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27

抑制剂 & 化合物

6

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Cat. No.	Product Name	Target	Signaling Pathways
T64048	HIV-IN-5
	HIV-IN-5 (compound 5r) 是 HIV-1 的有效抑制剂 (IC50: 0.16 μM)。HIV-IN-5 能够与 NNIBP (NNRTIs (非核苷逆转录酶抑制剂) 结合位点) 相结合。HIV-IN-5 能够抑制 HIV DNA 依赖的 DNA 聚合作用 (IC50: 2.18 μM)。
T64112	HIV-1 protease-IN-5
	HIV-1 protease-IN-5 是一种 HIV-1 protease 抑制剂 (IC50: 1.64 nM)。HIV-1 protease-IN-5 对野生型和 DRV 耐药型 HIV-1 表现出明显的作用。
T63143	DENV-IN-5	Virus Protease; HIV Protease	Microbiology/Virology; Proteases/Proteasome
	DENV-IN-5 是一种有效且具有选择性的登革热病毒 (DENV) 抑制剂，对 DENV-I ∼ IV 的 EC50 值分别为 1.47、9.23、7.08、8.91 μM，对HIV-1IIIB 的EC50 为 0.1512 μM。
T25913L	P-113 acetate	HIV Protease; Antibacterial; Antibiotic	Microbiology/Virology; Proteases/Proteasome
	P-113 acetate 是一种源自人类唾液蛋白组氨酸 5 的抗菌肽 (AMP)，在患有口腔念珠菌病的牙龈炎和人类免疫缺陷病毒 (HIV) 患者中显示出良好的安全性和有效性。
T29037	UC-781 NSC 675186,UC781,UC 781	Antiviral; HIV Protease	Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	UC-781 (NSC-675186) 是一种高效且具有选择性的人类免疫缺陷病毒 HIV-1 非核苷类逆转录酶(NNRTI)I抑制剂，C50 值为 5 nM。UC-781 具有抗病毒活性和耐药性。UC-781状态稳定，较低的 PH 或不同温度对其影响较小。
T3360	ZK 756326 ZK756326 2HCl	CCR	Immunology/Inflammation; Microbiology/Virology
	ZK 756326 是一种选择性的非肽 CCR8 趋化因子受体激动剂（IC50：1.8 μM，在人体内；2.6 μM，在小鼠体内）。对 CCR4/5 和 CXCR3/4 没有活性，比其他 26 种 GPCR 的选择性高 28 倍（对 α2A 和 5-HT 受体的选择性较低）。诱导趋化性并抑制 Env 介导的 (HIV) 细胞-细胞融合。
T0825	Ebselen SPI-1005,PZ-51,依布硒,CCG-39161	Phosphatase; Virus Protease; Calcium Channel; COX; HIV Protease	Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience; Proteases/Proteasome
	Ebselen (CCG-39161) 是一种谷胱甘肽过氧化物酶模拟物，是电压依赖性钙通道阻断剂。它抑制Mpro 和COVID-19病毒，是HIV-1衣壳 CTD 二聚化的抑制剂，具有抗炎、抗癌和抗氧化活性。
T11549	Helioxanthin 8-1 Helioxanthin analogue 8-1	Others	Others
	Helioxanthin 8-1, an analogue of helioxanthin, exhibits significant in vitro anti-HBV/HCV/HSV-1/HIV activity with EC50 of >5/10/1.4/15 μM.
T72203	Reverse transcriptase-IN-3
	Reverse transcriptase-IN-3, 作为一种嘧啶-5-羧酰胺衍生物，主要用于抑制HIV-1。它对HIV-1野生型及其突变型病毒株均展示出高效的抑制活性。
T72162	HIV-1 integrase inhibitor 10
	HIV-1integrase inhibitor 10 是一种 HIV-1变构整合酶抑制剂 (ALLINI)，具有口服活性。HIV-1integrase inhibitor 10 可抑制 NLRepRluc 病毒在 MT-2 细胞中的生长，其 EC50值为 3-5 nM。HIV-1integrase inhibitor 10 可用于人类免疫缺陷病毒-1 (HIV-1) 的研究。
T74488	HIV-1 protease-IN-4
	HIV-1protease-IN-4 (Compound II-22) 是一种有效的HIV-1蛋白酶抑制剂。HIV-1protease-IN-4 是阿扎那韦的前体。HIV-1蛋白酶-IN-4 作为前体，与口服母体活性分子相比，将母体 1 输送到大鼠血浆中的 AUC 高 5 倍，C24 高 67 倍[1]。
T28494	R-82913 NSC 637653, 9-Cl-Tibo,R 82913,R82913. 9-Cmbib
