dTRIM24 | PROTAC TRIM24 Degrader | AmBeed-信号通路专用抑制剂

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 3D分子结构
CAS号：2170695-14-2

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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 (2), Ki: 0.34 μM BRD4 (1), Ki: <0.085 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						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	++++ 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	+ 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 BD1, IC50: 27 nM BRD4 BD2, IC50: 32 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	+++ BRD4-BD1, IC50: 143 nM BRD2-BD1, IC50: 75nM						97%
SRX3207	+ BRD41, IC50: 3070 nM BRD42, IC50: 3070 nM					Syk	98%
GSK046	+++ BRD4_BD2, IC50: 214 nM BRD3_BD2, IC50: 98 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		+ L3MBTL3, IC50: 35 μM L3MBTL4, IC50: 6 μM					99%
PFI-3		+++ SMARCA2A, Kd: 72 nM SMARCA4, Kd: 55 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			++ BRPF2, IC50: 7.9 μM BRPF1, IC50: 80 nM				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			++++ BRPF3, IC50: 260 nM BRPF1, IC50: 48 nM				99%+
E-7386				+++ CBP/beta-catenin, IC50: 0.0484 μM			99%
I-CBP112					++ p300, Kd: 167 nM CBP, Kd: 151 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					✔	IGF-1R,HER2	99%+
Curcumin					+ p300, IC50: ~25 μM	Ferroptosis,Nrf2,NF-κB	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。

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 细胞实验

Cell Line JBR JeKo-1 ZBR Z-138 GBM#BG5 cells GBM#06 cells GBM#BG7 cells Raw 264.7 cells (M1 macrophages) MOLM-13 cells 293FT cells GBM#P3 cells	Concentration	Treated Time	Description	References
JBR	2.5, 5, 7.5, 10, 12.5 µM	24 hours	To evaluate the effect of dTRIM24 on TRIM24 and p53 levels, results showed dTRIM24 dose-dependently reduced TRIM24 levels.	Cell Death Discov. 2025 Mar 17;11(1):108
JeKo-1	2.5, 5, 7.5, 10, 12.5 µM	24 hours	To evaluate the effect of dTRIM24 on TRIM24 and p53 levels, results showed dTRIM24 dose-dependently reduced TRIM24 levels.	Cell Death Discov. 2025 Mar 17;11(1):108
ZBR	2.5, 5, 10 µM	24 hours	To evaluate the effect of dTRIM24 on TRIM24 and p53 levels, results showed dTRIM24 dose-dependently reduced TRIM24 levels and increased p53 accumulation.	Cell Death Discov. 2025 Mar 17;11(1):108
Z-138	2.5, 5, 10 µM	24 hours	To evaluate the effect of dTRIM24 on TRIM24 and p53 levels, results showed dTRIM24 dose-dependently reduced TRIM24 levels and increased p53 accumulation.	Cell Death Discov. 2025 Mar 17;11(1):108
GBM#BG5 cells	5, 10 μM		inhibited cell proliferation	J Transl Med. 2021 Dec 9;19(1):505
GBM#06 cells	5, 10 μM		inhibited cell proliferation	J Transl Med. 2021 Dec 9;19(1):505
GBM#BG7 cells	5, 10 μM		inhibited cell proliferation	J Transl Med. 2021 Dec 9;19(1):505
Raw 264.7 cells (M1 macrophages)	0.31, 0.62, 1.25, 2.50, 5.00 μg/mL	24 hours	Evaluate the effect of MELT on M1 macrophage polarization to M2 phenotype. Results showed MELT significantly downregulated iNOS (M1 marker) and upregulated Arg1 (M2 marker), promoting M2 polarization.	Acta Pharmacol Sin. 2023 Oct;44(10):1962-1976
MOLM-13 cells	2.5 µM	24 hours	Evaluate the degradation effect of dTRIM24 on TRIM24 protein, showing time-dependent degradation	Nat Chem Biol. 2018 Apr;14(4):405-412
293FT cells	5 µM	24 hours	Evaluate the degradation effect of dTRIM24 on TRIM24 protein, showing dose-dependent degradation	Nat Chem Biol. 2018 Apr;14(4):405-412
GBM#P3 cells	5, 10 μM	48 hours	inhibited tumorsphere formation and expression of stemness markers SOX2 and Nestin	J Transl Med. 2021 Dec 9;19(1):505

Cell Line

Concentration

Treated Time

Description

References

JBR

2.5, 5, 7.5, 10, 12.5 µM

24 hours

To evaluate the effect of dTRIM24 on TRIM24 and p53 levels, results showed dTRIM24 dose-dependently reduced TRIM24 levels.

Cell Death Discov. 2025 Mar 17;11(1):108

JeKo-1

2.5, 5, 7.5, 10, 12.5 µM

24 hours

To evaluate the effect of dTRIM24 on TRIM24 and p53 levels, results showed dTRIM24 dose-dependently reduced TRIM24 levels.

