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20

抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T6603	Nelarabine GW 506U78,Nelzarabine,奈拉滨,506U78	Apoptosis; Nucleoside Antimetabolite/Analog; DNA/RNA Synthesis	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Nelarabine (GW 506U78) 是一种嘌呤核苷酸类似物，为DNA 合成抑制剂，对肿瘤细胞的IC50为0.067-2.15 μM，可作用于T 细胞急性淋巴细胞白血病。
T2415	PP121	Apoptosis; VEGFR; Bcr-Abl; PDGFR; Src; mTOR; Hck	Angiogenesis; Apoptosis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
	PP121是一种多靶点激酶抑制剂，抑制 PDGFR、Hck、mTOR、VEGFR2、Src、Abl、DNK-PK 的 IC50值分别为2、8、10、12、14、18、60 nM。
T67737	gp120-α4β7 binding inhibitor 11	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	gp120-α4β7 binding inhibitor 11是一种抗HIV 药物。gp120-α4β7 binding inhibitor 11干扰HIV 相关糖蛋白gp12G 与整合素α4β7的结合（IC50=1.64nM）。
T9691L	(D-Trp12,Tyr34)-pTH (7-34) amide (bovine) acetate	Thyroid hormone receptor(THR)	Endocrinology/Hormones
	(D-Trp12,Tyr34)-pTH (7-34) amide (bovine) acetate 是一种高效的甲状旁腺激素 (PTH) 拮抗剂，在牛肾皮质膜中的 Ki 值为 69 nM。
T28993	TOP1210 TOP 1210,TOP-1210
	TOP1210, a narrow spectrum kinase inhibitor, potently inhibits P38α, Src, and Syk kinase activities.
T78846	EP12	Apoptosis	Apoptosis
	EP12是一种c-Myc抑制剂及c-MycG4稳定剂，能够诱导多发性骨髓瘤细胞的细胞凋亡(apoptosis)及DNA损伤，并通过干扰NF-κB信号通路破坏P65/P50的核转位，从而抑制多发性骨髓瘤的生长。
T76537	GP120, HIV-1 MN
	GP120，HIV-1MN 是一种肽。GP120,HIV-1MN 可用于 HIV 感染的研究。
T11292	FKBP12 PROTAC dTAG-7 dTAG-7	Epigenetic Reader Domain	Chromatin/Epigenetic
	FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional compound that selectively degrades the BET bromodomain transcriptional co-activator BRD4 by connecting BET bromodomains to the E3 ubiquitin ligase CRBN. Additionally, it serves as a degrader of FKBP12F36V when FKBP12F36V is expressed in-frame with a targeted protein.
T60871	gp120-IN-1
	gp120-IN-1 (compound 4e) 是 HIV-1 gp120蛋白的有效抑制剂，CC50值为 100.90 μM，IC50值为 2.2 μM。gp120-IN-1 抑制 gp120 蛋白介导的病毒进入细胞。gp120-IN-1 具有抗 HIV-1 活性。gp120-IN-1 在 SUP-T1 细胞中具有剂量依赖性细胞毒性。
T13694	FKBP12 PROTAC RC32 RC32	Others	Others
	FKBP12 PROTAC RC32 contains conjugation of Rapamycin and a ligand for an E3 ubiquitin ligase.FKBP12 PROTAC RC32 (RC32) is a potent FKBP12 degrader based on PROTAC technology.
T76586	(Asn10,Leu11,D-Trp12)-pTH-Related Protein (7-34) amide (human, mouse, rat)
	(Asn10,Leu11,D-Trp12)-pTH-Related Protein (7-34) amide (human, mouse, rat) 是一种有效的 PTH-1R 拮抗剂。
T60714	gp120-IN-2
	gp120-IN-2 (compound 4i) 显示出抗 HIV-1 活性。它是 HIV-1 gp120的有效抑制剂，IC50值为 7.5 μM，CC50值为 112.93 μM。gp120-IN-2 在癌细胞 SUP-T1 中表现出剂量依赖性的细胞毒性。
T9691	(D-Trp12,Tyr34)-pTH (7-34) amide (bovine)
	(D-Trp12,Tyr34)-pTH (7-34) amide (bovine) 在生命科学相关研究中具有广泛的应用。
T69965	TP1287
	TP-1287 is an oral phosphate prodrug of the CDK9 inhibitor, alvocidib.
T61287	CYP121A1-IN-1
	CYP121A1-IN-1 是一种有效的CYP121A1抑制剂，对抗结核分枝杆菌具有良好的活性 (H37RvMIC90～6.25 μM, ～2.2 μg/mL)。CYP121A1-IN-1 通过抑制 CYP121A1 介导的环(l-酪氨酸-l-酪氨酸)转化为真菌环素，可显著减少真菌环素的产生。
T83735	Pap12-6 TFA
	Pap12-6是一种从蝶类P. xuthus幼虫中发现的papiliocin十二个N-端氨基酸衍生的抗菌肽。它对包括E. coli、P. aeruginosa和S. syphimurium在内的八种革兰氏阴性细菌（MIC50s = 4-8 µM）以及革兰氏阳性细菌S. aureus、耐甲氧西林的S. aureus 3126（MRSA-3126）、B. subtilis和S. epidermidis（MIC50s = 4-8 µM）具有活性，但在25 µM浓度下不影响人类红细胞、小鼠RAW 264.7巨噬细胞、人类HaCaT角质形成细胞或人类HEK293肾细胞的活性。Pap12-6在4和8 µM浓度下可引起E. coli的膜去极化。Pap12-6（10 µM）预处理可降低LPS刺激的RAW 264.7巨噬细胞中一氧化氮（NO2-）、Tnf-α和Il-6的分泌水平。在体内，Pap12-6（10 mg/kg）可以提高感染E. coli的小鼠的存活率，并且在剂量为1 mg/kg时减少感染E. coli小鼠的肺、肝和肾中菌落形成单位（CFUs）的数量。Pap12-6（1 mg/kg）在E. co...
T70613	SLP120701 HCl
	SLP120701 is a potent and selective sphingosine kinase 2 inhibitor. Sphingosine-1-phosphate (S1P) is a ubiquitous, endogenous small molecule that is synthesized by two isoforms of sphingosine kinase (SphK1 and 2). Intervention of the S1P signaling pathway has attracted significant attention because alteration of S1P levels is linked to several disease states including cancer, fibrosis, and sickle cell disease.
T71840	FKBP12-IN-Q2
	FKBP12-IN-Q2 is an inhibitor of FKBP12.
T11291	FKBP12 PROTAC dTAG-13 dTAG-13	Epigenetic Reader Domain	Chromatin/Epigenetic
	FKBP12 PROTAC dTAG-13 (dTAG-13) is a degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 (dTAG-13) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN. FKBP12 PROTAC dTAG-13 (dTAG-13) is a PROTAC-based heterobifunctional degrader.
T83851	Tat-QFNP12 TFA
	Tat-QFNP12 是一种含有转录激活因子 (Tat) 跨膜结构域和抑制N-Myc下游调节基因2 (NDRG2) 与蛋白磷酸酶Mg2+/Mn2+依赖性1A (PPM1A) 蛋白-蛋白相互作用的肽。在以20 mg/kg剂量给药的内脑血管穿刺诱导的小鼠蛛网膜下腔出血模型中，它能减少由基质金属蛋白酶-9 (MMP-9) 浓度增高引起的血脑屏障内皮紧密连接的损失，减轻脑水肿，并且提高自发活动及肢体运动的对称性。

