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D-I03 {[allProObj[0].p_purity_real_show]}

货号:A1145758

D-I03 是一种选择性的 RAD52 抑制剂,其 Kd 为 25.8 μM。D-I03 抑制 RAD52 依赖的单链重组 (SSA) 和 D 环形成,IC50 值分别为 5 μM 和 8 μM。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
D-I03 化学结构 CAS号:688342-78-1
D-I03 化学结构
CAS号:688342-78-1
D-I03 3D分子结构
CAS号:688342-78-1
D-I03 化学结构 CAS号:688342-78-1
D-I03 3D分子结构 CAS号:688342-78-1
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D-I03 纯度/质量文件 产品仅供科研

货号:A1145758 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 DNA synthesis helicase RdRp ribonucleotide reductase tRNA synthetase YB-1 其他靶点 纯度
Fexinidazole 98%
Daptomycin 98%
Blasticidin S·HCl 98%
Metronidazole 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

98%
Triglycidyl isocyanurate p53 98+%
Nedaplatin 99%+
Bendamustine 98+%
Trifluridine 98%
Robinetin 99%+
Carboplatin 99%
Cidofovir 99%
Cisplatin 99%
Cytarabine ++++

DNA synthesis, IC50: 16 nM

98%
Acelarin ++++

DNA synthesis, EC50: 0.2 nM

99%+
Oxaliplatin 98%
YK-4-279 99%+
ML216 +

BLMfull-length, IC50: 2.98 μM

BLM636-1298, IC50: 0.97 μM

99%+
RK-33 98%
Brr2-IN-3 99%+
Phen-DC3 Trifluoromethanesulfonate 98%
Favipiravir 97%
Suramin sodium salt ++

RdRp, IC50: 0.26 μM

99%+
Clofarabine ++

Ribonucleotide reductase, IC50: 65 nM

97%
Didox 98%
(E)-3-AP 97%
Halofuginone +++

prolyl-tRNA synthetase, Ki: 18.3nM

99%+
BC-LI-0186 +++

Leucyl-tRNA synthetase, Kd: 42.1 nM

Leucyl-tRNA synthetase, IC50: 46.11 nM

98%
SU056 +

YB-1, IC50: 1.73 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。

D-I03 生物活性

描述 D-I03, with a KD of 25.8 µM, is a selective inhibitor of RAD52. It specifically targets RAD52-dependent single-strand annealing (SSA) and D-loop formation, with IC50s of 5 µM and 8 µM, respectively. D-I03 inhibits the growth of BRCA1- and BRCA2-deficient cells, and prevents the formation of damage-induced RAD52 foci, while not affecting RAD51 foci induced by Cisplatin[1][2].
体内研究

Treatment with D-I03 (50 mg/kg/day; intraperitoneal injection; daily; for 7 days) decreases the growth of BRCA1-deficient MDA-MB-436 tumors in nu/nu mice. The combination of talazoparib and D-I03 does not impact the growth of BRCA1-proficient tumors and does not cause significant toxicity to normal tissues and organs[3].

Pharmacokinetic and toxicity studies show that the maximum tolerated dose of D-I03 is ≥50 mg/kg, with a half-life (t1/2) of 23.4 hours, leading to a maximal concentration of >1 μM in peripheral blood[1].

体外研究

Treatment with D-I03 (0-10 μM; on days 1 and 3; Capan-1 and UWB1.289 cells) selectively inhibited the growth of Capan-1 and UWB1.289 cells in a concentration-dependent manner[1].

D-I03 inhibits RAD52 foci formation induced by cisplatin in BCR-ABL1-positive BRCA1-deficient 32Dcl3 murine hematopoietic cells expressing GFP-RAD52. In the presence of D-I03 (2.5 μM), the percentage of cells with RAD52 foci decreases from 38.7% to 17.1%, while the percentage of cisplatin-treated cells without foci increases from 48.4% to 71.9%. D-I03 has no effect on RAD51 foci induced by cisplatin. Moreover, D-I03 alone neither induces RAD51 foci nor RAD52 foci (in BRCA1-deficient cells), indicating its low genotoxicity[1].

D-I03 参考文献

[1]Huang F, et al. Targeting BRCA1- and BRCA2-deficient cells with RAD52 small molecule inhibitors. Nucleic Acids Res. 2016 May 19;44(9):4189-99.

[2]Hengel SR, et al. Small-Molecule Inhibitors Targeting DNA Repair and DNA Repair Deficiency in Research and Cancer Therapy. Cell Chem Biol. 2017 Sep 21;24(9):1101-1119.

[3]Sullivan-Reed K, et al. Simultaneous Targeting of PARP1 and RAD52 Triggers Dual Synthetic Lethality in BRCA-Deficient Tumor Cells. Cell Rep. 2018 Jun 12;23(11):3127-3136.

D-I03 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.33mL

0.47mL

0.23mL

11.66mL

2.33mL

1.17mL

23.33mL

4.67mL

2.33mL

D-I03 技术信息

CAS号688342-78-1
分子式C23H36N6S
分子量 428.637
别名
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(116.65 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

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