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35

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8986	ML198	Glucokinase	Metabolism
	ML198 是葡萄糖脑苷脂酶激活剂(EC50:0.4 μM)。它不会抑制该酶的作用，且能促进其易位至溶酶体，可用于研究戈谢病。
T4304	Azoramide	Apoptosis; PERK	Apoptosis
	Azoramide 是一种小分子调节剂，具有未折叠蛋白反应的抗糖尿病活性。
T8958	PU-H54	GPR	Endocrinology/Hormones; GPCR/G Protein
	PU-H54 是一种基于嘌呤的 Grp94 抑制剂。它是一种基于 Grp94 选择性间苯二酚的抑制剂，通过探测 Grp94 中 S2 亚袋的专有结合区而分离。
T6234	Ambroxol hydrochloride Mucosolvan,Mucoangin,盐酸氨溴索,Ambroxol HCl	Sodium Channel; Autophagy	Autophagy; Membrane transporter/Ion channel
	Ambroxol hydrochloride (Mucosolvan) 是前药溴己辛的活性代谢产物，是一种葡糖脑苷脂酶伴侣，可增加葡糖脑苷脂酶的活性。它可刺激粘液纤毛作用并清除呼吸道中的空气通道，具有强效祛痰作用。它可诱导肺细胞自噬，有用于帕金森氏病和神经性戈谢病的研究潜力。
T0920	Ambroxol 氨溴索,氨溴索碱,Ambroxolum,NA-872	P450; Autophagy	Autophagy; Metabolism
	Ambroxol (NA-872) 是前药溴己辛的活性代谢产物，是一种分泌溶解剂，具有强效祛痰作用，用于治疗与粘液或过多粘液相关的呼吸道疾病。它可诱导肺组织细胞自噬，有用于帕金森氏病和神经性戈谢病的研究潜力。它是一种葡糖脑苷脂酶伴侣，可增加葡糖脑苷脂酶的活性。
T8989	NCGC 607 NCGC607	Others	Others
	NCGC 607 是一种葡萄糖脑苷酶的非抑制性分子伴侣。
T15947	MAC13243 HCl	Antibacterial	Microbiology/Virology
	MAC13243 HCl 是一种将脂蛋白从内膜运输到外膜的周质伴侣LolA的抑制剂，是一种具有特异性的抗菌剂，对革兰氏阴性菌抑制作用显著。
T4663	QX77	Others; Autophagy	Autophagy; Others
	QX77 是一种分子伴侣介导的自噬激活剂，可上调 LAMP2A 的表达。它可抑制 ES 细胞的自我更新，促进分化。它诱导 Rab11 上调，挽救 Rab11 下调和转运缺陷。
T30480	BiP inducer X BIX	Apoptosis	Apoptosis
	BiP inducer X (BIX) 是免疫球蛋白重链结合蛋白 (BiP)/GRP78 的选择性诱导剂和 ER 伴侣诱导剂。 BiP inducer X 可防止神经元和视网膜细胞系中的细胞死亡。
T6284	Onalespib AT13387,Onalespib (AT13387)	HSP	Cytoskeletal Signaling; Metabolism
	Onalespib (AT13387) 是一种合成的、口服生物可利用的热休克蛋白 90 (Hsp90) 小分子抑制剂，Kd 值为 0.71 nM。具有潜在的抗肿瘤活性。它选择性地与 Hsp90 结合，从而抑制其伴侣功能并促进参与肿瘤细胞增殖和存活的致癌信号蛋白的降解。
T67717L	Questiomycin A derivatives 18 TFA
	Questiomycin A derivatives 18 TFA 是一种Questiomycin A 衍生物，Questiomycin A 具有抗菌和抗癌活性，对细胞保护性 ER 伴侣蛋白 GRP78 的表达具有抑制作用。
T11718	JI051 JI-051	Gamma-secretase	Neuroscience; Proteases/Proteasome; Stem Cells
	JI051 具有抗肿瘤作用，能够与癌症相关蛋白伴侣 prohibitin 2 (PHB2) 相互作用，通过抑制 Notch 下游效应基因 Hes1 转录来促使细胞周期停滞，抑制HEK293 细胞和胰腺癌细胞增殖。
T7265	HSP27 inhibitor J2 J2	HSP	Cytoskeletal Signaling; Metabolism
	HSP27 inhibitor J2 (J2) 是一种HSP27抑制剂，可显著增强 17-AAG 的抗增殖活性，并对顺铂诱导的肺癌细胞生长抑制具有敏感性。它显著诱导异常 HSP27 二聚体形成并抑制HSP27巨聚合物的产生，从而具有抑制HSP27的伴侣功能和降低细胞保护功能的作用。
T4361	CBL0137 hydrochloride CBL0137,CBLC137,Curaxin 137,CBL-C137 hydrochloride,Curaxin-137 hydrochloride	Others; NF-κB; p53	Apoptosis; NF-κB; Others
	CBL0137 hydrochloride (Curaxin-137 hydrochloride) 是一种组蛋白分子伴侣FACT 的抑制剂，也可激活p53并抑制NF-κB，对于它们的EC50值分别为 0.37 和 0.47 μM。
T25770	116-9e MAL-2-11B,MAL2-11B,MAL211B,MAL 2 11B,MAL2 11B	Virus Protease	Microbiology/Virology
	116-9e (MAL2-11B) 是一种有效的 Hsp70 共伴侣 DNAJA1 抑制剂，具有抗病毒，抑制猿猴病毒40 (SV40) 的复制，抑制肿瘤抗原 (TAg) 内源性 ATP 酶活性和 TAg 介导的 Hsp70 激活。116-9e 可用于研究癌症耐药性。
T8990	ML266	Glucokinase	Metabolism
	ML266 是葡萄糖脑苷脂酶 (GCase) 分子伴侣， IC50值为 2.5 µM。ML266与 GCase 结合并将其转运至溶酶体，恢复 GCase 酶的活性。ML266 不会抑制 GCase 的活性。ML266 具有研究戈谢病的潜力。
T6248	XL888	HSP	Cytoskeletal Signaling; Metabolism
