KU-57788是一种强效且选择性的 DNA-依赖性蛋白激酶 (DNA-PK) 抑制剂,IC50 为 14 nM,并在无细胞实验中抑制 PI3K,IC50 为 5 μM。NU7441在CRISPR-Cas9基因编辑中减少NHEJ的频率,并增加HDR的效率。


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| 产品名称 | DNA-PK ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| PI-103 |
++
DNA-PK, IC50: 23 nM |
99%+ | |||||||||||||||||
| CC-115 |
+++
DNA-PK, IC50: 0.013 μM |
mTOR | 98+% | ||||||||||||||||
| Samotolisib | ✔ | 99%+ | |||||||||||||||||
| NU 7026 |
+
DNA-PK, IC50: 0.23 μM |
PI3K | 98+% | ||||||||||||||||
| PIK-75 HCl |
++++
DNA-PK, IC50: 2 nM |
99%+ | |||||||||||||||||
| PP121 |
+
DNA-PK, IC50: 60 nM |
PDGFR,VEGFR | 99%+ | ||||||||||||||||
| KU-0060648 |
++++
DNA-PK, IC50: 5 nM |
98% | |||||||||||||||||
| KU-57788 |
+++
DNA-PK, IC50: 14 nM |
99%+ | |||||||||||||||||
| LTURM34 |
++
DNA-PK, IC50: 0.034 μM |
98%+ | |||||||||||||||||
| SF2523 |
+++
DNA-PK, IC50: 9 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。 | |||||||||||||||||||
| 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 |
+++
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 |
++++
BRD9, IC50: 19 nM BRD7, IC50: 117 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 |
+
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 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 |
+++
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% | |||||||||||||||||
| 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 |
++
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 |
++
BRPF1, IC50: 80 nM BRPF2, IC50: 7.9 μM |
99%+ | |||||||||||||||||
| OF-1 |
++
BRPF1B, Kd: 100 nM BRPF2, Kd: 500 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 |
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 |
++++
EP300, IC50: 38 nM CREBBP, IC50: 21 nM |
99%+ | |||||||||||||||||
| Nordihydroguaiaretic acid | ✔ | HER2,IGF-1R | 99%+ | ||||||||||||||||
| Curcumin |
+
p300, IC50: ~25 μM |
Nrf2,Ferroptosis,NF-κB | 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。 | |||||||||||||||||||
| 产品名称 | C2β ↓ ↑ | p110α ↓ ↑ | p110β ↓ ↑ | p110γ ↓ ↑ | p110δ ↓ ↑ | PI3K ↓ ↑ | Vps34 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| A66 |
+
C2β, IC50: 462 nM |
++
p110α, IC50: 32 nM |
99%+ | ||||||||||||||||
| Taselisib |
+
C2β, IC50: 292 nM |
++++
PI3Kα, Ki: 0.29 nM |
+++
PI3Kβ, Ki: 9.1 nM |
++++
PI3Kγ, Ki: 0.97 nM |
++++
PI3Kδ, Ki: 0.12 nM |
+
hVps34, IC50: 374 nM |
99%+ | ||||||||||||
| Gedatolisib |
++++
PI3Kα, IC50: 0.4 nM |
+++
PI3Kγ, IC50: 5.4 nM |
mTOR | 99% | |||||||||||||||
| HS-173 |
++++
PI3Kα , IC50: 0.8 nM |
99%+ | |||||||||||||||||
| Serabelisib |
+++
PI3Kα, IC50: 21 nM |
99%+ | |||||||||||||||||
| GNE-477 |
++++
PI3Kα, IC50: 4 nM |
mTOR | 99% | ||||||||||||||||
| YM-201636 |
+
p110α, IC50: 3.3 μM |
PIKfyve | 98% | ||||||||||||||||
| AS-252424 |
+
PI3Kα, IC50: 935 nM |
++
PI3Kγ, IC50: 33 nM |
99% | ||||||||||||||||
