kac binding site in BRD4 and BRD2.^[4]

PFI-1 细胞实验

Cell Line K-562 THP-1 MCF7 cells KASUMI-1 MV4;11 A549 cells H358 cells PC9 HCC827 TZMbl cells A10.6 cells Jurkat C11 cells Candida albicans C9BAC primary cortical neurons SH-SY5Y LE90 cells	Concentration	Treated Time	Description	References
K-562	>20 μM		PFI-1 showed weak antiproliferative effects on K-562 cells with a GI50 >20 μM	Cancer Res. 2013 Jun 1;73(11):3336-46.
THP-1	4 ± 2 μM		PFI-1 showed antiproliferative effects on THP-1 cells with a GI50 of 4 ± 2 μM	Cancer Res. 2013 Jun 1;73(11):3336-46.
MCF7 cells	500 μM	2 days	PFI-1 inhibits BRD4 binding to super-enhancers, reducing CD47 expression	Nat Commun. 2017 Apr 5;8:14802.
KASUMI-1	0.8 ± 1 μM		PFI-1 showed antiproliferative effects on KASUMI-1 cells with a GI50 of 0.8 ± 1 μM	Cancer Res. 2013 Jun 1;73(11):3336-46.
MV4;11	1.5 ± 1 μM		PFI-1 showed antiproliferative effects on MV4;11 cells with a GI50 of 1.5 ± 1 μM	Cancer Res. 2013 Jun 1;73(11):3336-46.
A549 cells	5 μM	48 h	Combination of PFI-1 with SAHA in A549 cells reduced the expression of NRP2 and ZEB1.	Clin Epigenetics. 2017 Aug 8;9:80.
H358 cells	5 μM	48 h	PFI-1 treatment in H358 cells decreased PD-L1 and SEMA3C expression. When combined with TGF-β1, PFI-1 significantly reduced the expression of NRP2, PD-L1, SEMA3C, vimentin, and ZEB1.	Clin Epigenetics. 2017 Aug 8;9:80.
PC9	2 μM	48 h	PFI-1 restored CBX5 expression and resensitized EGFRi-resistant LUAD cells to EGFRi/BETi combination therapy.	Proc Natl Acad Sci U S A. 2023 Jan 24;120(4):e2218118120.
HCC827	2 μM	48 h	PFI-1 restored CBX5 expression and resensitized EGFRi-resistant LUAD cells to EGFRi/BETi combination therapy.	Proc Natl Acad Sci U S A. 2023 Jan 24;120(4):e2218118120.
TZMbl cells	5 μM	48 h	PFI-1 significantly increased luciferase expression, indicating its ability to activate HIV-1 LTR	Sci Rep. 2017 Nov 30;7(1):16646.
A10.6 cells	5 μM	72 h	PFI-1 robustly increased GFP expression, indicating its ability to reactivate latent HIV-1	Sci Rep. 2017 Nov 30;7(1):16646.
Jurkat C11 cells	5 μM	72 h	PFI-1 robustly increased GFP expression, indicating its ability to reactivate latent HIV-1	Sci Rep. 2017 Nov 30;7(1):16646.
Candida albicans	0.3-410μM		To evaluate the inhibitory effect of PFI-1 on CaBdf1 BDs, the results showed that PFI-1 had poor inhibitory effect on CaBdf1 BDs, with IC50 values ranging from 0.3-410μM.	Nat Commun. 2017 May 18;8:15482.
C9BAC primary cortical neurons	5 µM	24 h	PFI-1 treatment significantly increased the expression of V1-V3 transcripts of the human mutant C9ORF72 gene in C9BAC primary cortical neurons, reduced poly(GP)-DPR inclusions, but enhanced intranuclear RNA foci.	Clin Epigenetics. 2021 Mar 16;13(1):56.
SH-SY5Y LE90 cells	5 µM	24 h	PFI-1 significantly enhanced luciferase reporter activity in SH-SY5Y LE90 cells, indicating its ability to increase C9ORF72 gene expression.	Clin Epigenetics. 2021 Mar 16;13(1):56.