	XL888 是一种 ATP 竞争性的 Hsp90 抑制剂，IC50值为 24 nM。
T15646	KBU2046	Others	Others
	KBU2046 是口服有效的，体外细胞运动和侵袭的高选择性抑制剂。它结合伴侣异源复合物，选择性地改变调节运动性的侣伴蛋白的结合，并且缺乏经典 HSP90抑制剂的所有标志。它抑制癌症转移并延长寿命。
T3527	TRC051384 TRC 051384	HSP	Cytoskeletal Signaling; Metabolism
	TRC051384 是一种热休克蛋白70 (HSP70) 诱导剂，可减少中风相关的神经元损伤并增加短暂性缺血性中风大鼠模型的存活率，激活热休克因子-1 并导致分子伴侣和抗炎活性升高，增强神经元和神经胶质细胞中 Hsp72 的表达。
T25771	MAL3-101 MAL3 101
	MAL3-101 is a molecular chaperone inhibitor of heat shock protein 70 (Hsp 70).
T68764	Acetylbritannilactone
	Acetylbritannilactone is a Natural inhibitor of HSP60 chaperone activity through covalent binding.
T19181	Afegostat D-Isofagomine,Isofagomine	Others	Others
	Afegostat is a pharmacological chaperone that specifically and reversibly binds acid-β-glucosidase (GCase) in the endoplasmic reticulum with high affinity.
T19182	Afegostat D-Tartrate Isofagomine D-Tartrate,D-Isofagomine D-Tartrate	Others	Others
	Afegostat D-Tartrate is a pharmacological chaperone that specifically and reversibly binds acid-β-glucosidase (GCase) in the endoplasmic reticulum with high affinity.
T61819	Claficapavir
	Claficapavir (A1752) is a potent nucleocapsid protein (NC) inhibitor that effectively binds the HIV-1 NC with a dissociation constant (Kd) of 20 nM, resulting in the inhibition of its chaperone properties. This specific molecular interaction leads to strong antiviral activity against HIV-1, with an IC50 of approximately 1 μM [1].
T13076	Tamoxifen-d5 ICI 47699-d5,(Z)-Tamoxifen-d5,trans-Tamoxifen-d5	HSP	Cytoskeletal Signaling; Metabolism
	Tamoxifen-d5 is a deuterium labeled Tamoxifen. Tamoxifen is a selective modulator of estrogen receptor (SERM). Tamoxifen is a potent activator of Hsp90 and enhances the Hsp90 molecular chaperone ATPase activity.
T23653	Afegostat HCl Afegostat,AT-2101,Afegostat hydrochloride,AT2101
	Afegostat is an acid β-glucosidase (GCase) active site inhibitor that acts as a pharmacological chaperone. Afegostat inhibits GCase with K(i) ~30 nM for wild-type and mutant enzymes. Afegostat was an experimental drug for the treatment of certain forms of
T27128	DCB-3503 NSC716802,NSC 716802,NSC-716802,DCB3503,DCB 3503
	Tylophorine analog DCB-3503 is a potential anticancer and immunosuppressive agent. DCB-3503 suppresses the translation of cellular regulatory proteins, including cyclin D1, at the elongation step. DCB-3503 allosterically regulates the ATPase and chaperone activities of HSC70 by promoting ATP hydrolysis in the presence of specific RNA binding motifs (AUUUA) of cyclin D1 mRNA.
T28266	Org-6906 Org6906,Org 6906,Org-6906 free
	Tylophorine analog Org-6906 is a potential anticancer and immunosuppressive agent. Org-6906 suppresses the translation of cellular regulatory proteins, including cyclin D1, at the elongation step. Org-6906 allosterically regulates the ATPase and chaperone activities of HSC70 by promoting ATP hydrolysis in the presence of specific RNA binding motifs (AUUUA) of cyclin D1 mRNA.
