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dTRIM24 {[allProObj[0].p_purity_real_show]}

货号:A449341

dTRIM24 是一种强效且选择性的 PROTAC,靶向 TRIM24,而 TRIM24 被认为是许多癌症中的依赖因子,dTRIM24 将 TRIM24 配体 IACS-9571 与 VHL 配体结合。

dTRIM24 化学结构 CAS号:2170695-14-2
dTRIM24 化学结构
CAS号:2170695-14-2
dTRIM24 3D分子结构
CAS号:2170695-14-2
dTRIM24 化学结构 CAS号:2170695-14-2
dTRIM24 3D分子结构 CAS号:2170695-14-2
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dTRIM24 纯度/质量文件 产品仅供科研

货号:A449341 标准纯度: {[allProObj[0].p_purity_real_show]}
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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 +++

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 BD1, Kd: 90 nM

BRD4 BD2, Kd: 28 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 +

BRD4BD1, 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-BD2, IC50: 41 nM

BRD4-BD1, IC50: 5 nM

97%
A1874 99%+
Y06036 ++

BRD4 (1), Kd: 82 nM

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

BRD2-BD1, IC50: 75nM

BRD4-BD1, IC50: 143 nM

97%
SRX3207 +

BRD42, IC50: 3070 nM

BRD41, IC50: 3070 nM

Syk 98%
GSK046 +++

BRD3BD2, IC50: 98 nM

BRD4BD2, IC50: 214 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, IC50: 120 nM

L3MBTL3- D274A, IC50: 3.5 μM

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 ++

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 ++++

BRPF3, IC50: 260 nM

BRPF1, IC50: 48 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 ++++

EP300, IC50: 38 nM

CREBBP, IC50: 21 nM

99%+
Nordihydroguaiaretic acid IGF-1R,HER2 99%+
Curcumin +

p300, IC50: ~25 μM

Nrf2,NF-κB,Ferroptosis 98%
PF-CBP1 HCl ++

p300/CBP, IC50: 363nM

CREBBP, IC50: 125nM

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。

dTRIM24 生物活性

描述 dTRIM24 is a potent and selective PROTAC targeting on TRIM24 which has been posited as a dependency in numerous cancers, with TRIM24 ligand IACS-9571 conjugated to a VHL ligand. Treatment with dTRIM24 led to a max degradation of TRIM24 by 72% at concentration of 5μM in 293FT cells post 24h. A prolonged treatment with 5μM dTRIM24 for 48h degrade TRIM24 by 76% in 293FT cells. The two factors, time and concentration, exhibited interaction effect on the function of dTRIM24. dTRIM24 at concentration of 5μM possessing the max degradation of TRIM24 by 72% but almost not effect at concentration of 10μM post 24h in MOLM-13 cells, and a degradation of TRIM24 by 89% could be achieved by dTRIM24 at concentration of 2.5μM post 48h in the same cell line. dTRIM24 at concentration of 5μM inhibited MOLM-13cell proliferation within 7 days, with apoptosis shown by cleaved PARP observed at 48h[1].

dTRIM24 参考文献

[1]Gechijian LN, Buckley DL, et al. Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands. Nat Chem Biol. 2018 Apr;14(4):405-412.

dTRIM24 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

0.90mL

0.18mL

0.09mL

4.49mL

0.90mL

0.45mL

8.98mL

1.80mL

0.90mL

dTRIM24 技术信息

CAS号2170695-14-2
分子式C55H68N8O13S2
分子量 1113.304
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,2-8°C

溶解度

DMSO: 105 mg/mL(94.31 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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