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34

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T38514	PMEDAP	Others; HIV Protease	Microbiology/Virology; Others; Proteases/Proteasome
	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。
T13166	TK216	Others; DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Others
	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。
T4527	Seclidemstat SP-2577	Histone Demethylase	Chromatin/Epigenetic
	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。
T2465	PF-562271 PF562271,PF 562271	FAK; PYK2; CDK	Angiogenesis; Cell Cycle/Checkpoint; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	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。
T21768	PF-562271 hydrochloride PF-562271 HCl	FAK; PYK2; CDK	Angiogenesis; Cell Cycle/Checkpoint; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	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。
T70841	Osteosarcoma-IN-D14
	Osteosarcoma-IN-D14 is an inhibitor of migration and invasion of osteosarcoma cells mediated by p53, regulating EMT-related genes.
T73425	CFT8634
	CFT8634 是一种靶向 BRD9的降解剂，可用于滑膜肉瘤和 SMARCB1 缺失实体瘤的研究。
T4349	Sitravatinib MG516,MGCD516	Discoidin Domain Receptor (DDR); VEGFR; FLT; Trk receptor; TAM Receptor; c-Kit; Ephrin Receptor	Angiogenesis; Tyrosine Kinase/Adaptors
	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。
T1788	Tazemetostat E-7438,EPZ6438	Histone Methyltransferase	Chromatin/Epigenetic
	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。
T4350	Palifosfamide ZIO-201,Isophosphamide mustard,帕利伐米,Isophosphoramide mustard	DNA Alkylator/Crosslinker; DNA Alkylation; Drug Metabolite	DNA Damage/DNA Repair; Metabolism
	Palifosfamide (Isophosphamide mustard) 是一种新 DNA 烷化剂，是异环磷酰胺的活性代谢物，。它在体外肉瘤细胞系中具有广泛的活性，具有抗癌活性。
T35480	dBRD9-A dBRD9-A
	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.
T24709	RETRA
	RETRA is an agent of anticancer that acts by exerting anticancer activity in Ewing's sarcoma cells independent of their TP53 status.
T19771	SXT1596 NSC-65667,SXT-1596,NSC 65667,SXT 1596,NSC65667
	SXT1596 is a novel SS18-SSX/TLE1 interaction inhibitor. SXT1596 reduces cell viability and reactivates EGR1 expression in synovial sarcoma.
T70230	FPTI
	FPTI is an inhibitor against SYT-SSX1 fusion protein in synovial sarcoma which down-regulates SYT-SSX1 and modulates its downstream target genes.
T1120L2	Dacarbazine citrate DTIC citrate
	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
T69283	Amikhellin HCl
	Amikhellin HCl, an antimitotic drug, is a synthetic water-soluble derivative of khellin, an alkaloid extracted from seeds of Ammi Visnaga. Amikhellin has been used so far mostly as a vasodiator. Amikhellin binds to double-stranded DNA by an intercalation process. It inhibits the DNA-polymerase from murine sarcoma leukemia virus.
T83064	Anti-hepatic fibrosis agent 2
	Fibrosis agent 2为针对Ewing肉瘤断点区域1 (EWSR1) 的特定抗纤维化化合物。
T78982	BK60106	Apoptosis	Apoptosis
	BK60106是一种选择性针对CD99的抑制剂，能够直接与CD99的胞外结构域结合。它能特异性地诱导尤文肉瘤(ES)细胞凋亡(apoptosis)，而且伴随的DNA损伤相对较少。
T68946	Antibiotic MA 144M1
	Antibiotic MA 144M1 is an anthracycline glycoside that inhibits the growth of gram-positive bacteria, e.g. Staphyococcus aureaus, Bacillus subtilis and Sarcina lutea, and inhibits the growth of animal tumors such as leukemia L 1210, P 388 and sarcoma 180. It's produced by fermentation of MA 144-producing strains of streptomyces and by the chemical or enzymatic conversion of aclacinomycin A or cinerubin A.
T68945	Antibiotic MA 144M2