T74277	NJH-2-056
	NJH-2-056 是一种去泛素酶靶向嵌合体 (DUBTAC)，连接OTUB1的招募因子 EN523 和CFTR 伴侣蛋白 lumacaftor。NJH-2-056 可用于囊性纤维化研究。
T71476	Afegostat TFA
	Afegostat, aslo known as Isofagomine, and AT2101, was an experimental drug for the treatment of certain forms of Gaucher's disease. Isofagomine (IFG) is an acid β-glucosidase (GCase) active site inhibitor that acts as a pharmacological chaperone. FG inhibits GCase with K(i) ~30 nM for wild-type and mutant enzymes (N370S and V394L). Administration of IFG (30 mg/kg/day) to the mice homozygous for GCase mutations (V394L, D409H, or D409V) led to increased GCase activity in visceral tissues and brain...
T68383	BIIB028
	BIIB028 is a small-molecule inhibitor of heat shock protein (Hsp) 90 with potential antineoplastic activity. Hsp90 inhibitor BIIB028 blocks the binding of oncogenic client proteins to Hsp90, which may result in the proteasomal degradation of these proteins and so the inhibition of tumor cell proliferation. Hsp90 is a molecular chaperone that plays a key role in the conformational maturation of oncogenic signaling proteins, such as Her2/Erbb2, Akt, Raf1, Bcr-Abl, and mutated p53, in addition to o...
T78371	Ac2-26 ammonium
	Ac2-26 ammonium是一种具抗炎作用的annexin 1 N末端肽。该化合物能够通过伴侣介导的自噬(CMA)机制降低溶酶体中的IKKβ蛋白含量，从而改善肺缺血再灌注损伤，并在哮喘大鼠模型中抑制气道炎症以及高反应性的表现。
T36436	Spergualin trihydrochloride
	Spergualin trihydrochloride is a natural product that first identified as an antibiotic from culture filtrates of Bacillus laterosporus BMG162-aF2[1]. Spergualin trihydrochloride derivatives likely acts as Hsp70 modulators[1]. [1]. Srikanth Patury, et al. Pharmacological Targeting of the Hsp70 Chaperone. Curr Top Med Chem. 2009;9(15):1337-51.
T36499	CuATSM
	The metallo-protein Cu/Zn-superoxide dismutase (SOD1) is a ubiquitous enzyme responsible for scavenging superoxide radicals. Mutations in SOD1, which alter its metal binding capacity and can result in protein misfolding and aggregation, have been linked to familial amyotrophic lateral sclerosis (ALS). Cu-ATSM is an orally bioavailable, blood-brain barrier permeable complex that has traditionally been used in cellular imaging experiments to selectively label hypoxic tissue via its susceptibility ...
T38142	Phosphatidylethanolamines (soy)
	Phosphatidylethanolamine is the most abundant phospholipid in prokaryotes and the second most abundant found in the membrane of mammalian, plant, and yeast cells, comprising approximately 25% of total mammalian phospholipids. In the brain, phosphatidylethanolamine comprises almost half of the total phospholipids. It is synthesized mainly through the cytidine diphosphate-ethanolamine and phosphatidylserine decarboxylation pathways, which occur in the endoplasmic reticulum (ER) and mitochondrial m...

