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31

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T11564	HIV-1 inhibitor-3	Others	Others
	HIV-1 inhibitor-3 is an HIV infection inhibitor.
T11567	HIV-1 integrase inhibitor 3	Others	Others
	HIV-1 integrase inhibitor 3 is an HIV-1 integrase strand transfer (INST) inhibitor (IC50: 2.7 nM).
T9854	HIV-1 inhibitor-6 3-Pyridinecarboxamide, 1,4-dihydro-1-methyl-N-(5-nitro-1,2-benzisothiazol-3-yl)-4-oxo-	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	HIV-1 inhibitor-6 (3-Pyridinecarboxamide, 1,4-dihydro-1-methyl-N-(5-nitro-1,2-benzisothiazol-3-yl)-4-oxo-) 是一种有效的HIV-1 pre-mRNA 选择性剪接抑制剂，可以阻断HIV 复制。
T11074	Dolutegravir intermediate-1 1-(2,2-dimethoxyethyl)-5-methoxy-6-methoxycarbonyl-4-oxopyridine-3-carboxylic acid,1-(2,2-dimethoxyethyl)-5-methoxy-6-(methoxycarbonyl)-4-oxo-1,4-dihydropyridine-3-carboxylic acid	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	Dolutegravir intermediate-1 (1-(2,2-dimethoxyethyl)-5-methoxy-6-(methoxycarbonyl)-4-oxo-1,4-dihydropyridine-3-carboxylic acid) 是 Dolutegravir 的一种新合成中间体。它是一种整合酶抑制剂，有潜力研究人类免疫缺陷病毒 (HIV)-1 感染。
T7700	Lersivirine 3-氰基-5-[[3,5-二乙基-1-(2-羟基乙基)-1H-吡唑-4-基]氧基]苯腈,Lersivirine(UK 453061),UK-453061	HIV Protease; Reverse Transcriptase	Microbiology/Virology; Proteases/Proteasome
	Lersivirine (UK-453061) 是非核苷逆转录的抑制剂 (NNRTI)，有效抑制 NNRTI 耐药病毒。它对野生型人类免疫缺陷病毒和临床相关 NNRTI 耐药菌株显示出强大的抗逆转录病毒活性。
T6418	BMS-378806 BMS378806,BMS-806,1-[(2R)-4-苯甲酰基-2-甲基-1-哌嗪基]-2-(4-甲氧基-1H-吡咯并[2,3-B]吡啶-3-基)-1,2-乙二酮	gp120/CD4; HIV Protease	Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	BMS-378806 (BMS-806) 是一种 HIV-1 抑制剂，可选择性抑制 HIV-1 gp120 结合到 CD4 受体，EC50为 0.85-26.5 nM。
T5949	Dideoxyadenosine
	2',3'-Dideoxyadenosine 是HIV 复制抑制剂，具有抗逆转录病毒活性和抗病毒的作用[1]。
T10133	3'-Azido-3'-deoxy-5-methylcytidine	Antiviral; HIV Protease	Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	3'-Azido-3'-deoxy-5-methylcytidine 抑制 HIV-1 逆转录酶 (EC50 = 0.06 μM)，是异嗜性鼠白血病相关逆转录病毒 (XMRV, CC50 = 43.5 μM) 的有效抑制剂。
T14313	Apricitabine AVX754,SPD754	HIV Protease; DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology; Proteases/Proteasome
	Apricitabine (SPD754) 是一种具有高选择性和口服活性的HIV-1逆转录酶抑制剂(Ki=0.08μM)，是2′-脱氧-3′-氧-4′-硫代胞苷(dOTC)的(-)对映体。 Apricitabine 对DNA 聚合酶α、β和γ具有抑制作用，Ki 值分别为300μM、12μM 和112.25μM。Apricitabine 在抗逆转录病毒HIV 感染者中显示出良好的抗逆转录病毒治疗效果，具有良好的耐受性和较低的选择性抗性。
T0682	Lamivudine GR109714X,BCH-189,拉米夫定	HIV Protease; Reverse Transcriptase	Microbiology/Virology; Proteases/Proteasome
	Lamivudine (BCH-189) 是一种核苷逆转录酶抑制剂，可抑制HIV 逆转录酶1和2 以及乙型肝炎病毒的逆转录酶。
T2279	Tizoxanide 替唑尼特,Desacetyl-nitazoxanide,TIZ	Antiviral; HIV Protease; Antibacterial; Autophagy	Autophagy; Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	Tizoxanide (Desacetyl-nitazoxanide) 是 Nitazoxanide 活性代谢物，有抗HIV-1的活性。Nitazoxanide 可抗细菌和多种病毒复制。
T10603	BRD-6929	HIV Protease; HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair; Microbiology/Virology; Proteases/Proteasome
	BRD-6929 是一种选择性的脑渗透性的HDAC1和HDAC2抑制剂，IC50值为 1 和 8 nM。它对 HDAC1 和 HDAC2 有高亲和力，Ki 值为 0.2 和 1.5 nM。它可研究情绪相关行为。
T24266	KNI-1657
	KNI-1657 is a potent and selective HIV-1 protease inhibitor (Anti-HIV-1 pNL4-3, EC50: 3 nM). KNI-1657 is a highly potent HIV-1 Protease Inhibitor against Lopinavir.
