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33

抑制剂 & 化合物

9

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T21000	PiB 2-(4-(二甲基氨基)苯基)苯并[D]噻唑-6-醇,Pittsburgh Compound-B,6-OH-BTA-1	Others	Others
	PiB (Pittsburgh Compound-B) 是分析 11C-PiB 的标准品。 11C-PiB 是一种用于阿尔茨海默病诊断的 β-淀粉样蛋白 PET 成像示踪剂。
T29476	6-OH-BTA-0 Pittsburgh Compound-B precursor,11C-PiB Precursor
	6-OH-BTA-0 is the precursor for preparing 11C-PiB, which is a β-amyloid PET imaging tracer for Alzheimer's disease diagnosis.
T16994	Pimitespib TAS-116	HSP	Cytoskeletal Signaling; Metabolism
	Pimitespib (TAS-116) 是一种 ATP 竞争性和高度特异性的 HSP90α/HSP90β 抑制剂，Ki 值分别为 34.7 nM 和 21.3 nM。
T28225	Obicetrapib TA8995,AMG899,Obicetrapib (free base),AMG 899,AMG-899,Obicetrapib,TA-8995	CETP	Metabolism
	Obicetrapib (AMG-899) 是胆固醇酯转移蛋白的抑制剂。
T19764	Trepibutone AA-149,Colibil, Supacal,AA149,AA 149,曲匹布通	Others	Others
	Trepibutone (AA-149) 是一种酸性药物，具有不依赖于 pH 值的释放能力。
T1928	Anacetrapib 安塞曲匹,MK-0859	CETP	Metabolism
	Anacetrapib (MK-0859) 是 CETP 的抑制剂，能够抑制 rhCETP (IC50:7.9±2.5 nM) 和 C13S CETP 突变型 (IC50:11.8±1.9 nM) 的活性。
T8987	Epiblastin A	Casein Kinase	Metabolism; Stem Cells
	Epiblastin A 是 ATP 竞争性的酪蛋白激酶 1 (CK1) 抑制剂，能够抑制 CK1α (IC50:8.9 µM)、 CK1δ (IC50:0.5 µM)、CK1 ɛ (IC50:4.7 µM)。它能够抑制 CK1 诱导外胚层干细胞重编程为胚胎干细胞。
T2499	Torcetrapib CP-529414,托彻普	CETP	Metabolism
	是胆固醇酯转移蛋白 (CETP) 选择性抑制剂。根据人血浆的抑制曲线，Torcetrapib (CP-529414) 对CETP 的最有效浓度为 37 nM。
T2309	Ganetespib STA-9090	Apoptosis; HSP; HIF	Angiogenesis; Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; Metabolism
	Ganetespib (STA-9090) 是一种热休克蛋白 90 抑制剂，通过抑制 HIF-1α 和 STAT3 对大肠癌具有抗血管生成作用。它还具有细胞毒性。
T1989	Luminespib AUY922,VER-52296,NVP-AUY922	Apoptosis; HSP; Autophagy	Apoptosis; Autophagy; Cytoskeletal Signaling; Metabolism
	Luminespib (VER-52296) 是一种 HSP90抑制剂，抑制 HSP90α 和 HSP90β 的 IC50分别为 7.8 和 21 nM。
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。
T10979	DCPIB	Potassium Channel; Chloride channel	Membrane transporter/Ion channel
	DCPIB 是选择性可逆体积调节性阴离子通道抑制剂，抑制肿胀激活氯电流，在 CPAE 细胞中，IC50值为 4.1 μM。它能够电压依赖性激活钾离子通道 TREK1 和 TRAAK，抑制 TRESK、TASK1 和 TASK3的 IC50值分别为 0.14、0.95 和 50.72 μM。
T6262	Evacetrapib LY2484595	CETP	Metabolism
	Evacetrapib (LY2484595) 是 CETP 的选择性抑制剂，在人血浆中，抑制人重组 CETP 蛋白 (IC50:5.5 nM) 和 CETP (IC50:36 nM) 活性。
T6048	Dalcetrapib JTT-705,达塞曲匹,RO4607381	CETP	Metabolism
	Dalcetrapib (RO4607381) 是rhCETP 抑制剂(IC50:0.2 μM)，具有增加血浆中HDL 胆固醇含量的作用。
T2278	Piboserod SB-207266,N-[(1-丁基哌啶-4-基)甲基]-3,4-二氢-2H-[1,3]恶嗪并[3,2-a]吲哚-10-甲酰胺	5-HT Receptor	GPCR/G Protein; Neuroscience
	Piboserod (SB-207266) 是一种5-HT4选择性抑制剂。
T62670	Cemdomespib
	Cemdomespib (KU-596) 是一种高效的二代 Hsp90 调节剂。Cemdomespib 能够诱导热休克反应，诱导 Hsp70 水平，具有神经保护作用。Cemdomespib 具有改善糖尿病周围神经病变模型感觉缺陷的疗效。
T71626	Epibestatin Hydrochloride
	Epibestatin Hydrochloride is a stabilizer of 14-3-3 PPIs, as well as a diastereoepimer of aminopeptidase inhibitor bestatin.
T28236	Onalespib lactate AT-13387 lactate,ATI-13387AU,ATI-13387,ATI 13387,ATI-13387A
	Onalespib lactate is a second-generation, potent and selective HSP90 Inhibitor with antitumor activity.
T2278L	Piboserod hydrochloride SB 207266 hydrochloride,Piboserod HCl,SB 207266A
	Piboserod HCl is a selective antagonist of 5-HT4 and muscarinic receptor.
T38391	Icapamespib PU-HZ151,Icapamespib