| Alpelisib |
+++
PI3Kα, IC50: 5 nM |
99%+ | |||||||||||||||||
| AS-604850 |
+
PI3Kα, IC50: 4.5 μM |
+
PI3Kγ, IC50: 0.25 μM |
99% | ||||||||||||||||
| SF2523 |
++
PI3Kα, IC50: 34 nM |
++
PI3Kγ, IC50: 158 nM |
mTOR,DNA-PK | 99%+ | |||||||||||||||
| Inavolisib |
++++
PI3K alpha, IC50: 0.038 nM |
99%+ | |||||||||||||||||
| Bimiralisib |
++++
PI3Kα, Kd: 1.5 nM |
+++
PI3Kβ, Kd: 11 nM |
++
PI3Kγ, Kd: 25 nM |
++
PI3Kδ, Kd: 25 nM |
mTOR | 99%+ | |||||||||||||
| GSK1059615 |
++++
PI3Kα, IC50: 0.4 nM |
++++
PI3Kβ, IC50: 0.6 nM |
+++
PI3Kγ, IC50: 5 nM |
++++
PI3Kδ, IC50: 2 nM |
mTOR | 98% | |||||||||||||
| GSK2636771 | ✔ | 99% | |||||||||||||||||
| Fimepinostat |
+++
PI3Kα, IC50: 19 nM |
++
PI3Kβ, IC50: 54 nM |
++
PI3Kδ, IC50: 39 nM |
99%+ | |||||||||||||||
| VS-5584 |
++++
PI3Kα, IC50: 2.6 nM |
+++
PI3Kβ, IC50: 21 nM |
++++
PI3Kγ, IC50: 3.0 nM |
++++
PI3Kδ, IC50: 2.7 nM |
mTOR | 98% | |||||||||||||
| Dactolisib |
++++
p110α1, IC50: 4 nM |
++
p110β, IC50: 75 nM |
+++
p110γ, IC50: 5 nM |
+++
p110δ, IC50: 7 nM |
98+% | ||||||||||||||
| PI-103 |
++++
p110α, IC50: 2 nM |
++++
p110β, IC50: 3 nM |
+++
p110γ, IC50: 15 nM |
++++
p110δ, IC50: 3 nM |
mTOR,DNA-PK | 99%+ | |||||||||||||
| PI-3065 |
+
p110β, IC50: 1078 nM |
+++
p110δ, IC50: 15 nM |
99%+ | ||||||||||||||||
| Voxtalisib |
++
PI3Kα, IC50: 39 nM |
++
PI3Kβ, IC50: 113 nM |
+++
PI3Kγ, IC50: 9 nM |
++
PI3Kδ, IC50: 43 nM |
mTOR,DNA-PK | 99%+ | |||||||||||||
| AZD-8835 |
+++
PI3Kα, IC50: 6.2 nM |
+
PI3Kβ, IC50: 431 nM |
++
PI3Kγ, IC50: 90 nM |
+++
PI3Kδ, IC50: 5.7 nM |
99% | ||||||||||||||
| Pilaralisib analogue |
++
PI3Kα, IC50: 39 nM |
++
PI3Kβ, IC50: 36 nM |
+++
PI3Kγ, IC50: 23 nM |
++
PI3Kδ, IC50: 36 nM |
99%+ | ||||||||||||||
| ZSTK474 |
+++
PI3Kα, IC50: 16 nM |
++
PI3Kβ, IC50: 44 nM |
++
PI3Kγ, IC50: 49 nM |
+++
PI3Kδ, IC50: 4.6 nM |
++
PI3K, IC50: 37 nM |
98% | |||||||||||||
| AS-605240 |
++
PI3Kα, IC50: 60 nM |
+
PI3Kβ, IC50: 270 nM |
+++
PI3Kγ, IC50: 8 nM |
+
PI3Kδ, IC50: 300 nM |
98% | ||||||||||||||
| TGX-221 |
+++
p110β, IC50: 5 nM |
++
p110δ, IC50: 0.1 μM |
99%+ | ||||||||||||||||
| PF-04691502 |
++++
PI3Kα, Ki: 1.8 nM |
++++
PI3Kβ, Ki: 2.1 nM |
++++
PI3Kγ, Ki: 1.9 nM |
++++
PI3Kδ, Ki: 1.6 nM |
mTOR | 98+% | |||||||||||||
| GDC-0084 |
++++
PI3Kα, Ki app: 2 nM |
++
PI3Kβ, Ki app: 46 nM |
+++
PI3Kγ, Ki app: 10 nM |
++++
PI3Kδ, Ki app: 3 nM |
mTOR | 99%+ | |||||||||||||
| Buparlisib |
++
p110α, IC50: 52 nM |
+
p110β, IC50: 166 nM |
+
p110γ, IC50: 262 nM |
++
p110δ, IC50: 116 nM |
+
Vps34, IC50: 2.4 μM |
mTOR | 98% | ||||||||||||
| LY294002 |
+
p110α, IC50: 0.5 μM |
+
p110β, IC50: 0.97 μM |
+
p110δ, IC50: 0.57 μM |
DNA-PK | 99%+ | ||||||||||||||
| AZD 6482 |
+
PI3Kα, IC50: 870 nM |
+++
PI3Kβ, IC50: 10 nM |
++
PI3Kδ, IC50: 80 nM |
DNA-PK | 99%+ | ||||||||||||||
| Pictilisib |
++++
p110α, IC50: 3 nM |
++
p110β, IC50: 33 nM |
++