	R-82913 is a RNA-directed DNA polymerase inhibitor. R 82913 reduce 5-HT2 receptor-mediated DOI-head-shakes in mice. R82913 inhibited the replication of thirteen different strains of HIV-1 in CEM cells with a median IC50 of 0.15 microM. R82913 was 20-fold
FL0097	beta-L-D4A 2'3'-didehydro-2'3'-dideoxyadenosine
	beta-L-D4A 是一种核苷类型的HIV-1逆转录酶抑制剂。
T83837	Rp-Thymidine-5'-O-(1-thiotriphosphate) sodium Rp-dTTP-α-S
	Rp-Thymidine-5'-O-(1-thiotriphosphate) (Rp-TTP-α-S) 是含硫核苷酸衍生物 TTP-α-S 的一个异构体。它能与HIV-1逆转录酶结合（在镁、锰酸盐和钴存在下的Kds分别为45.7、27.32和39.44 µM）。
T37874	Feglymycin
	Feglymycin is a 13-amino acid peptide originally isolated from Streptomyces that has antibacterial and antiviral activities. It is active against Gram-positive bacteria (MICs = 32-64 μg/ml) and inhibits HIV viral replication in H9 cells (IC50 = ~5 μM). Feglymycin is also active against clinical isolates of HIV-1 from clades A-D, A/E, and G (EC50s = 0.5-6.7 μM). It interacts with gp120 and inhibits HIV-1 NL4.3 binding to human soluble CD4 (EC50 = 4.4 μM) and to CD4+ SupT1 T cells by 74.5% when us...
T69081	KRH-1636
	KRH-1636 is an orally active, selective and extremely potent CXC chemokine receptor 4 antagonist. KRH-1636 exhibits a potent and selective anti-HIV-1 activity. KRH-1636 efficiently blocked replication of various T cell line-tropic (X4) HIV type 1 (HIV-1) in MT-4 cells and peripheral blood mononuclear cells through the inhibition of viral entry and membrane fusion via the CXC chemokine receptor (CXCR)4 coreceptor but not via CC chemokine receptor 5. KRH-1636 also inhibits binding of the CXC chem...
T83838	Sp-Thymidine-5'-O-(1-thiotriphosphate) sodium Sp-TTP-α-S
	Sp-Thymidine-5'-O-(1-thiotriphosphate)（Sp-TTP-α-S）是含硫核苷酸衍生物TTP-α-S的一个异构体。它能够结合HIV-1逆转录酶（在镁、锰酸盐和钴存在时，Kds分别为2.88、4.23和20.21 µM）。Sp-TTP-α-S抑制脱氧核苷酸三磷酸三磷酸水解酶SAMHD1（Ki为46 nM）。
T83670	F1 TFA Tat-IKIP (46-60),Tat-Inhibitor of NF-κB Kinase-interacting Peptide
	F1是一种抗炎肽，由HIV-1 Tat蛋白质转导域与对应于抑制因子NF-κB激酶-相互作用肽（IKIP）46-60残基的15氨基酸肽链接而成。在5 µM浓度下，F1抑制了小鼠腹腔巨噬细胞中LPS诱导的IκB激酶α（IKKα）和IKKβ的磷酸化以及NF-κB（p65）的核内转移。在体内，F1（5 mg/kg）降低了LPS诱导的脓毒症小鼠模型中IL-6、TNF-α和IL-1β的血清水平，并增加了生存率。
T83667	A11 TFA CPP-EYVQTVKSSKG
	A11是一种细胞穿透肽，由HIV-1 Tat蛋白质转导域与对应于脂联素A1 N末端第20至30残基的11氨基酸肽连接而成。它减少脂联素A1与Eph受体酪氨酸激酶A2(EphA2)的结合，并在HK1鼻咽癌(NPC)细胞中增加EphA2的泛素化。A11（10 µM）抑制HK1和5-8F NPC细胞的增殖、迁移和侵袭。在体内，A11减少5-8F和HK1 NPC小鼠异种移植模型中的肿瘤体积。
TP1910	CALP1
	Cell-permeable calmodulin (CaM) agonist that binds to the EF-hand/Ca2+-binding site; produces CaM-dependent activation of phosphodiesterase. Also binds to cytoplasmic sites on other Ca2+ channels, including NMDA and HIV-1 gp120-activated channels, inhibit
T36794	Dolutegravir O-β-D-Glucuronide