	Icapamespib (PU-HZ151), a potent HSP90 inhibitor, exhibits an EC50 of 5 nM and possesses the capability to cross the blood-brain barrier.
T69712	Icapamespib HCl
	Icapamespib, also known as PU-HZ 151, is a heat shock protein 90 (HSP90) inhibitor. PU-HZ151 showed EC50 of 5 nM in the FP assay as compared to 11 nM for PU-H71 and a logD of 2.37 as compared to 1.21 for PU-H71. PU-HZ151 and radiolabeled PU-HZ151 showed selectivity for epichaperomes over the individual chaperome members. Icapamespib demonstrated the ability to productively engage the target in cells, mice, and humans.
T70462	Pibrozelesin
	Pibrozelesin is a water-soluble derivative of duocarmycin B2 that alkylates DNA by binding to adenine-thymine (A-T)-rich sequences in the minor groove of DNA, thereby inhibiting DNA replication and inducing apoptosis.
T74131	Epiboxidine hydrochloride
	Epiboxidine hydrochloride 是一种有效的选择性神经nAChR 激动剂，对大鼠和人α4β2nAChR 的Ki 分别为 0.46 nM 和 1.2 nM。Epiboxidine hydrochloride 是生物碱 Epibatidine 的甲基异恶唑类似物，也是另一种烟碱样受体激动剂 ABT 418 的类似物。
T68504	Obicetrapib calcium
	Obicetrapib calcium is a cholesteryl ester transfer protein (CETP) inhibitor. CETP inhibitors substantially increase the concentration of high-density lipoprotein cholesterol (HDL-C), which may have a possible beneficial effect for cardiovascular disease risk reduction.
T60993	Alpibectir
	Alpibectir 具有抗细菌活性。
T25379	Epibatidine 2HCl Epibatidine HCl,Epibatidine Dihydrochloride
	Epibatidine 2HCl is a potent nicotinic agonist.
T74130	Epiboxidine
	Epiboxidine 是一种有效的选择性神经nAChR 激动剂，对大鼠和人α4β2nAChR 的Ki 分别为 0.46 nM 和 1.2 nM。Epiboxidine 是生物碱 Epibatidine 的甲基异恶唑类似物，也是另一种烟碱样受体激动剂 ABT 418 的类似物。
T68505	Obicetrapib sodium
	Obicetrapib sodium is a cholesteryl ester transfer protein (CETP) inhibitor. CETP inhibitors substantially increase the concentration of high-density lipoprotein cholesterol (HDL-C), which may have a possible beneficial effect for cardiovascular disease risk reduction.
T68503	Obicetrapib potassium
	Obicetrapib potassium is a cholesteryl ester transfer protein (CETP) inhibitor. CETP inhibitors substantially increase the concentration of high-density lipoprotein cholesterol (HDL-C), which may have a possible beneficial effect for cardiovascular disease risk reduction.
T68632	Pibaxizine
	Pibaxizine is diphenylmethyl piperazine derivatives. It is a histamine H1 receptor antagonist.
T68760	Luminespib mesylate
	Luminespib, also known as AUY-922, NVP-AUY922, VER52296, is a derivative of 4,5-diarylisoxazole and a third-generation heat shock protein 90 (Hsp90) inhibitor with potential antineoplastic activity. Hsp90 inhibitor AUY922 has been shown to bind with high affinity to and inhibit Hsp90, resulting in the proteasomal degradation of oncogenic client proteins; the inhibition of cell proliferation; and the elevation of heat shock protein 72 (Hsp72) in a wide range of human tumor cell lines.
T80742	Zelavespib hydrochloride PU-H71 hydrochloride	HSP	Cytoskeletal Signaling; Metabolism
	Zelavespib (PU-H71) hydrochloride is a potent Hsp90 inhibitor with an IC50 of 51 nM in MDA-MB-468 cells.
T73495	q-FTAA
	q-FTAA 与 Aβ1-42 原纤维结合，对 Aβ1-42 原纤维和阿尔茨海默病 PIB 结合复合物 (ADPBC) 的 EC50值分别为 330-630，300-500 nM。q-FTAA 具有研究阿尔茨海默病 (AD) 的潜力。