	Antibiotic MA 144M2 is an anthracycline glycoside that inhibits the growth of gram-positive bacteria, e.g. Staphyococcus aureaus, Bacillus subtilis and Sarcina lutea, and inhibits the growth of animal tumors such as leukemia L 1210, P 388 and sarcoma 180. It's produced by fermentation of MA 144-producing strains of streptomyces and by the chemical or enzymatic conversion of aclacinomycin A or cinerubin A.
T81953	LANA-DNA-IN-2
	LANA-DNA-IN-2 (Compound 20) 是抑制潜伏期相关核抗原 (LANA) 与 DNA 相互作用的化合物。它适用于研究卡波西肉瘤相关疱疹病毒 (KSHV) 感染。
T39439	Seclidemstat mesylate SP-2577 mesylate
	Seclidemstat mesylate (SP-2577) is a highly effective and reversible inhibitor of KDM1A (LSD1), with a Ki of 31 nM and an IC 50 of 13 nM. It demonstrates significant potential in promoting antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, while also exhibiting inhibitory effects on virus production, viral DNA replication, and late gene expression. Seclidemstat mesylate is a valuable tool for studying Ewing Sarcoma in research settings.
T76759	Robatumumab
	Robatumumab (Sch 717454) 为针对人胰岛素样生长因子 1 受体(anti-humanIGF-1R)的抗体，展现出抗肿瘤及阻止癌细胞增殖的作用，适用于骨肉瘤与尤文肉瘤的研究。
T27367	FR 900490 BMY 28700,FR-900490,FR900490
	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
T79810	Porcn-IN-2
	Porcn-IN-2（Example 107）是Wnt信号通路的一种高效抑制剂，具有0.05 nM的IC50。该化合物适用于癌症、肉瘤、黑色素瘤、皮肤癌、血液肿瘤、淋巴瘤以及白血病等多种恶性肿瘤的研究。
T75869	PSI TFA
	PSI (TFA) 是一种有效的蛋白酶体proteasome 抑制剂。PSI (TFA) 抑制原发性渗出性淋巴瘤 (PEL) 细胞的增殖。PSI (TFA) 可用于卡波济氏肉瘤相关疱疹病毒 (KSHV) 感染和 KSHV 相关淋巴瘤的研究。
T76989	Tabituximab barzuxetan
	Tabituximab barzuxetan (OTSA101-DTPA-90Y) 是一种放射免疫偶联物，由靶向FZD-10 (OTSA-101)的人源化单克隆抗体组成，并用钇 90 标记。Tabituximab barzuxetan 具有抗肿瘤活性。Tabituximab barzuxetan 可用于滑膜肉瘤的研究。
T78896	SHP2-IN-22
	SHP2-IN-22 作为变构抑制剂，靶向SHP2，具有 17.7 nM 的 IC50。该化合物能够有效抑制MIA PaCa-2胰腺癌细胞的增殖、迁移和侵袭行为。SHP2-IN-22 主要用于研究含Kirsten大鼠肉瘤病毒癌基因(KRAS)突变型的癌症。
T35762	MC1742
	MC1742 is an inhibitor of class I histone deacetylases (HDACs; IC50s = 0.1, 0.11, 0.02, and 0.61 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 7 and 40 nM for HDAC6 and HDAC10, respectively).1 It is selective for class I and class IIb over class IIa HDACs (IC50s = >50 μM for HDAC4, -5, -7, and -9). MC1742 reduces proliferation of HOS, MG-63, RD, A204, SK-ES-1, and A673 sarcoma cancer stem cells (CSCs). It increases levels of acetylated histone H3 and acetylated tubulin...
T36745	cDPCP
	cDPCP is a platinum-containing DNA-crosslinking agent.1Unlike cisplatin or oxaliplatin , cDPCP forms monofunctional DNA adducts. It is transported into cells by organic cation transporter 1 (OCT1) and OCT2, inhibiting proliferation of MDCK cells expressing the human transporters with IC50values of 8.1 and 1.5 μM, respectively. cDPCP inhibits RNA polymerase II-mediated transcription in a reporter assay using HeLa cells. It increases survival in murine S180 sarcoma and P388 leukemia models when ad...
T36108	YW3-56 (hydrochloride) (technical grade) YW3-56 (hydrochloride) (technical grade)
	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 pept...
T76305	[Ala2] Endothelin-3, human
	[Ala2] Endothelin-3, human 为ET-3的线性类似物，其结构中的Cys残基被Ala所替代。ET-3是由人体横纹肌肉瘤细胞系产生，且仅在此细胞系中表达的一种具有血管活性的肽。在非肌肉来源的肉瘤细胞系中不表达。该肽能够作为旁分泌因子，促进内皮细胞迁移。
T73700	Daunorubicin citrate
	Daunorubicin citrate（Daunomycin citrate）作为一种拓扑异构酶 II（topoisomerase II）抑制剂，展现出有效的抗肿瘤活性，通过抑制 DNA 和 RNA 合成（DNA and RNA synthesis）发挥作用。作为一种细胞毒性药物，Daunorubicin citrate 能够抑制癌细胞活性，并诱导细胞凋亡（apoptosis）和坏死（necrosis），属于蒽环类抗生素范畴。该化合物广泛应用于包括白血病、非霍奇金淋巴瘤、尤文氏肉瘤、维尔姆斯氏瘤在内的多种癌症和感染研究领域。
T36253	dTAGV-1
	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...

