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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| 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+ |


| 规格 | 价格 | 会员价 | 库存 | 数量 | |||
|---|---|---|---|---|---|---|---|
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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%+ | |||||||||||||||||
| Oxolinic acid | ✔ | 98+% | |||||||||||||||||
| 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 |
+
BLM636-1298, IC50: 0.97 μM BLMfull-length, IC50: 2.98 μM |
99%+ | |||||||||||||||||
| RK-33 | ✔ | 98% | |||||||||||||||||
| Brr2-IN-3 | ✔ | 99%+ | |||||||||||||||||
| Phen-DC3 Trifluoromethanesulfonate | ✔ | 98% | |||||||||||||||||
| Favipiravir | ✔ | 99% | |||||||||||||||||
| Suramin sodium salt |
++
RdRp, IC50: 0.26 μM |
99%+ | |||||||||||||||||
| Clofarabine |
++
Ribonucleotide reductase, IC50: 65 nM |
97% | |||||||||||||||||
| Didox | ✔ | 98% | |||||||||||||||||
| (E)-3-AP | ✔ | 99% | |||||||||||||||||
| Halofuginone |
+++
prolyl-tRNA synthetase, Ki: 18.3nM |
99%+ | |||||||||||||||||
| BC-LI-0186 |
+++
Leucyl-tRNA synthetase, IC50: 46.11 nM Leucyl-tRNA synthetase, Kd: 42.1 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。 | |||||||||||||||||||
| 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]. |
| 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 |
|
| CAS号 | 688342-78-1 |
| 分子式 | C23H36N6S |
| 分子量 | 428.64 |
| SMILES Code | S=C(NC1=CC=C2N=C(N3CCN(CC)CC3)C=C(C)C2=C1)NCCN(CC)CC |
| MDL No. | MFCD14739485 |
| 别名 | |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
| 溶解方案 |
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 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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