货号:A650610 同义名: PRI-724;C-82 prodrug
PRI-724 is a selective inhibitor of the CBP/β-catenin interaction.
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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 |
99+% | |||||||||||||||||
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 (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 |
+++
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 |
++++
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 |
++++
BRD3-BD1, IC50: 9 nM BRD4-BD1, IC50: 119 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 | 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 |
++
BAZ2A, Kd: 257 nM BAZ2B, Kd: 136 nM |
99%+ | |||||||||||||||||
KG-501 | ✔ | 99%+ | |||||||||||||||||
UNC 669 |
+
L3MBTL4, IC50: 6 μM L3MBTL3, IC50: 35 μM |
98% | |||||||||||||||||
PFI-3 |
+++
SMARCA2A, Kd: 72 nM SMARCA4, Kd: 55 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 |
++++
EP300, IC50: 38 nM CREBBP, IC50: 21 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。 |
靶点 |
|
描述 | PRI-724 is a selective inhibitor of the CBP/β-catenin interaction. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT01606579 | Acute Myeloid Leukemia ... 展开 >> Chronic Myeloid Leukemia 收起 << | Phase 1 Phase 2 | Completed | - | United States, Georgia ... 展开 >> Emory University / Winship Cancer Institute Atlanta, Georgia, United States, 30322 United States, Massachusetts University of Massachusetts Medical Center Worcester, Massachusetts, United States, 01655 United States, New Mexico New Mexico Cancer Care Alliance Albuquerque, New Mexico, United States, 87106 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27710 United States, Ohio Ohio State University Columbus, Ohio, United States, 43210-1267 United States, Texas University of Texas M.D. Anderson Cancer Center Houston, Texas, United States, 77030 收起 << |
NCT02195440 | Hepatitis C Virus-infected Cir... 展开 >>rhosis 收起 << | Phase 1 | Completed | - | Japan ... 展开 >> Tokyo metropolitan Komagome Hospital Tokyo, Japan 收起 << |
NCT02413853 | Colorectal Adenocarcinoma ... 展开 >> Stage IVA Colorectal Cancer Stage IVB Colorectal Cancer 收起 << | Phase 2 | Withdrawn(Study drug supply is... 展开 >>sues) 收起 << | November 2018 | United States, California ... 展开 >> USC Norris Comprehensive Cancer Center Los Angeles, California, United States, 90033 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.52mL 0.30mL 0.15mL |
7.59mL 1.52mL 0.76mL |
15.18mL 3.04mL 1.52mL |
CAS号 | 1422253-38-0 |
分子式 | C33H35N6O7P |
分子量 | 658.641 |
别名 | PRI-724;C-82 prodrug;ICG-001 analog |
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 | |
动物实验配方 |