Cell Line

Concentration

Treated Time

Description

References

K-562

>20 μM

PFI-1 showed weak antiproliferative effects on K-562 cells with a GI50 >20 μM

Cancer Res. 2013 Jun 1;73(11):3336-46.

THP-1

4 ± 2 μM

PFI-1 showed antiproliferative effects on THP-1 cells with a GI50 of 4 ± 2 μM

Cancer Res. 2013 Jun 1;73(11):3336-46.

MCF7 cells

500 μM

2 days

PFI-1 inhibits BRD4 binding to super-enhancers, reducing CD47 expression

Nat Commun. 2017 Apr 5;8:14802.

KASUMI-1

0.8 ± 1 μM

PFI-1 showed antiproliferative effects on KASUMI-1 cells with a GI50 of 0.8 ± 1 μM

Cancer Res. 2013 Jun 1;73(11):3336-46.

MV4;11

1.5 ± 1 μM

PFI-1 showed antiproliferative effects on MV4;11 cells with a GI50 of 1.5 ± 1 μM

Cancer Res. 2013 Jun 1;73(11):3336-46.

A549 cells

5 μM

48 h

Combination of PFI-1 with SAHA in A549 cells reduced the expression of NRP2 and ZEB1.

Clin Epigenetics. 2017 Aug 8;9:80.

H358 cells

5 μM

48 h

PFI-1 treatment in H358 cells decreased PD-L1 and SEMA3C expression. When combined with TGF-β1, PFI-1 significantly reduced the expression of NRP2, PD-L1, SEMA3C, vimentin, and ZEB1.

Clin Epigenetics. 2017 Aug 8;9:80.

PC9

2 μM

48 h

PFI-1 restored CBX5 expression and resensitized EGFRi-resistant LUAD cells to EGFRi/BETi combination therapy.

Proc Natl Acad Sci U S A. 2023 Jan 24;120(4):e2218118120.

HCC827

2 μM

48 h

PFI-1 restored CBX5 expression and resensitized EGFRi-resistant LUAD cells to EGFRi/BETi combination therapy.

Proc Natl Acad Sci U S A. 2023 Jan 24;120(4):e2218118120.

TZMbl cells

5 μM

48 h

PFI-1 significantly increased luciferase expression, indicating its ability to activate HIV-1 LTR

Sci Rep. 2017 Nov 30;7(1):16646.

A10.6 cells

5 μM

72 h

PFI-1 robustly increased GFP expression, indicating its ability to reactivate latent HIV-1

Sci Rep. 2017 Nov 30;7(1):16646.

Jurkat C11 cells

5 μM

72 h

PFI-1 robustly increased GFP expression, indicating its ability to reactivate latent HIV-1

Sci Rep. 2017 Nov 30;7(1):16646.

Candida albicans

0.3-410μM

To evaluate the inhibitory effect of PFI-1 on CaBdf1 BDs, the results showed that PFI-1 had poor inhibitory effect on CaBdf1 BDs, with IC50 values ranging from 0.3-410μM.

Nat Commun. 2017 May 18;8:15482.

C9BAC primary cortical neurons

5 µM

24 h

PFI-1 treatment significantly increased the expression of V1-V3 transcripts of the human mutant C9ORF72 gene in C9BAC primary cortical neurons, reduced poly(GP)-DPR inclusions, but enhanced intranuclear RNA foci.

Clin Epigenetics. 2021 Mar 16;13(1):56.

SH-SY5Y LE90 cells

5 µM

24 h

PFI-1 significantly enhanced luciferase reporter activity in SH-SY5Y LE90 cells, indicating its ability to increase C9ORF72 gene expression.

Clin Epigenetics. 2021 Mar 16;13(1):56.