p110γ, IC50: 75 nM |
++++
p110δ, IC50: 3 nM |
mTOR | 99%+ | |||||||||||||
| PKI-402 |
++++
PI3Kα, IC50: 2 nM |
+++
PI3Kβ, IC50: 7 nM |
+++
PI3Kγ, IC50: 16 nM |
+++
PI3Kδ, IC50: 14 nM |
mTOR | 98% | |||||||||||||
| Copanlisib |
++++
PI3Kα, IC50: 0.5 nM |
++++
PI3Kβ, IC50: 3.7 nM |
+++
PI3Kγ, IC50: 6.4 nM |
++++
PI3Kδ, IC50: 0.7 nM |
99%+ | ||||||||||||||
| Omipalisib |
++++
p110α, Ki: 0.019 nM |
++++
p110β, Ki: 0.13 nM |
++++
p110γ, Ki: 0.06 nM |
++++
p110δ, Ki: 0.024 nM |
99%+ | ||||||||||||||
| Izorlisib |
+++
PI3Kα, IC50: 14 nM |
++
PI3Kβ, IC50: 0.12 μM |
++
PI3Kγ, IC50: 36 nM |
+
PI3Kδ, IC50: 0.50 μM |
99%+ | ||||||||||||||
| AZD8186 |
++
PI3Kα, IC50: 35 nM |
++++
PI3Kβ, IC50: 4 nM |
+++
PI3Kδ, IC50: 12 nM |
99% | |||||||||||||||
| KU-0060648 |
++++
PI3Kα, IC50: 4 nM |
++++
PI3Kβ, IC50: 0.5 nM |
+
PI3Kγ, IC50: 0.59 μM |
++++
PI3Kδ, IC50: 0.1 nM |
DNA-PK | 98% | |||||||||||||
| Apitolisib |
+++
p110α, IC50: 5 nM |
++
p110β, IC50: 27 nM |
+++
p110γ, IC50: 14 nM |
+++
p110δ, IC50: 7 nM |
mTOR | 98%+ | |||||||||||||
| CZC24832 |
+
PI3Kβ, IC50: 1.1 μM |
++
PI3Kγ, IC50: 27 nM |
98+% | ||||||||||||||||
| BGT226 maleate |
++++
PI3Kα, IC50: 4 nM |
++
PI3Kβ, IC50: 63 nM |
++
PI3Kγ, IC50: 38 nM |
mTOR | 99%+ | ||||||||||||||
| TG 100713 |
++
PI3Kα, IC50: 165 nM |
+
PI3Kβ, IC50: 215 nM |
++
PI3Kγ, IC50: 50 nM |
+++
PI3Kδ, IC50: 24 nM |
98%+ | ||||||||||||||
| PI3K-IN-1 |
++
PI3Kα, IC50: 39 nM |
++
PI3Kβ, IC50: 113 nM |
+++
PI3Kγ, IC50: 9 nM |
++
PI3Kδ, IC50: 43 nM |
mTOR,DNA-PK | 98+% | |||||||||||||
| TG100-115 |
+
PI3Kα, IC50: 1.3 μM |
+
PI3Kβ, IC50: 1.2 μM |
++
PI3Kγ, IC50: 83 nM |
+
PI3Kδ, IC50: 235 nM |
98% | ||||||||||||||
| PIK-90 |
+++
PI3Kα, IC50: 11 nM |
+
PI3Kβ, IC50: 350 nM |
+++
PI3Kγ, IC50: 18 nM |
++
PI3Kδ, IC50: 58 nM |
99%+ | ||||||||||||||
| PIK-294 |
+
p110β, IC50: 490 nM |
++
p110γ, IC50: 160 nM |
+++
p110δ, IC50: 10 nM |
99%+ | |||||||||||||||
| Duvelisib |
++++
PI3Kβ, Ki: 1564 pM |
++
PI3Kγ, Ki: 243 pM |
++++
PI3Kδ, Ki: 23 pM |
99%+ | |||||||||||||||
| GDC-0326 |
++++
PI3Kα, Ki: 0.2 nM |
++
PI3Kβ, Ki: 26.6 nM |
+++
PI3Kγ, Ki: 10.2 nM |
++++
PI3Kδ, Ki: 4 nM |
98% | ||||||||||||||
| Quercetin Dihydrate |
+
PI3Kβ, IC50: 5.4 μM |
+
PI3Kγ, IC50: 2.4 μM |
+
PI3Kδ, IC50: 3.0 μM |
95% | |||||||||||||||
| Quercetin |
+
PI3Kβ, IC50: 5.4 μM |
+
PI3Kγ, IC50: 2.4 μM |
+
PI3Kδ, IC50: 3.0 μM |
PKC,Src,Sirtuin | 95% | ||||||||||||||
| Leniolisib |
+
PI3Kα, IC50: 0.244 μM |
+
PI3Kβ, IC50: 0.424 μM |
+
PI3Kγ, IC50: 2.23 μM |
+++
PI3Kδ, IC50: 0.011 μM |
DNA-PK | 99%+ | |||||||||||||
| PIK-108 | ✔ | 99% | |||||||||||||||||
| Eganelisib |
+++
PI3Kγ, IC50: 16 nM |
99%+ | |||||||||||||||||
| CAY10505 | ✔ | 99% | |||||||||||||||||
| IPI-3063 |
++++
p110δ, IC50: 2.5 nM |
99% | |||||||||||||||||
| Nemiralisib |
++++
PI3Kδ, pKi: 9.9 |
99%+ | |||||||||||||||||
| PF-4989216 |
++++
p110α, IC50: 2 nM |
