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产品名称 | Bax ↓ ↑ | Bcl-2 ↓ ↑ | Bcl-B ↓ ↑ | Bcl-w ↓ ↑ | Bcl-xL ↓ ↑ | Bfl-1 ↓ ↑ | Mcl-1 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
BTSA1 | ✔ | 99%+ | |||||||||||||||||
HA14-1 |
+
Bcl-2, IC50: 9 μM |
98% | |||||||||||||||||
Venetoclax |
++++
Bcl-2, Ki: <0.01 nM |
99% | |||||||||||||||||
Navitoclax | 99%+ | ||||||||||||||||||
Obatoclax Mesylate |
+++
Bcl-2, Ki: 0.22 μM |
98% | |||||||||||||||||
ABT-737 |
+++
Bcl-2, EC50: 30.3 nM |
+
Bcl-B, EC50: 1.82 μM |
+++
Bcl-w, EC50: 197.8 nM |
+++
Bcl-xL, EC50: 78.7 nM |
99%+ | ||||||||||||||
Gambogic Acid |
+
Bfl-1, IC50: 1.06 μM Bcl-2, IC50: 1.21 μM |
++
Bcl-B, IC50: 0.66 μM |
++++
Bcl-w, IC50: 0.02 μM |
+
Bcl-xL, IC50: 1.47 μM |
+
Bfl-1, IC50: 1.06 μM |
++
Mcl-1, IC50: 0.79 μM |
Caspase | 99% HPLC | |||||||||||
BH3I-1 |
+
BH3-Bcl-xL interaction, Ki: 2.4 μM |
98% | |||||||||||||||||
A-1331852 |
++++
Bcl-xL, Ki: <0.01 nM |
99%+ | |||||||||||||||||
A-1210477 |
++++
MCL-1, IC50: 26.2 nM |
99%+ | |||||||||||||||||
Maritoclax | ✔ | 97% | |||||||||||||||||
TW-37 |
+++
Bcl-2, Ki: 0.29 μM |
+
Bcl-xL, Ki: 1.11 μM |
+++
Mcl-1, Ki: 0.26 μM |
98% | |||||||||||||||
UMI-77 |
++
Mcl-1, Ki: 490 nM |
97% | |||||||||||||||||
(R)-(-)-Gossypol acetic acid |
++
Bcl-2, Ki: 0.32 μM |
++
Bcl-xL, Ki: 0.48 μM |
+++
Mcl-1, Ki: 0.18 μM |
98% | |||||||||||||||
Sabutoclax |
++
Bfl-1, IC50: 0.62 μM Bcl-2, IC50: 0.32 μM |
++
Bcl-xL, IC50: 0.31 μM |
++
Bfl-1, IC50: 0.62 μM |
+++
Mcl-1, IC50: 0.20 μM |
98% | ||||||||||||||
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。 |
描述 | BCL6, a member of the BTB/POZ family of transcription factors, is the most frequently involved oncogene in diffuse large B cell lymphomas (DLBCLs) [2]. CID5721353 is an inhibitor of BCL6 with an IC50 value of 212 μM, which corresponds to a Ki of 147 μM PMID: 20385364. CID5721353 specifically disrupts BCL6 corepressor recruitment and can specifically reactivate BCL6 target genes in BCL6-dependent DLBCLs. It can also Selectively Kill BCL6-Dependent DLBCL Cells [2]. CID5721353 Suppresses Human DLBCL Xenografts in Mice. The levels of serum human β2-microglobulin (a surrogate marker of the xenograft burden) are significantly reduced by CID5721353 in the xenografted mice as compared with their respective controls for the OCI-Ly7 and SU-DHL6 xenografts (p=0.0117 and p=0.0004, respectively) [2]. |
作用机制 | CID5721353 binds to a Pocket in the Lateral Groove of the BCL6BTB Domain [2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.19mL 0.44mL 0.22mL |
10.93mL 2.19mL 1.09mL |
21.87mL 4.37mL 2.19mL |
CAS号 | 301356-95-6 |
分子式 | C15H9BrN2O6S2 |
分子量 | 457.276 |
别名 | BCL6 inhibitor |
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: 50 mg/mL(109.34 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 |