PFI-1 动物实验

Species Mice Mice Mice	Animal Model B-ALL xenograft model Human EGFR-mutant LUAD xenograft model Breast cancer model	Administration	Dosage	Frequency	Description	References
Mice	B-ALL xenograft model	Intraperitoneal injection	50 mg/kg	Four times per week for 3 weeks	PFI-1 could not reach the effective dose in vivo, so (+)-JQ1 was used instead, which significantly reduced the expression of Aurora B and c-Myc	Cancer Res. 2013 Jun 1;73(11):3336-46.
Mice	Human EGFR-mutant LUAD xenograft model	Oral	2.5 mg/kg	3 times per week until the end of the experiment	Combination treatment with PFI-1 and EGFRi significantly inhibited the growth of EGFRi-resistant LUAD tumors.	Proc Natl Acad Sci U S A. 2023 Jan 24;120(4):e2218118120.
Mice	Breast cancer model	Intraperitoneal injection	20 mg/kg	Three times per week for two weeks	To evaluate the anti-tumour effect of PFI-1 in breast cancer, results showed that PFI-1 had no significant anti-tumour effect	Nat Biomed Eng. 2021 Nov;5(11):1320-1335

Species

Mice Mice Mice

Animal Model

B-ALL xenograft model Human EGFR-mutant LUAD xenograft model Breast cancer model

Administration

Dosage

Frequency

Description

References

Mice

B-ALL xenograft model

Intraperitoneal injection

50 mg/kg

Four times per week for 3 weeks

PFI-1 could not reach the effective dose in vivo, so (+)-JQ1 was used instead, which significantly reduced the expression of Aurora B and c-Myc

Cancer Res. 2013 Jun 1;73(11):3336-46.

Mice

Human EGFR-mutant LUAD xenograft model

Oral

2.5 mg/kg

3 times per week until the end of the experiment

Combination treatment with PFI-1 and EGFRi significantly inhibited the growth of EGFRi-resistant LUAD tumors.

Proc Natl Acad Sci U S A. 2023 Jan 24;120(4):e2218118120.

Mice

Breast cancer model

Intraperitoneal injection

20 mg/kg

Three times per week for two weeks

To evaluate the anti-tumour effect of PFI-1 in breast cancer, results showed that PFI-1 had no significant anti-tumour effect

Nat Biomed Eng. 2021 Nov;5(11):1320-1335

PFI-1 动物研究

Dose

Rat: 1 mg/kg^[1] (i.v.); 2 mg/kg^[1] (p.o.) Mice: 2 mg/kg^[1] (s.c.)

Administration

i.v., p.o.

Pharmacokinetics

Animal	Mice^[1]	Rats^[1]
Dose	2 mg/kg	1 mg/kg (i.v.) 2 mg/kg (p.o.)
Administration	s.c.	i.v. p.o.
F		32% (p.o.)
V_d		1 L/kg (i.v.)
T_1/2	2 h	1 h (i.v.)
T_max	1 h
CL		18 ml/min/kg (i.v.)
C_max	58 ng/ml

PFI-1 参考文献

PFI-1 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.88mL

0.58mL

0.29mL

14.39mL

2.88mL

1.44mL

28.79mL

5.76mL

2.88mL

PFI-1 技术信息

CAS号	1403764-72-6
分子式	C₁₆H₁₇N₃O₄S
分子量	347.39
SMILES Code	O=S(C1=CC=CC=C1OC)(NC2=CC3=C(NC(N(C)C3)=O)C=C2)=O
MDL No.	MFCD22580416

别名	PF-06405761; PF-6405761
运输	蓝冰
InChI Key	TXZPMHLMPKIUGK-UHFFFAOYSA-N
Pubchem ID	71271629

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: 35 mg/mL(100.75 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

PFI-1 {[allProObj[0].p_purity_real_show]}

PFI-1 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

PFI-1 质控信息

PFI-1 生物活性

PFI-1 细胞实验

PFI-1 动物实验

PFI-1 动物研究

PFI-1 参考文献

PFI-1 实验方案

PFI-1 技术信息

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PFI-1 {[allProObj[0].p_purity_real_show]}

PFI-1 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

PFI-1 质控信息

PFI-1 生物活性

PFI-1 细胞实验

PFI-1 动物实验

PFI-1 动物研究

PFI-1 参考文献

PFI-1 实验方案

PFI-1 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

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