KG-501 | Naphtholas-ephosphate;2-naphthol-AS-E-phosphate | Epigenetic Reader Domain

KG-501 {[allProObj[0].p_purity_real_show]}

货号：A631283 同义名： Naphtholas-ephosphate; 2-naphthol-AS-E-phosphate

KG-501是一种碱性磷酸酶的组织化学底物，可抑制 CREB-CBP 相互作用。

KG-501 化学结构
CAS号：18228-17-6

KG-501 3D分子结构
CAS号：18228-17-6

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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	+++ 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。

KG-501 生物活性

靶点

bromodomain

描述

KG-501 is a CREB inhibitor, with an IC50 of 6.89 μM^[1]. KG-501 disrupts phospho (Ser-133) CREB binding to KIX with a Ki of ~90 μM, using concentrations of CREB that are within the linear range of the binding assay. Treatment of HEK293T cells with KG-501 also blocks induction of endogenous CREB target genes (NR4A2, αCG, c-fos, and RGS2) by forskolin, indicating that KG-501 likely exerts a general effect on CREB activity^[2]. In addition, KG-501 and CREB knockdown significantly decreased the levels of phosphorylated Akt, leading to a reduced number of oocytes with Foxo3a nuclear export. KG-501 also inhibited bpV (HOpic)-stimulated primordial follicle activation^[3]. At 10 μM, KG-501 suppresses the expression of all of the IL-1β-induced CXC chemokine genes except CXCL8. For the protein level, KG-501 significantly suppresses IL-1β-induced CXCL5 protein secretion^[4]. BAA (Bulleyaconitine) treatment induced phosphorylation of CREB (rather than NF-κB) and prodynorphin expression in cultured primary microglia, and antiallodynia in neuropathy, which were totally inhibited by the CREB inhibitor KG-501^[5].

KG-501 细胞实验

Cell Line PC12 cells Human mesenchymal stem cells (hMSCs) RAW264.7 cells CCD-18Co cells Primary microglial cells HEK293T cells Huh7 cells LNCaP cells 1273/99 FUJI SYO-I CME-1 HS-SY-II	Concentration	Treated Time	Description	References
PC12 cells	10 µM	30 min	Inhibited HJG-induced neurite outgrowth	Front Pharmacol. 2017 Nov 21;8:850.
Human mesenchymal stem cells (hMSCs)	30 µM	1 hour	KG-501 abrogated PTH1-34 upregulation of CYP27B1 at both 2 hours and 8 hours	Aging Cell. 2011 Dec;10(6):962-71.
RAW264.7 cells	10 µM	24 hours	KG-501 significantly decreased the boosting effect of curcumin on HGF expression	Acta Pharmacol Sin. 2021 Mar;42(3):422-435.
CCD-18Co cells	10 µM	24 hours	KG-501 significantly decreased the boosting effect of curcumin on HGF expression	Acta Pharmacol Sin. 2021 Mar;42(3):422-435.
Primary microglial cells	25 µM	30 minutes	KG-501 completely inhibited BAA-induced CREB phosphorylation and prodynorphin expression.	Sci Rep. 2017 Mar 22;7:45056.
HEK293T cells	10-25 µM	4 hours	KG-501 inhibits CREB-dependent transcription	Proc Natl Acad Sci U S A. 2004 Dec 21;101(51):17622-7.
Huh7 cells	10 µM	48 hours	Inhibited CREB1 phosphorylation and partially reversed TUFT1 overexpression-induced CREB1 nuclear translocation and lipid accumulation	J Immunol Res. 2022 Jun 19;2022:1590717.
LNCaP cells	25 µM	48 hours	KG-501 inhibited CREB-mediated transcriptional activation and significantly reduced Nurr1 promoter activity	BMC Cancer. 2016 Mar 31;16:257.
1273/99	0.63-5 µM	72 hours	Inhibition of CREB activity reduces downstream target expression, accompanied by suppression of SySa cell proliferation and induction of apoptosis in vitro and in vivo.	Cell Oncol (Dordr). 2022 Jun;45(3):399-413.
FUJI	0.63-5 µM	72 hours	Inhibition of CREB activity reduces downstream target expression, accompanied by suppression of SySa cell proliferation and induction of apoptosis in vitro and in vivo.	Cell Oncol (Dordr). 2022 Jun;45(3):399-413.
SYO-I	0.63-5 µM	72 hours	Inhibition of CREB activity reduces downstream target expression, accompanied by suppression of SySa cell proliferation and induction of apoptosis in vitro and in vivo.	Cell Oncol (Dordr). 2022 Jun;45(3):399-413.
CME-1	0.63-5 µM	72 hours	Inhibition of CREB activity reduces downstream target expression, accompanied by suppression of SySa cell proliferation and induction of apoptosis in vitro and in vivo.	Cell Oncol (Dordr). 2022 Jun;45(3):399-413.
HS-SY-II	0.63-5 µM	72 hours	Inhibition of CREB activity reduces downstream target expression, accompanied by suppression of SySa cell proliferation and induction of apoptosis in vitro and in vivo.	Cell Oncol (Dordr). 2022 Jun;45(3):399-413.

Cell Line

Concentration

Treated Time

Description

References

PC12 cells

10 µM

30 min

Inhibited HJG-induced neurite outgrowth

Front Pharmacol. 2017 Nov 21;8:850.

Human mesenchymal stem cells (hMSCs)

30 µM

1 hour

KG-501 abrogated PTH1-34 upregulation of CYP27B1 at both 2 hours and 8 hours

Aging Cell. 2011 Dec;10(6):962-71.

RAW264.7 cells

10 µM

24 hours

KG-501 significantly decreased the boosting effect of curcumin on HGF expression

Acta Pharmacol Sin. 2021 Mar;42(3):422-435.

CCD-18Co cells

10 µM

24 hours

KG-501 significantly decreased the boosting effect of curcumin on HGF expression

Acta Pharmacol Sin. 2021 Mar;42(3):422-435.

Primary microglial cells

25 µM

30 minutes

KG-501 completely inhibited BAA-induced CREB phosphorylation and prodynorphin expression.

Sci Rep. 2017 Mar 22;7:45056.

HEK293T cells

10-25 µM

4 hours

KG-501 inhibits CREB-dependent transcription

Proc Natl Acad Sci U S A. 2004 Dec 21;101(51):17622-7.

Huh7 cells

10 µM

48 hours

Inhibited CREB1 phosphorylation and partially reversed TUFT1 overexpression-induced CREB1 nuclear translocation and lipid accumulation

J Immunol Res. 2022 Jun 19;2022:1590717.

LNCaP cells

25 µM

48 hours

KG-501 inhibited CREB-mediated transcriptional activation and significantly reduced Nurr1 promoter activity

BMC Cancer. 2016 Mar 31;16:257.

1273/99

0.63-5 µM

72 hours

Inhibition of CREB activity reduces downstream target expression, accompanied by suppression of SySa cell proliferation and induction of apoptosis in vitro and in vivo.