++
p110γ, IC50: 65 nM |
++++
p110δ, IC50: 1 nM |
99%+ | |||||||||||||||
| PIK-75 HCl |
+++
p110α, IC50: 5.8 nM |
++
p110γ, IC50: 76 nM |
+
p110δ, IC50: 0.51 μM |
DNA-PK | 99%+ | ||||||||||||||
| Tenalisib |
++
PI3Kγ, IC50: 33.2 nM |
++
PI3Kδ, IC50: 24.5 nM |
98% | ||||||||||||||||
| Acalisib |
+++
p110δ, IC50: 14 nM |
99%+ | |||||||||||||||||
| Umbralisib |
+++
PI3Kδ, IC50: 22.2 nM |
99%+ | |||||||||||||||||
| AMG319 |
+
PI3Kγ, IC50: 850 nM |
+++
PI3Kδ, IC50: 18 nM |
99% | ||||||||||||||||
| IC-87114 |
+
PI3Kγ, IC50: 29 μM |
+
PI3Kδ, IC50: 0.5 μM |
99%+ | ||||||||||||||||
| Idelalisib |
++
p110γ, IC50: 89 nM |
++++
p110δ, IC50: 2.5 nM |
98% | ||||||||||||||||
| PIK-293 |
+
p110γ, IC50: 10 μM |
+
p110δ, IC50: 0.24 μM |
99%+ | ||||||||||||||||
| Vps34-PIK-III |
+
PI3Kδ, IC50: 1.2μM |
+++
Vps34, IC50: 0.018μM |
99%+ | ||||||||||||||||
| GSK2292767 | ✔ | 98% | |||||||||||||||||
| Seletalisib |
+
PI3Kγ, IC50: 282 nM |
+++
PI3Kδ, IC50: 12 nM |
99%+ | ||||||||||||||||
| P110δ-IN-1 |
++++
P110δ, IC50: 0.6 nM |
99% | |||||||||||||||||
| PI3Kδ-IN-5 |
++++
PI3Kδ, IC50: 0.9 nM |
99% | |||||||||||||||||
| SRX3207 |
+
PI3K alpha, IC50: 244 nM |
+
PI3K gamma, IC50: 9790 nM |
+
PI3K delta, IC50: 388 nM |
Syk | 98% | ||||||||||||||
| Parsaclisib HCl |
++++
PI3Kδ, IC50: 1 nM |
98% | |||||||||||||||||
| IHMT-PI3Kδ-372 |
+++
PI3Kδ, IC50: 14 nM |
98% | |||||||||||||||||
| Trigonelline | ✔ | Akt | 99%+ | ||||||||||||||||
| Wortmannin |
++++
PI3K, IC50: 3 nM |
MLCK,DNA-PK | 99%+ | ||||||||||||||||
| Samotolisib | ✔ | DNA-PK | 99%+ | ||||||||||||||||
| GNE-317 | ✔ | 99%+ | |||||||||||||||||
| Oroxin B | ✔ | PTEN,Akt | 99%+ | ||||||||||||||||
| NU 7026 |
+
PI3K, IC50: 13 μM |
DNA-PK | 98+% | ||||||||||||||||
| Deguelin | ✔ | Akt | 99%+ | ||||||||||||||||
| Ailanthone | ✔ | Akt,ATM/ATR,CDK | 98% | ||||||||||||||||
| Resibufogenin | ✔ | ROS | 98% | ||||||||||||||||
| KU-57788 |
+
PI3K, IC50: 5 μM |
mTOR,DNA-PK | 99%+ | ||||||||||||||||
| Cinobufagine | ✔ | Akt | 99% | ||||||||||||||||
| α-Linolenic acid | ✔ | 97% (GC) | |||||||||||||||||
| MTX-211 | ✔ | EGFR | 98% | ||||||||||||||||
| PI3K/mTOR Inhibitor-2 |
++++
PI3K, IC50: 3.4 nM |
mTOR | 99%+ | ||||||||||||||||
| SPP-86 | ✔ | 99%+ | |||||||||||||||||
| (E)-Akt inhibitor-IV | ✔ | 98% | |||||||||||||||||
| Vps34-IN-1 |
++
Vps34, IC50: 25 nM |
98% | |||||||||||||||||
| SAR405 |
++++
Vps34, IC50: 1.2 nM |
98+% | |||||||||||||||||
| 3-Methyladenine |
+
PI3Kγ, IC50: 60 μM |
+
Vps34, IC50: 25 μM |
Autophagy | 98% | |||||||||||||||
| Vps34-IN-4 |
+++
VPS34, IC50: 15 nM |
98%+ | |||||||||||||||||
| Autophinib |
+++
Vps34, IC50: 19 nM |