	Dolutegravir O-β-D-glucuronide is a metabolite of the HIV integrase inhibitor dolutegravir .1It is formed from dolutegravir primarily by the UDP-glucuronosyltransferase (UGT) isoform UGT1A1in vivobut is also metabolized by UGT1A9 in human liver and kidney microsomes and UGT1A3 in human intestinal microsomes.2,1 1.Liu, S.N., Lu, J.B., Watson, C.J.W., et al.Mechanistic assessment of extrahepatic contributions to glucuronidation of integrase strand transfer inhibitorsDrug Metab. Dispos.47(5)535-544...
T36490	AZT triphosphate TEA
	AZT triphosphate TFA (3'-Azido-3'-deoxythymidine-5'-triphosphate TFA) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate TFA exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate TFA also inhibits the DNA polymerase of HBV. AZT triphosphate TFA activates the mitochondria-mediated apoptosis pathway[1][2][3]. Treatment with 100 μM Zidovudine (AZT) for 48h disrupts the mitochondrial tubular network via accumulation of AZT triphosphate (AZT-TP) in ...
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...
T78579	NSC260594
	NSC260594是一种化合物，具有诱导细胞凋亡（Apoptosis）的作用。它通过与Mcl-1蛋白的浅沟结合并下调Wnt信号蛋白，抑制Mcl-1的表达。此外，NSC260594能够识别HIV的G9-G10-A11-G12 RNA四环，防止5'-UTR中的Gag蛋白结合。它被认为对抑制肿瘤生长具有潜在作用，特别是在三阴性乳腺癌（TNBC）研究中。
T37347	6'-Sialyllactose Sodium Salt 6'-Sialyllactose Sodium Salt,6'-N-Acetylneuraminyl-D-lactose
	6'-Sialyllactose consists of the monosaccharide N-acetylneuraminic acid linked to the galactosyl subunit of lactose at the 6 position. This connection is at the 3 position in the related compound, 3’-sialyllactose. Both are major milk oligosaccharides that avidly bind several viral strains, including strains of influenza, HIV-1, reovirus, and polyomavirus.[1],[2],[3],[4],[5],[6] These compounds can be used to differentiate and characterize the binding domains of viruses that recognize N-acetylne...
T16973	TAK-220	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	TAK-220 is a selective and orally bioavailable CCR5 antagonist (IC50s: 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively).
T35428	β-Rubromycin
	β-Rubromycin is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities.1 It inhibits the growth of HMO2, KATO-III, and MCF-7 cells with GI50 values of 0.5, 0.84, and <0.1 μM, respectively. β-rubromycin inhibits HIV-1 reverse transcriptase activity by 39.7% when used at a concentration of 10 μM. It also has antibacterial activity against Gram-positive bacteria. The structure of β-rubromycin was originally described as containing an ortho-quinone group,...