化合物

Cat.No: T21000

Synonym: 2-(4-(二甲基氨基)苯基)苯并[D]噻唑-6-醇,Pittsburgh Compound-B,6-OH-BTA-1

Target: Others

Cat.No: T29476

Synonym: Pittsburgh Compound-B precursor,11C-PiB Precursor

Cat.No: T16994

Synonym: TAS-116

Target: HSP

Cat.No: T28225

Synonym: TA8995,AMG899,Obicetrapib (free base),AMG 899,AMG-899,Obicetrapib,TA-8995

Target: CETP

Cat.No: T19764

Synonym: AA-149,Colibil, Supacal,AA149,AA 149,曲匹布通

Target: Others

Cat.No: T1928

Synonym: 安塞曲匹,MK-0859

Target: CETP

Cat.No: T8987

Target: Casein Kinase

Cat.No: T2499

Synonym: CP-529414,托彻普

Target: CETP

Cat.No: T2309

Synonym: STA-9090

Target: Apoptosis, HSP, HIF

Cat.No: T1989

Synonym: AUY922,VER-52296,NVP-AUY922

Target: Apoptosis, HSP, Autophagy

Cat.No: T6284

Synonym: AT13387,Onalespib (AT13387)

Target: HSP

Cat.No: T10979

Target: Potassium Channel, Chloride channel

Cat.No: T6262

Synonym: LY2484595

Target: CETP

Cat.No: T6048

Synonym: JTT-705,达塞曲匹,RO4607381

Target: CETP

Cat.No: T2278

Synonym: SB-207266,N-[(1-丁基哌啶-4-基)甲基]-3,4-二氢-2H-[1,3]恶嗪并[3,2-a]吲哚-10-甲酰胺

Target: 5-HT Receptor

Cat.No: T62670

Epibestatin Hydrochloride

Cat.No: T71626

Onalespib lactate

Cat.No: T28236

Synonym: AT-13387 lactate,ATI-13387AU,ATI-13387,ATI 13387,ATI-13387A

Piboserod hydrochloride

Cat.No: T2278L

Synonym: SB 207266 hydrochloride,Piboserod HCl,SB 207266A

Cat.No: T38391

Synonym: PU-HZ151,Icapamespib

Icapamespib HCl

Cat.No: T69712

Cat.No: T70462

Epiboxidine hydrochloride

Cat.No: T74131

Obicetrapib calcium

Cat.No: T68504

Cat.No: T60993

Epibatidine 2HCl

Cat.No: T25379

Synonym: Epibatidine HCl,Epibatidine Dihydrochloride

Cat.No: T74130

Obicetrapib sodium

Cat.No: T68505

Obicetrapib potassium

Cat.No: T68503

Cat.No: T68632

Luminespib mesylate

Cat.No: T68760

Zelavespib hydrochloride

Cat.No: T80742

Synonym: PU-H71 hydrochloride

Target: HSP

Cat.No: T73495

Cat. No.	Product Name	Target	Signaling Pathways
T5S2361	Epiberberine	ERK; Beta-Secretase; MEK; BACE; AMPK; AChR; AChE	Chromatin/Epigenetic; MAPK; Neuroscience; PI3K/Akt/mTOR signaling
	Epiberberine 是一种从黄连中得到的生物碱，是AChE 和BChE 抑制剂，和非竞争性BACE1抑制剂。在 3T3-L1 细胞分化早期，它能够下调 Raf/MEK1/2/ERK1/2 和 AMPKα/Akt 信号通路。它具有抗氧化作用，能够清除 ONOO-，可用于阿尔滋海默症和糖尿病的研究。