Autophagy | 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 | NU7441 increases the persistence of γH2AX foci after ionizing radiation–induced or etoposide-induced DNA damage. NU7441 (0.5 μM or 1 μM) appreciably increases G2-M accumulation induced by ionizing radiation, etoposide, and doxorubicin in both SW620 and LoVo cells. NU7441 causes persistence of doxorubicin- and ionising radiation-induced DNA double-strand break and also slightly decreases homologous recombination activity DNA-PK-proficient M059-Fus-1 and DNA-PK-deficient M059 J human tumour cells. NU7441 inhibits UV-induced RPA p34 hyperphosphorylation in a dose-dependent manner both in cells lacking and cells expressing polymerase η. NU7441 increases levels of fludarabine-induced γH2AX foci and correspondingly decreased fludarabine-induced cell death in chronic lymphocytic leukemia cells. NU7441 also inhibits mitoxantrone-induced DNA-PKcs autophosphorylation and repair in chronic lymphocytic leukemia cells. It reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage. |
| Concentration | Treated Time | Description | References | |
| SLK cells | 15 μM | 2 h | To evaluate the effect of KU-57788 on KSHV circularization in SLK cells. Results showed that KU-57788 significantly reduced KSHV circularization efficiency. | Nucleic Acids Res. 2024 Feb 28;52(4):1814-1829. |
| HDMVEC cells | 15 μM | 2 h | To evaluate the effect of KU-57788 on KSHV circularization in HDMVEC cells. Results showed that KU-57788 significantly reduced KSHV circularization efficiency. | Nucleic Acids Res. 2024 Feb 28;52(4):1814-1829. |
| GBM cells | 1 μM | KU-57788 inhibited the activation of DNA-PKcs, reducing TMZ-induced DNA damage repair, thereby enhancing the cytotoxicity of TMZ on GBM cells. | Cell Res. 2021 Oct;31(10):1072-1087. | |
| SAS cells | 5 μM | 1 h | Inhibited NHEJ repair of radiation-induced DSBs, TGF β inhibition partially rescued the repair | Sci Transl Med. 2021 Feb 10;13(580):eabc4465. |
| U2OS cells | 2 μM | 2 h | To inhibit DNA-PK activity and study its effect on the induction of pUbT12 foci | Mol Cell. 2020 Nov 5;80(3):423-436.e9. |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | Ovarian cancer peritoneal metastasis model | Oral | 60 mg/kg | Once daily for 21 days | To evaluate the in vivo efficacy of HIPET combined with WEE1 inhibitor | Nat Commun. 2024 Mar 7;15(1):2089 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.42mL 0.48mL 0.24mL |
12.09mL 2.42mL 1.21mL |
24.18mL 4.84mL 2.42mL |
|
| CAS号 | 503468-95-9 |
| 分子式 | C25H19NO3S |
| 分子量 | 413.49 |
| SMILES Code | O=C1C=C(N2CCOCC2)OC3=C(C4=C5C(C6=CC=CC=C6S5)=CC=C4)C=CC=C13 |
| MDL No. | MFCD11983069 |
| 别名 | NU7441 |
| 运输 | 蓝冰 |
| InChI Key | JAMULYFATHSZJM-UHFFFAOYSA-N |
| Pubchem ID | 11327430 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, store in freezer, under -20°C |
| 溶解方案 |
DMSO: 15 mg/mL(36.28 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 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
|
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