化合物

Cat.No: T6603

Synonym: GW 506U78,Nelzarabine,奈拉滨,506U78

Target: Apoptosis, Nucleoside Antimetabolite/Analog, DNA/RNA Synthesis

Cat.No: T2415

Target: Apoptosis, VEGFR, Bcr-Abl, PDGFR, Src, mTOR, Hck

gp120-α4β7 binding inhibitor 11

Cat.No: T67737

Target: HIV Protease

(D-Trp12,Tyr34)-pTH (7-34) amide (bovine) acetate

Cat.No: T9691L

Target: Thyroid hormone receptor(THR)

Cat.No: T28993

Synonym: TOP 1210,TOP-1210

Cat.No: T78846

Target: Apoptosis

GP120, HIV-1 MN

Cat.No: T76537

FKBP12 PROTAC dTAG-7

Cat.No: T11292

Synonym: dTAG-7

Target: Epigenetic Reader Domain

Cat.No: T60871

FKBP12 PROTAC RC32

Cat.No: T13694

Synonym: RC32

Target: Others

(Asn10,Leu11,D-Trp12)-pTH-Related Protein (7-34) amide (human, mouse, rat)

Cat.No: T76586

Cat.No: T60714

(D-Trp12,Tyr34)-pTH (7-34) amide (bovine)

Cat.No: T9691

Cat.No: T69965

Cat.No: T61287

Cat.No: T83735

Cat.No: T70613

Cat.No: T71840

FKBP12 PROTAC dTAG-13

Cat.No: T11291

Synonym: dTAG-13

Target: Epigenetic Reader Domain

Cat.No: T83851

Cat. No.	Product Name	Target	Signaling Pathways
T19329	Fructo-oligosaccharide DP12/GF11 蔗果十二糖	Others	Others
	Fructo-oligosaccharide DP12/GF11 is a member of fructooligosaccharides (FOS) characterized by a degree of polymerization (DP) of 12. FOS compounds consist of 11 fructose units connected by (2→1)-β-glycosidic bonds, with a lone D-glucosyl unit located at the non-reducing end.

天然产物

Fructo-oligosaccharide DP12/GF11

Cat.No: T19329

Synonym: 蔗果十二糖

Target: Others

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