Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T10601 |
BRCA1-IN-2
|
Others | Others |
BRCA1-IN-2 是一种可穿过细胞膜的 BRCA1 蛋白-蛋白相互作用(PPI)抑制剂,具有抗肿瘤活性,通过破坏 BRCA1 (BRCT)2 与蛋白质的相互作用来发挥作用。 | |||
T10600 |
BRCA1-IN-1
|
Others | Others |
BRCA1-IN-1 is a novel small-molecule-like inhibitor of BRCA1 (IC50: 0.53 μM; Ki: 0.71 μM). | |||
T8873 |
Bractoppin
|
Others; DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Others |
Bractoppin 是一种BRCA1 (t)BRCT domain 识别磷酸肽的选择性抑制剂,IC50为 74 nM。它优先抑制 BRCA1 -tBRCT 依赖的 DNA 损伤。它减少 BRCA1 对 DNA 断裂片段的招募,进而抑制损伤诱导的 G2 期阻滞和重组酶 RAD51 的组装。 | |||
T16807 |
Rucaparib monocamsylate
瑞卡帕布樟脑磺酸盐,Rucaparib Camsylate |
PARP | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Rucaparib monocamsylate (Rucaparib Camsylate) 是一种口服有效的 PARP 蛋白抑制剂,对 PARP-1 的Ki 为 1.4 nM。它是六磷酸己糖脱氢酶 (H6PD) 抑制剂,有用于去势抵抗性前列腺癌 (CRPC) 的研究潜力。 | |||
T6253 |
Talazoparib
LT-673,BMN-673,他拉唑帕利 |
PARP | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Talazoparib (LT-673) 是一种具有口服活性的 PARP 1/2抑制剂,IC50为0.58 nM,具有抗肿瘤活性。它抑制 PARP1 和 PARP2 酶活性的 Ki 值分别为 1.2 nM 和 0.87 nM。 | |||
T4463 |
Rucaparib
AG-14447,PF-01367338,瑞卡帕布,AG014699 |
PARP | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Rucaparib (PF-01367338) 是一种口服有效的 PARP 蛋白抑制剂,对 PARP-1 的 Ki 为 1.4 nM。它是六磷酸己糖脱氢酶 (H6PD) 抑制剂,有用于去势抵抗性前列腺癌 (CRPC) 的研究潜力。 | |||
T6127 |
Rucaparib Phosphate
AG-014699 phosphate,PF-01367338,芦卡帕利,AG-014699,瑞卡帕布磷酸盐,PF-01367338 phosphate |
PARP | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Rucaparib Phosphate (PF-01367338 phosphate) 是一种口服有效的PARP 蛋白抑制剂,对 PARP-1 的Ki 为 1.4 nM。它是六磷酸己糖脱氢酶 (H6PD) 抑制剂,有用于去势抵抗性前列腺癌 (CRPC) 的研究潜力。 | |||
T10936 |
D-I03
DI03 |
DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
D-I03 是一种选择性的RAD52 抑制剂,Kd 为 25.8 µM。D-I03 抑制 RAD52 依赖性单链退火 (SSA) 和 D 环形成,IC50 分别为 5 µM 和 8 µM。D-I03 抑制 BRCA1 和 BRCA2 缺陷细胞的生长,并抑制顺铂诱导的 RAD52 病灶形成,但对 RAD51 无影响。 | |||
T73343 | BAP1-IN-1 | ||
BAP1-IN-1 是一种 BRCA1 相关蛋白 1 (BAP1) 催化活性抑制剂,其IC50为 0.1-1 μM。 | |||
T71757 | SC-10914 | ||
SC10914 is a highly potent PARP inhibitor (PARP1 IC50 = 7.87 nM) with potent anti-proliferative activity against human BRCA deficient tumor cells (MDA-MB-436, BRCA1 deficient, IC50 = 4.03 nM, Capan-1 BRCA2 deficient, IC50 = 11.66 nM) and PTEN deficient tumor cells (HGC-27,PTEN deficient, IC50 = 0.35 μM). SC10914 showed potent anti-tumor activity in BRCA1/2 mutant tumor models and better pharmacokinetics profile has the potential to be selected as the clinical candidate for the treatment of treat... | |||
TP2299 |
tumor protein p53 binding protein fragment [Homo sapiens]/[Mus musculus]
|
Others | Others |
Tumor protein p53 binding protein (53BP1) has been identified in a yeast two-hybrid screen as a protein that interacts with the central DNA–binding domain of p532. Similar to breast cancer susceptibility gene 13, 4 (BRCA1; 53BP1 enhances p53-dependent tra | |||
T79593 | PARP1-IN-14 | PARP | Chromatin/Epigenetic; DNA Damage/DNA Repair |
PARP1-IN-14 (compound 19k) 为高效PARP1抑制剂,IC50值为0.6 ± 0.1 nM。此化合物对MDA-MB-436 (BRCA1−/−) 及Capan-1 (BRCA2−/−) 细胞线展现出显著的抗增殖效应,IC50低至0.3 nM以下。 | |||
T79405 |
PARP1-IN-15
|
PARP | Chromatin/Epigenetic; DNA Damage/DNA Repair |
PARP1-IN-15(Compound 6)是一款针对PARP1的抑制剂,能够抑制坦聚合酶(TNKS)并促进DNA双链断裂损伤。该化合物在诱导肿瘤细胞凋亡(apoptosis)方面具有显著作用,且在三阴性乳腺癌(TNBC)细胞及来源于TNBC患者的类器官中显示出抗癌活性,适用于探究BRCA1突变状态下的TNBC研究。 | |||
T69596 |
SK-575
|
||
SK-575 is a Highly Potent and Efficacious Proteolysis-Targeting Chimera Degrader of PARP1 for Treating Cancers. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations and induces potent and specific degradation of PARP1 in various human cancer cells even at low picomolar concentrations. SK-575 achieves durable tumor growth inhibition in mice when used as a single agent or in combination with cytotoxic agents, such as temozolomide and cisplatin. | |||
T83855 |
TG2-179-1
|
||
TG2-179-1是BRCA1相关蛋白1(BAP1)的抑制剂。它在25 µM至1.5 mM的浓度范围内,通过无细胞测定法抑制BAP1的去泛素化活性。TG2-179-1对八种结肠癌细胞系表现出细胞毒性(IC50s = 4.48-7.52 µM)。在体内,TG2-179-1(10和30 mg/kg)能够减少HCT116结肠癌小鼠异种移植模型中的肿瘤体积。 | |||
T36701 | Phosphoramide mustard (cyclohexanamine) | ||
Phosphoramide mustard cyclohexanamine is the major metabolite for Cyclophosphamide , with anticancer activitiy. Phosphoramide mustard cyclohexanamine induces DNA adduct formation in ovarian granulosa cells, induces DNA damage and elicits the ovarian DNA repair response[1][2]. Phosphoramide mustard cyclohexanamine causes cytotoxicity through forming cross-linked DNA adducts which inhibit DNA strand separation during replication[1].Phosphoramide mustard cyclohexanamine destroys rapidly dividing ce... |