化合物

Cat.No: T38514

Target: Others, HIV Protease

Cat.No: T13166

Target: Others, DNA/RNA Synthesis

Cat.No: T4527

Synonym: SP-2577

Target: Histone Demethylase

Cat.No: T2465

Synonym: PF562271,PF 562271

Target: FAK, PYK2, CDK

PF-562271 hydrochloride

Cat.No: T21768

Synonym: PF-562271 HCl

Target: FAK, PYK2, CDK

Osteosarcoma-IN-D14

Cat.No: T70841

Cat.No: T73425

Cat.No: T4349

Synonym: MG516,MGCD516

Target: Discoidin Domain Receptor (DDR), VEGFR, FLT, Trk receptor, TAM Receptor, c-Kit, Ephrin Receptor

Cat.No: T1788

Synonym: E-7438,EPZ6438

Target: Histone Methyltransferase

Cat.No: T4350

Synonym: ZIO-201,Isophosphamide mustard,帕利伐米,Isophosphoramide mustard

Target: DNA Alkylator/Crosslinker, DNA Alkylation, Drug Metabolite

Cat.No: T35480

Synonym: dBRD9-A

Cat.No: T24709

Cat.No: T19771

Synonym: NSC-65667,SXT-1596,NSC 65667,SXT 1596,NSC65667

Cat.No: T70230

Dacarbazine citrate

Cat.No: T1120L2

Synonym: DTIC citrate

Cat.No: T69283

Anti-hepatic fibrosis agent 2

Cat.No: T83064

Cat.No: T78982

Target: Apoptosis

Antibiotic MA 144M1

Cat.No: T68946

Antibiotic MA 144M2

Cat.No: T68945

Cat.No: T81953

Seclidemstat mesylate

Cat.No: T39439

Synonym: SP-2577 mesylate

Cat.No: T76759

Cat.No: T27367

Synonym: BMY 28700,FR-900490,FR900490

Cat.No: T79810

Cat.No: T75869

Tabituximab barzuxetan

Cat.No: T76989

Cat.No: T78896

Cat.No: T35762

Cat.No: T36745

YW3-56 (hydrochloride) (technical grade)

Cat.No: T36108

Synonym: YW3-56 (hydrochloride) (technical grade)

[Ala2] Endothelin-3, human

Cat.No: T76305

Daunorubicin citrate

Cat.No: T73700

Cat.No: T36253

Cat. No.	Product Name	Target	Signaling Pathways
TN3548	Bulleyanin	Others	Others
	Bulleyanin 是从 isodon species (Labiatae) 中分离出来的一种物质。
T17155	Trabectedin Ecteinascidin 743,曲贝替定,ET-743	Apoptosis; Reactive Oxygen Species	Apoptosis; Immunology/Inflammation; Metabolism; NF-κB
	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。
TN4455	Lucialdehyde B	Integrase; HSV	Microbiology/Virology
	Lucialdehyde B exhibits potent inhibitory activity against herpes simplex virus. It shows cytotoxic effects on Lewis lung carcinoma (LLC), T-47D, Sarcoma 180, and Meth-A tumor cell lines.
TN4457	Lucidal	Others	Others
	Lucialdehyde C (Lucidal) exhibits potent cytotoxicity against LLC, T-47D, Sarcoma 180, and Meth-A tumor cells with ED(50) values of 10.7, 4.7, 7.1, and 3.8 microg/ml, respectively.

天然产物

Cat.No: TN3548

Target: Others

Cat.No: T17155

Synonym: Ecteinascidin 743,曲贝替定,ET-743

Target: Apoptosis, Reactive Oxygen Species

Cat.No: TN4455

Target: Integrase, HSV

Cat.No: TN4457

Target: Others

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