Cell Death Discov. 2025 Mar 17;11(1):108

ZBR

2.5, 5, 10 µM

24 hours

To evaluate the effect of dTRIM24 on TRIM24 and p53 levels, results showed dTRIM24 dose-dependently reduced TRIM24 levels and increased p53 accumulation.

Cell Death Discov. 2025 Mar 17;11(1):108

Z-138

2.5, 5, 10 µM

24 hours

To evaluate the effect of dTRIM24 on TRIM24 and p53 levels, results showed dTRIM24 dose-dependently reduced TRIM24 levels and increased p53 accumulation.

Cell Death Discov. 2025 Mar 17;11(1):108

GBM#BG5 cells

5, 10 μM

inhibited cell proliferation

J Transl Med. 2021 Dec 9;19(1):505

GBM#06 cells

5, 10 μM

inhibited cell proliferation

J Transl Med. 2021 Dec 9;19(1):505

GBM#BG7 cells

5, 10 μM

inhibited cell proliferation

J Transl Med. 2021 Dec 9;19(1):505

Raw 264.7 cells (M1 macrophages)

0.31, 0.62, 1.25, 2.50, 5.00 μg/mL

24 hours

Evaluate the effect of MELT on M1 macrophage polarization to M2 phenotype. Results showed MELT significantly downregulated iNOS (M1 marker) and upregulated Arg1 (M2 marker), promoting M2 polarization.

Acta Pharmacol Sin. 2023 Oct;44(10):1962-1976

MOLM-13 cells

2.5 µM

24 hours

Evaluate the degradation effect of dTRIM24 on TRIM24 protein, showing time-dependent degradation

Nat Chem Biol. 2018 Apr;14(4):405-412

293FT cells

5 µM

24 hours

Evaluate the degradation effect of dTRIM24 on TRIM24 protein, showing dose-dependent degradation

Nat Chem Biol. 2018 Apr;14(4):405-412

GBM#P3 cells

5, 10 μM

48 hours

inhibited tumorsphere formation and expression of stemness markers SOX2 and Nestin

J Transl Med. 2021 Dec 9;19(1):505

dTRIM24 动物实验

Species Chicken embryo ApoE−/− mice	Animal Model Chick embryo chorioallantoic membrane (CAM) model Atherosclerosis model	Administration	Dosage	Frequency	Description	References
Chicken embryo	Chick embryo chorioallantoic membrane (CAM) model	Topical administration	5 nM BTZ, 10 µM dTRIM24	Twice weekly until embryonic day 16	To evaluate the effect of dTRIM24 and BTZ combination therapy on tumor growth and metastasis, results showed the combination significantly inhibited tumor growth and metastasis.	Cell Death Discov. 2025 Mar 17;11(1):108
ApoE−/− mice	Atherosclerosis model	Intravenous injection	5 mg/kg	Every 3 days for 31 days	Evaluate the anti-atherosclerotic effects of MELT in vivo. Results showed MELT significantly reduced aortic plaque area (over 60% reduction) and promoted M2 macrophage polarization.	Acta Pharmacol Sin. 2023 Oct;44(10):1962-1976

Species

Chicken embryo ApoE−/− mice

Animal Model

Chick embryo chorioallantoic membrane (CAM) model Atherosclerosis model

Administration

Dosage

Frequency

Description

References

Chicken embryo

Chick embryo chorioallantoic membrane (CAM) model

Topical administration

5 nM BTZ, 10 µM dTRIM24

Twice weekly until embryonic day 16

To evaluate the effect of dTRIM24 and BTZ combination therapy on tumor growth and metastasis, results showed the combination significantly inhibited tumor growth and metastasis.

Cell Death Discov. 2025 Mar 17;11(1):108

ApoE−/− mice

Atherosclerosis model

Intravenous injection

5 mg/kg

Every 3 days for 31 days

Evaluate the anti-atherosclerotic effects of MELT in vivo. Results showed MELT significantly reduced aortic plaque area (over 60% reduction) and promoted M2 macrophage polarization.

Acta Pharmacol Sin. 2023 Oct;44(10):1962-1976

dTRIM24 参考文献

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	1113.3
SMILES Code	CC1=C(C2=CC=C(CNC([C@@H]3C[C@@H](O)CN3C([C@H](C(C)(C)C)NC(COCCOCCOCCNC(C4=CC=CC(S(=O)(NC5=CC(N(C)C(N6C)=O)=C6C=C5OC7=CC(OCCC)=CC=C7)=O)=C4)=O)=O)=O)=O)C=C2)SC=N1
MDL No.	MFCD31692370

别名
运输	蓝冰

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: 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：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

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dTRIM24 生物活性

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dTRIM24 参考文献

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dTRIM24 技术信息

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