sarcoma

TK216 是一种口服有效的 E26 转录因子抑制剂，具有抗癌活性。它直接结合 EWS-FLI1 并抑制 EWS-FLI1 蛋白质相互作用，也可阻止 EWS-FLI1 与 RNA 解旋酶 A 的结合。

Seclidemstat (SP-2577) 是非竞争性可逆KDM1A (LSD1)抑制剂，可用于尤文肉瘤的研究。它促进 SWI SNF 复合物突变卵巢癌的抗肿瘤免疫，并抑制病毒产生、病毒 DNA 复制和晚期基因表达。

PF-562271 hydrochloride (PF-562271 HCl) 是一种可逆的，有效的，ATP 竞争性的 FAK (IC50:1.5 nM)和 Pyk2 (IC50:13 nM)激酶抑制剂。

PMEDAP 是有效的人类免疫缺陷病毒 (HIV) 复制抑制剂。它具有抗小鼠巨细胞病毒活性。它有效抑制莫罗尼鼠肉瘤病毒诱导的肿瘤形成和相关死亡率。

PF-562271 是一种可逆的，有效的，ATP 竞争性的 FAK (IC50:1.5 nM)和 Pyk2 (IC50:13 nM)激酶抑制剂。

Laminin β2 (Engelbreth-Holm-Swarm murine sarcoma basement membrane) 是动物组织中的重要结构成分，是支撑组织的基底结构的一部分。它与 IV 型胶原蛋白、内切蛋白和基底膜蛋白聚糖有相互作用，通过整合素受体、肌营养不良蛋白复合物和路德血型糖蛋白连接细胞膜，并含有促进胶原蛋白结合、细胞黏附、肝素作用及神经突生长的功能域。

Osteosarcoma-IN-D14 is an inhibitor of migration and invasion of osteosarcoma cells mediated by p53, regulating EMT-related genes.

AGI-14100 是一种新型且可口服的 mIDH1 抑制剂。AGI-14100 用于治疗原发性人类髓性白血病。

S 14063 is a potent 5-HT1A receptor antagonist devoid of beta-adrenoceptor blocking properties.

p-Hydroxy-5,6-dehydrokawain (4'-Hydroxydehydrokawain) 是一种分离自 Kawain 的天然产物。

Tazemetostat (EPZ6438) 是一种组蛋白甲基转移酶 EZH2 抑制剂 (IC50=11 nM)，具有口服活性、选择性和 SAM 竞争性。Tazemetostat 具有抗肿瘤活性，可以用于治疗上皮样肉瘤 滤泡性淋巴瘤。

BK60106是一种选择性的跨膜蛋白CD99的抑制剂，通过直接结合CD99的胞外结构域导致Ewing Sarcoma (尤因肉瘤)细胞死亡。

Sitravatinib (MGCD516) 是一种有口服活性的受体酪氨酸激酶抑制剂。它单独使用即具有有效的抗肿瘤功效，且通过促进抗肿瘤免疫微环境增强了 PD-1 阻断的活性。

Dacarbazine citrate is an alkylating agent used to treat cancers of the lymphatic system and malignant melanoma (a type of skin cancer) in patients with certain conditions: islet cell carcinoma (part of the pancreas) Soft tissue sarcoma (cancer of muscles

Trabectedin (Ecteinascidin 743) 是一种四氢异喹啉生物碱，有抗肿瘤的活性， 通过与 DNA 的小沟结合，阻断应激诱导的蛋白质的转录，诱导 DNA 骨架裂解和癌细胞凋亡，并增加 MCF-7 和 MDA-MB-453 细胞中 ROS 的生成。Trabectedin 在软组织肉瘤和卵巢癌中具有的研究价值。

SXT1596 is a novel SS18-SSX TLE1 interaction inhibitor. SXT1596 reduces cell viability and reactivates EGR1 expression in synovial sarcoma.

NSC635437 是艾文氏肉瘤中EWS-FLI1癌蛋白的抑制剂。

Olomorasibum 是一种针对Kirsten rat sarcoma viral oncogene homolog (KRAS)的抑制剂，属于抗肿瘤化合物类别。

RETRA is an agent of anticancer that acts by exerting anticancer activity in Ewing's sarcoma cells independent of their TP53 status.

FR 900490 is an immunoactive substance produced by a fungus Discosia sp. F-11809. In vitro FR-900490 restores the colony forming units in culture (cfu-c) in bone marrow cells, which were suppressed by immunosuppressive factor obtained from the serum of sa

DC 86M 是一种从 Streptomyces uteogriseus DO-86 培养液中分离出来的抗肿瘤抗生素。 DC 86M 对革兰氏阳性菌和革兰氏阴性菌以及实验性鼠肉瘤 180 具有活性。

Potent BRD9 degrader. Selectively binds BRD9 and elicits near complete degradation of BRD9 at nanomolar concentrations. Inhibits growth of synovial sarcoma cells in vitro and tumor progression in a synovial sarcoma xenograft mouse model.

YW3-56 is an inhibitor of protein arginine deiminase 2 (PAD2) and PAD4 (IC50s = 0.5-1 and 1-5 μM, respectively).1It inhibits the growth of U2OS osteosarcoma cells (IC50= ~2.5 μM) in a p53-dependent mannerviainduction of SESN2 and subsequent inhibition of mTORC1. YW3-56 (10 mg kg) reduces tumor growth in an S-180 murine sarcoma tumor model. It also inhibits tumor growth in the 1883 MDA-MB-231 breast cancer bone metastasis mouse xenograft model.2 1.Wang, Y., Li, P., Wang, S., et al.Anticancer peptidylarginine deiminase (PAD) inhibitors regulate the autophagy flux and the mammalian target of rapamycin complex 1 activityThe Journal of Biological Chemisty287(31)25941-25952(2012) 2.Wang, S., Chen, X.A., Hu, J., et al.ATF4 gene network mediates cellular response to the anticancer PAD inhibitor YW3-56 in triple-negative breast cancer cellsMol. Cancer Ther.14(4)877-888(2015)

Degrader targeting mutant FKBP12F36V fusion proteins. Comprises a ligand selective for F36V single-point mutated FKBP12, a linker and a von Hippel-Lindau (VHL)-binding ligand. Induces potent and selective degradation of FKBP12F36V fusion proteins in vitro and in vivo. Selectively degrades FKBP12F36V-EWS FLI fusion proteins and inhibits cell proliferation in FKBP12F36V-EWS FLI-expressing Ewing sarcoma cells. Hydrochloride salt (Cat.No. 7374) available; suitable for in vivo use. Negative control dTAGV-1-NEG (Cat. No. 6915) also available. FKBP12F36V can be expressed as a fusion with a target protein of interest using genome engineering techniques, via transgene expression or CRISPR-mediated locus-specific knock-in. Custom knock-in cell lines for the dTAG and aTAG platforms are available from our sister brand R&D Systems. Email TPD@bio-techne.com to enquire. Plasmid vectors for the lentiviral expression and CRISPR-mediated knock-in of FKBP12F36V are available from Addgene.