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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
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。
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。
T74698	RMC-6236 RAS-IN-2
	RMC-6236是一种相关的 RAS（ON）多选择性抑制剂，对CypA蛋白(KD1)的亲和力为55.3 nmol/L，RMC-6236对KRAS突变癌细胞系HPAC (KRASG12D/WT, PDAC)和Capan-2 (KRASG12V/WT, PDAC)， EC50分别为1.2和1.4 nmol/L，可用于癌症治疗。[1,2]
T79667	YCH1899	PARP	Chromatin/Epigenetic; DNA Damage/DNA Repair
	YCH1899为一种口服活性PARP抑制剂，其对PARP1/2的IC50均低于0.001 nM。该化合物对Olaparib和Talazoparib耐药的Capan-1细胞株(Capan-1/OP及Capan-1/TP细胞)表现出显著抗增殖能力，IC50分别为0.89 nM和1.13 nM。在大鼠体内，YCH1899展现优良的药代动力学属性。
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。
T74558	SK-575-NEG
	SK-575-NEG（化合物28）是SK-575的甲基化对应物，通过对SK-575中的哌啶-2,6-二酮氨基进行甲基化合成而得，用作对照化合物。SK-575-NEG强效结合PARP1，IC50值仅为2.64 nM。在1 μM浓度下，SK-575-NEG对MDA-MB-436和Capan-1细胞中PARP1的降解完全无效。
T36703	CAY10760
	CAY10760 is an inhibitor of the protein-protein interaction between RAD51 recombinase and BRCA2 (EC50= 19 μM in a cell-free competitive ELISA).1It decreases homologous recombination by 54% in wild-typeBRCA2-expressing BxPC-3 pancreatic cancer cells when used at a concentration of 20 μM. CAY10760 (20 μM) decreases proliferation of BxPC-3, as well as mutantBRCA2-expressing Capan-1, cancer cells when used alone or in combination with the poly(ADP-ribose) polymerase (PARP) inhibitor olaparib . 1.Bag...
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...

化合物

Rucaparib monocamsylate

Cat.No: T16807

Synonym: 瑞卡帕布樟脑磺酸盐,Rucaparib Camsylate

Target: PARP

Rucaparib

Cat.No: T4463

Synonym: AG-14447,PF-01367338,瑞卡帕布,AG014699

Target: PARP

Rucaparib Phosphate

Cat.No: T6127

Synonym: AG-014699 phosphate,PF-01367338,芦卡帕利,AG-014699,瑞卡帕布磷酸盐,PF-01367338 phosphate

Target: PARP

RMC-6236

Cat.No: T74698

Synonym: RAS-IN-2

Cat. No.	Product Name	Target	Signaling Pathways
TWS2045	Bruceine D 鸦胆子素D,鸦胆子苦素D	Apoptosis; Antiviral; Gamma-secretase; Parasite	Apoptosis; Immunology/Inflammation; Microbiology/Virology; Neuroscience; Proteases/Proteasome; Stem Cells
	Bruceine D 是Notch 抑制剂，有抗癌活性，诱导几种人癌细胞调亡。它是一种有效的植物性昆虫拒食剂，有显著的系统特性和抑制害虫生长的作用。它具有较强的驱虫活性，抑制D. intermedius 的 EC50值为 0.57 mg/L。
T36954	Nemorosone
	Nemorosone is a polycyclic polyprenylated acylphloroglucinol (PPAP) originally isolated from C. rosea that has antiproliferative properties.1 Nemorosone inhibits growth of NB69, Kelly, SK-N-AS, and LAN-1 neuroblastoma cells (IC50s = 3.1-6.3 μM), including several drug-resistant clones, but not MRC-5 human embryonic fibroblasts (IC50 = >40 μM).2 It increases DNA fragmentation in LAN-1 cells in a dose-dependent manner, and decreases N-Myc protein levels and phosphorylation of ERK1/2 by MEK1/2. Nem...
T15949	Mahanimbine	AChE	Neuroscience
	Mahanimbine 存在于Murraya koenigii 的根、叶和茎中，是从Murraya koenigii 中的提取的一种具有口服活性的生物碱。Mahanimbine 具有乙酰胆碱酯酶抑制活性，可抑制了高脂肪饮食（HFD）引起的小鼠代谢并发症的发展，对科尼氏分枝杆菌叶对链脲佐菌素诱导的糖尿病大鼠胰腺β细胞组织病理学变化有作用。