T5514	Epibrassinolide 24-Epibrassinolide,B1105,表油菜素内酯,BP55	Apoptosis	Apoptosis
	Epibrassinolide (BP55) 是一种广泛存在的植物生长激素，具有缓解植物重金属和农药胁迫潜力。它在各种癌细胞中是一种潜在的凋亡诱导剂。
T8187	Tetrahydroepiberberine	Others; Influenza Virus; Antifungal	Microbiology/Virology; Others
	Tetrahydroepiberberine 是从Corydalis impatiens(Pall) 中分离得到的一种异喹啉生物碱，具有抗真菌和选择性抑制 PI-3 病毒活性的作用。
TN2023	8-Oxoepiberberine 氧化表小檗碱,Oxyepiberberine	Others	Others
	8-Oxoepiberberine (Oxyepiberberine) 是口服左金方剂后血清中产生的生物碱代谢物。其中左金方剂是一种中药，可以用于胃肠道疾病的研究。
T2S0765	Epibetulinic acid	NO Synthase; Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	Epibetulinic acid 对细菌内毒素刺激的小鼠巨噬细胞 (RAW 264.7) 中 NO 和前列腺素 E(2) 的产生具有有效的抑制作用，IC50分别为 0.7 和 0.6 μM，具有抗炎活性。
TN2986	3a-Epiburchellin	Others	Others
	3a-Epiburchellin 是一种天然产物，可用于生命科学领域的相关研究。其产品编号为 TN2986，CAS号为 155551-61-4。
T8306	Epiberberine chloride 表小檗碱氯化物,Epiberberine (chloride),盐酸表小檗碱	Reactive Oxygen Species; Beta-Secretase; BACE; AChR; AChE	Immunology/Inflammation; Metabolism; Neuroscience; NF-κB
	Epiberberine chloride (Epiberberine (chloride)) 是一种从黄连中得到的生物碱，是一种AChE 和BChE 抑制剂，和非竞争性的BACE1抑制剂。它具有抗氧化作用，能够清除 ONOO-，可用于研究阿尔滋海默症和糖尿病。
TN2756	2-Epi-3a-epiburchellin	Others	Others
	2-Epi-3a-epiburchellin 是一种天然产物，可用于生命科学领域的相关研究。其产品编号为 TN2756，CAS号为 57457-99-5。
TN3317	9-Epiblumenol B	Others	Others
	9-Epiblumenol B 是一种天然产物，可用于生命科学领域的相关研究。其产品编号为 TN3317，CAS号为 22841-42-5。

天然产物

Cat.No: T5S2361

Target: ERK, Beta-Secretase, MEK, BACE, AMPK, AChR, AChE

Epibrassinolide

Cat.No: T5514

Synonym: 24-Epibrassinolide,B1105,表油菜素内酯,BP55

Target: Apoptosis

Tetrahydroepiberberine

Cat.No: T8187

Target: Others, Influenza Virus, Antifungal

8-Oxoepiberberine

Cat.No: TN2023

Synonym: 氧化表小檗碱,Oxyepiberberine

Target: Others

Epibetulinic acid

Cat.No: T2S0765

Target: NO Synthase, Prostaglandin Receptor

3a-Epiburchellin

Cat.No: TN2986

Target: Others

Epiberberine chloride

Cat.No: T8306

Synonym: 表小檗碱氯化物,Epiberberine (chloride),盐酸表小檗碱

Target: Reactive Oxygen Species, Beta-Secretase, BACE, AChR, AChE

2-Epi-3a-epiburchellin

Cat.No: TN2756

Target: Others

9-Epiblumenol B

Cat.No: TN3317

Target: Others

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