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UNC 669 {[allProObj[0].p_purity_real_show]}

货号:A223382

UNC 669是L3MBTL1和L3MBTL3的甲基赖氨酸结合结构域的配体,其抑制L3MBTL1和L3MBTL3的IC50值分别为4.2 μM和3.1 μM。

UNC 669 化学结构 CAS号:1314241-44-5
UNC 669 化学结构
CAS号:1314241-44-5
UNC 669 3D分子结构
CAS号:1314241-44-5
UNC 669 化学结构 CAS号:1314241-44-5
UNC 669 3D分子结构 CAS号:1314241-44-5
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UNC 669 纯度/质量文件 产品仅供科研

货号:A223382 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Histone Methyltransferase 其他靶点 纯度
BRD4770 99%+
UNC1999 +++

EZH1, IC50: 45 nM

EZH2, IC50: 2 nM

99%+
EPZ005687 ++

EZH2, Ki: 24 nM

98+%
EPZ015666 +++

PRMT5, Ki: 5 nM

99%+
3-Deazaneplanocin A HCl ++++

S-adenosylhomocysteine hydrolase, Ki: 50 pM

99%+
Tazemetostat +++

EZH2, IC50: 11 nM

EZH2, Ki: 2.5 nM

98%
GSK126 ++

EZH2, IC50: 9.9 nM

99%+
MI-3 +

Menin-MLL, IC50: 648 nM

98%
MM-102 ++

MLL1, IC50: 0.4 μM

99%
EI1 ++

Ezh2 (wild-type), IC50: 15 nM

EZH2 (Y641F), IC50: 13 nM

98%
SGC0946 ++++

DOT1L, IC50: 0.3 nM

99%+
PFI-2 HCl ++++

SETD7, Ki: 0.33 nM

SETD7, IC50: 2 nM

99%+
Pinometostat ++++

DOT1L, Ki: 80 pM

99%+
EPZ004777 +++

DOT1L, IC50: 0.4 nM

99%+
Entacapone ++

COMT, IC50: 151 nM

95%
UNC0379 +

SETD8, IC50: 7.9 μM

99%+
Menin-MLL inhibitor MI-2 +

Menin-MLL, IC50: 446 nM

98%
GSK343 +++

EZH1, IC50: 240 nM

EZH2, IC50: 4 nM

99%+
BIX-01294 3HCl +

G9a, IC50: 2.7 μM

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。
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 +

BRD4, IC50: 0.5 μM

BRD3, IC50: 0.25 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

99+%
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 ++++

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 +

BRD4BD1, 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-BD1, IC50: 5 nM

BRD4-BD2, IC50: 41 nM

97%
A1874 99%+
Y06036 ++

BRD4 (1), Kd: 82 nM

99%+
Alobresib NF-κB 98%
ODM-207 99%
GSK778 +++

BRD4-BD1, IC50: 143 nM

BRD2-BD1, IC50: 75nM

97%
SRX3207 +

BRD42, IC50: 3070 nM

BRD41, IC50: 3070 nM

Syk 98%
GSK046 +++

BRD4BD2, IC50: 214 nM

BRD3BD2, IC50: 98 nM

98%
GSK620 97%
Thalidomide-NH-C4-NH-Boc 98%
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

98%
PFI-3 +++

SMARCA4, Kd: 55 nM

SMARCA2A, Kd: 72 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 ++

BRPF2, IC50: 7.9 μM

BRPF1, IC50: 80 nM

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

97%
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 ++++

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%
PF-CBP1 HCl ++

CREBBP, IC50: 125nM

p300/CBP, IC50: 363nM

97%
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

98%
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。

UNC 669 生物活性

靶点
  • bromodomain

    L3MBTL4, IC50:6 μM

    L3MBTL3, IC50:35 μM

描述 UNC669 is a selective MBT antagonist with IC50 values of 6μM, 35μM and 69μM for L3MBTL1, 3 and 4, respectively[3]. It inhibits L3MBTL1-methylated histone protein-protein interaction[2].
作用机制 UNC669 is a small molecule ligand for a methyl-lysine binding domain.[2]

UNC 669 参考文献

[1]Herold JM, Wigle TJ, et al. Small-molecule ligands of methyl-lysine binding proteins. J Med Chem. 2011 Apr 14;54(7):2504-11.

[2]Structure–activity relationships of methyl-lysine reader antagonists

[3]Herold JM, Wigle TJ, Norris JL, Lam R, Korboukh VK, Gao C, Ingerman LA, Kireev DB, Senisterra G, Vedadi M, Tripathy A, Brown PJ, Arrowsmith CH, Jin J, Janzen WP, Frye SV. Small-molecule ligands of methyl-lysine binding proteins. J Med Chem. 2011 Apr 14;54(7):2504-11. doi: 10.1021/jm200045v. Epub 2011 Mar 18. PMID: 21417280; PMCID: PMC3109722.

UNC 669 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.96mL

0.59mL

0.30mL

14.78mL

2.96mL

1.48mL

29.56mL

5.91mL

2.96mL

UNC 669 技术信息

CAS号1314241-44-5
分子式C15H20BrN3O
分子量 338.243
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

溶解度

DMSO: 50 mg/mL(147.82 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

动物实验配方
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