化合物

Cat.No: T64048

HIV-1 protease-IN-5

Cat.No: T64112

Cat.No: T63143

Target: Virus Protease, HIV Protease

Cat.No: T25913L

Target: HIV Protease, Antibacterial, Antibiotic

Cat.No: T29037

Synonym: NSC 675186,UC781,UC 781

Target: Antiviral, HIV Protease

Cat.No: T3360

Synonym: ZK756326 2HCl

Target: CCR

Cat.No: T0825

Synonym: SPI-1005,PZ-51,依布硒,CCG-39161

Target: Phosphatase, Virus Protease, Calcium Channel, COX, HIV Protease

Helioxanthin 8-1

Cat.No: T11549

Synonym: Helioxanthin analogue 8-1

Target: Others

Reverse transcriptase-IN-3

Cat.No: T72203

HIV-1 integrase inhibitor 10

Cat.No: T72162

HIV-1 protease-IN-4

Cat.No: T74488

Cat.No: T28494

Synonym: NSC 637653, 9-Cl-Tibo,R 82913,R82913. 9-Cmbib

Cat.No: FL0097

Synonym: 2'3'-didehydro-2'3'-dideoxyadenosine

Rp-Thymidine-5'-O-(1-thiotriphosphate) sodium

Cat.No: T83837

Synonym: Rp-dTTP-α-S

Cat.No: T37874

Cat.No: T69081

Sp-Thymidine-5'-O-(1-thiotriphosphate) sodium

Cat.No: T83838

Synonym: Sp-TTP-α-S

Cat.No: T83670

Synonym: Tat-IKIP (46-60),Tat-Inhibitor of NF-κB Kinase-interacting Peptide

Cat.No: T83667

Synonym: CPP-EYVQTVKSSKG

Cat.No: TP1910

Dolutegravir O-β-D-Glucuronide

Cat.No: T36794

AZT triphosphate TEA

Cat.No: T36490

Cat.No: T35762

Cat.No: T78579

6'-Sialyllactose Sodium Salt

Cat.No: T37347

Synonym: 6'-Sialyllactose Sodium Salt,6'-N-Acetylneuraminyl-D-lactose

Cat.No: T16973

Target: HIV Protease

Cat.No: T35428

Cat. No.	Product Name	Target	Signaling Pathways
T4S0797	Berberine 小檗碱,Berberin,Umbellatine,黄连素	Reactive Oxygen Species; Topoisomerase; Endogenous Metabolite; Antibacterial; Antibiotic; Autophagy	Autophagy; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; Microbiology/Virology; NF-κB
	Berberine (Umbellatine) 是从中草药黄连中分离出来的一种生物碱抗生素。它诱导活性氧生成并抑制 DNA 拓扑异构酶，具有抗肿瘤特性。
TN2951	3-(hydroxymethyl)cyclopentanone	CCR	Immunology/Inflammation; Microbiology/Virology
	3-Hydroxymethylcyclopentanone is a precursor to synthesize methyl epijasmonate. 3-Hydroxymethylcyclopentanone compounds, which are useful as intermediates in the preparation of HIV chemokine CCR-5 receptor antagonists.
TN5133	3',5,5',7-Tetrahydroxy-4',6-dimethoxyflavone	HIV Protease; Topoisomerase	DNA Damage/DNA Repair; Microbiology/Virology; Proteases/Proteasome
	5,7,3',5'-tetrahydroxy-6,4'-dimethoxyflavone exhibits anti-HIV-1 activity in the anti-syncytium assay using (∆Tat/rev)MC99 virus and 1A2 cell line system, it shows considerably activity against HIV-1 reverse transcriptase. It exhibits cytotoxic activity against P-388 cell lines, it can inhibit DNA topoisomerase IIα activity, which may be responsible for the observed cytotoxicity.
TN3152	6-Acetonyldihydrochelerythrine	ERK; BCL; Akt; HIV Protease; PPAR; p53	Apoptosis; Cytoskeletal Signaling; DNA Damage/DNA Repair; MAPK; Metabolism; Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome
	6-Acetonyldihydrochelerythrine exhibits significant antioxidant activities, it exhibits significant anti-HIV activity in H9 lymphocytes with EC50 and TI (Therapeutic Index) values of 1.77 microg/mL and 14.6, respectively. 6-Acetonyldihydrochelerythrine is
T72429	α-Lipoic Acid sodium Thioctic acid sodium,DL-α-Lipoic acid sodium,Thioctic acid sodium ; (±)-α-Lipoic acid sodium ; DL-α-Lipoic acid sodium,(±)-α-Lipoic acid sodium
	α-Lipoic Acid (Thioctic acid) sodium 是一种抗氧化剂，是线粒体酶复合物的重要辅助因子。α-Lipoic Acid sodium 可抑制NF-κB 依赖性的HIV-1LTR 活化。α-Lipoic Acid sodium 诱导内质网应激 (ERS) 介导的肝癌细胞凋亡 (apoptosis)。α-Lipoic Acid sodium 可与CPUL1 合成自组装的纳米聚合体 CPUL1-LA NA，其抗肿瘤效果优于 CPUL1。
T36438	Sporogen-AO 1
	Sporogen-AO 1 is a fungal metabolite originally isolated fromA. oryzaethat has diverse biological activities.1,2,3,4,5It inhibits HIV-1 Tat transactivation in a cell-based assay with an IC50value of 15.8 μM.4Sporogen-AO 1 is cytotoxic to HeLa, KB, and NCI H187 cancer cells (IC50s = 8.3, 9, and 5.1 μM, respectively).2,5It is active againstC. albicans(MIC = 4 mM).3 1.Tanaka, S., Wada, K., Marumo, S., et al.Structure of sporogen-ao 1, a sporogenic substance of Aspergillus oryzaeTetrahedron Lett.25(...

天然产物

Cat.No: T4S0797

Synonym: 小檗碱,Berberin,Umbellatine,黄连素

Target: Reactive Oxygen Species, Topoisomerase, Endogenous Metabolite, Antibacterial, Antibiotic, Autophagy

3-(hydroxymethyl)cyclopentanone

Cat.No: TN2951

Target: CCR

3',5,5',7-Tetrahydroxy-4',6-dimethoxyflavone

Cat.No: TN5133

Target: HIV Protease, Topoisomerase

6-Acetonyldihydrochelerythrine

Cat.No: TN3152

Target: ERK, BCL, Akt, HIV Protease, PPAR, p53

α-Lipoic Acid sodium

Cat.No: T72429

Synonym: Thioctic acid sodium,DL-α-Lipoic acid sodium,Thioctic acid sodium ; (±)-α-Lipoic acid sodium ; DL-α-Lipoic acid sodium,(±)-α-Lipoic acid sodium

Cat.No: T36438

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