化合物

Cat.No: T8986

Target: Glucokinase

Cat.No: T4304

Target: Apoptosis, PERK

Cat.No: T8958

Target: GPR

Ambroxol hydrochloride

Cat.No: T6234

Synonym: Mucosolvan,Mucoangin,盐酸氨溴索,Ambroxol HCl

Target: Sodium Channel, Autophagy

Cat.No: T0920

Synonym: 氨溴索,氨溴索碱,Ambroxolum,NA-872

Target: P450, Autophagy

Cat.No: T8989

Synonym: NCGC607

Target: Others

Cat.No: T15947

Target: Antibacterial

Cat.No: T4663

Target: Others, Autophagy

Cat.No: T30480

Synonym: BIX

Target: Apoptosis

Cat.No: T6284

Synonym: AT13387,Onalespib (AT13387)

Target: HSP

Questiomycin A derivatives 18 TFA

Cat.No: T67717L

Cat.No: T11718

Synonym: JI-051

Target: Gamma-secretase

HSP27 inhibitor J2

Cat.No: T7265

Synonym: J2

Target: HSP

CBL0137 hydrochloride

Cat.No: T4361

Synonym: CBL0137,CBLC137,Curaxin 137,CBL-C137 hydrochloride,Curaxin-137 hydrochloride

Target: Others, NF-κB, p53

Cat.No: T25770

Synonym: MAL-2-11B,MAL2-11B,MAL211B,MAL 2 11B,MAL2 11B

Target: Virus Protease

Cat.No: T8990

Target: Glucokinase

Cat.No: T6248

Target: HSP

Cat.No: T15646

Target: Others

Cat.No: T3527

Synonym: TRC 051384

Target: HSP

Cat.No: T25771

Synonym: MAL3 101

Acetylbritannilactone

Cat.No: T68764

Cat.No: T19181

Synonym: D-Isofagomine,Isofagomine

Target: Others

Afegostat D-Tartrate

Cat.No: T19182

Synonym: Isofagomine D-Tartrate,D-Isofagomine D-Tartrate

Target: Others

Cat.No: T61819

Cat.No: T13076

Synonym: ICI 47699-d5,(Z)-Tamoxifen-d5,trans-Tamoxifen-d5

Target: HSP

Cat.No: T23653

Synonym: Afegostat,AT-2101,Afegostat hydrochloride,AT2101

Cat.No: T27128

Synonym: NSC716802,NSC 716802,NSC-716802,DCB3503,DCB 3503

Cat.No: T28266

Synonym: Org6906,Org 6906,Org-6906 free

Cat.No: T74277

Cat.No: T71476

Cat.No: T68383

Ac2-26 ammonium

Cat.No: T78371

Spergualin trihydrochloride

Cat.No: T36436

Cat.No: T36499

Phosphatidylethanolamines (soy)

Cat.No: T38142

Cat. No.	Product Name	Target	Signaling Pathways
T3324	Lycorine Galanthidine,Narcissine,石蒜碱,Amarylline,Belamarine,Licorine,番石榴碱	Apoptosis; Virus Protease; Antibacterial; AChR; Fatty Acid Synthase	Apoptosis; Metabolism; Microbiology/Virology; Neuroscience
	Lycorine (Narcissine) 是从金眼科植物科中提取的一种天然生物碱。它是一种具有口服活性的SCAP 抑制剂，Kd 值 15.24 nM。它也是黑色素瘤血管生成抑制剂，有用于前列腺癌和代谢疾病的研究潜力。
T36818	Questiomycin A	GPR; Antibacterial	Endocrinology/Hormones; GPCR/G Protein; Microbiology/Virology
	Questiomycin A 是一种在鲜奶油中生产的抗生素，具有抗菌和抗癌活性。 Questiomycin A 抑制细胞保护性 ER 伴侣蛋白 GRP78 的表达。
T74207	Ribostamycin
	Ribostamycin (Vistamycin) 是一种广谱氨基糖苷类抗生素 (antibiotic)。Ribostamycin 对革兰氏阴性和革兰氏阳性细菌感染有效。Ribostamycin 还抑制PDI 的伴侣活性。

天然产物

Cat.No: T3324

Synonym: Galanthidine,Narcissine,石蒜碱,Amarylline,Belamarine,Licorine,番石榴碱

Target: Apoptosis, Virus Protease, Antibacterial, AChR, Fatty Acid Synthase

Cat.No: T36818

Target: GPR, Antibacterial

Cat.No: T74207

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