1. Epigenetics PROTAC
  2. Histone Acetyltransferase Epigenetic Reader Domain PROTACs
  3. BT-O2C

BT-O2C 是一种具有高选择性的 p300 PROTAC 降解剂。BT-O2C 可以显著降解 HAP1 细胞中 p300 的水平。BT-O2C 在 CIC:DUX4 肉瘤 (CDS) 细胞系中具有显著的细胞毒性 (IC50 = 152-221 nM) 并且显著减少 CDS 靶基因 (ETV1, ETV4, ETV5) 的表达。BT-O2C 可用于癌症的研究。(粉色: p300 配体 (HY-174868); 蓝色: CRBN 配体 (HY-W023573); 黑色: 连接子; CRBN 配体+连接子 (HY-174869))。

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BT-O2C

BT-O2C Chemical Structure

CAS No. : 3055107-34-8

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5 mg ¥11400
10 - 12 周
10 mg 询价 10 - 12 周
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生物活性

BT-O2C is a highly selective p300 PROTAC degrader. BT-O2C can significantly degrade the level of p300 in HAP1 cells. BT-O2C has significant cytotoxicity in CIC:DUX4 sarcoma (CDS) cell lines (IC50 ranges from 152 to 221 nM) and significantly reduces the expression of CDS target genes (ETV1, ETV4, ETV5). BT-O2C can be used for research on cancer. (Pink: p300 Ligand (HY-174868); Blue: CRBN Ligand (HY-W023573); Black: Linker; CRBN Ligand+Linker (HY-174869))[1].

IC50 & Target[1]

p300

 

Cereblon

 

体外研究
(In Vitro)

BT-O2C (0.1-10 μM,24 小时) 在 HAPI 细胞中可以显著降解 p300,对 CBP 的降解作用微弱[1]
BT-O2C (0.25-4 μM,48-72 小时) 在 NCC-CDS-X1 (IC50 = 152 nM) 和 KITRA (IC50 = 221 nM) 细胞中表现出显著的细胞毒性[1]
BT-O2C (4 μM,6 小时) 显著降低 NCC-CDS-X1 中 CDS 靶基因的表达[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: HAPI cells
Concentration: 0.1, 1 and 10 μM
Incubation Time: 24 h
Result: Selectively degraded the protein level of p300, superior to JQAD1 (HY-145765).

RT-PCR[1]

Cell Line: NCC-CDS-X1 cells
Concentration: 4 μM
Incubation Time: 6 h
Result: Significantly reduced the expression of ETV1, ETV4, ETV5, CCNEE1 and MYC.
分子量

973.94

Formula

C48H48F5N9O8

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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BT-O2C
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HY-174866
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