T64131	HIV-1 inhibitor-17
	HIV-1 inhibitor-18 是一种 HIV-1 衣壳的有效抑制剂，能够作用于 HIV-1 NL4-3 病毒株 (EC50: 2.57 μM)。HIV-1 inhibitor-18 表现出一定的细胞毒性，其 MT-4CC50 值大于8.55。
T63687	HIV-1 inhibitor-18
	HIV-1 inhibitor-18 是 HIV-1 衣壳的有效抑制剂，能够作用于 HIV-1 NL4-3 病毒株 (EC50: 5.14 μM)，并表现出一定的细胞毒性 (MT-4CC50>9.51)。
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。
T10986	DDX3-IN-1	Others	Others
	DDX3-IN-1 is a DEAD-box polypeptide 3 (DDX3) inhibitor with CC50 of 50 and 36 μM for HIV and HCV, respectively. Antiviral activity.
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。
T60342	HIV-1 inhibitor-47
	HIV-1 inhibitor-47 is a compound that effectively inhibits HIV-1 by preventing the vif-dependent degradation of human APOBEC3G. It has a notable inhibition effect, with an IC50 value of 14.33 μM. Additionally, HIV-1 inhibitor-47 is involved in the synthesis of derivatives of 1-(2-pyrimidinyl)piperazine, which have the potential to exhibit antianxiety, antidepressant, and antipsychotic effects [1] [2] [3].
TNU0208	2’,3’-Dideoxy-3’-fluorocytidine
	Nucleoside Derivatives - 2’,3’-Dideoxy-nucleosides, Fluoro-modified nucleosides, 3’-Modified nucleosides; Drugs and Inhibitors; HIV-1 inhibitor
T78950	HIV-1 protease-IN-8	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	HIV-1protease-IN-8（compound 34b）是一款高效的HIV-1蛋白酶抑制剂，其IC50为0.32 nM。该化合物对野生型HIV-1（HIV-1NL4-3）及耐药变体（HIV-1MDR）的IC50分别为0.29 μM与1.90 μM，表明其对这两种型别均展现出显著的抗病毒效果。
T78737	NNRTIs-IN-3	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	NNRTIs-IN-3（化合物8）作为一种HIV-1非核苷逆转录酶抑制剂，表现出较高的效力（EC50=0.01 µM）。
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。
T79579	ddUTP 2′,3′-Dideoxyuridine-5′-triphosphate	Reverse Transcriptase	Microbiology/Virology
	ddUTP (2′,3′-Dideoxyuridine-5′-triphosphate) 作为HIV与AMV逆转录酶的选择性抑制剂，其Ki为0.05 µM及1 µM。ddUTP在dTTP位点掺入生长中的DNA链，从而抑制其进一步的链延伸。
T60356	Stavudine sodium
	Stavudine (d4T) sodium 是一种口服活性核苷逆转录酶抑制剂 (NRTI)，具有抗HIV-1和HIV-2的活性。Stavudine sodium 还抑制线粒体 DNA (mtDNA) 的复制。Stavudine sodium 降低 NLRP3 炎症小体激活并调节淀粉样 β 自噬。Stavudine sodium 诱导细胞凋亡。
T61679	Abacavir monosulfate
	Abacavir monosulfate is an orally active, competitive nucleoside reverse transcriptase inhibitor that effectively inhibits HIV replication. Additionally, it exhibits anticancer properties in prostate cancer cell lines, and has the ability to penetrate the blood-brain-barrier and suppress telomerase activity [1] [2] [3].
T74513	RPR103611
	RPR103611，一个桦木酸衍生物，作为HIV-1入侵抑制剂表现出高效性，其对CCR5（热带）病毒YU2、CXCR4（热带）病毒NL4-3及双热带病毒89.6的IC50分别达到80、0.27和0.17。
T61193	DDX3-IN-2
	DDX3-IN-2, a potent inhibitor of DEADbox polypeptide 3 (DDX3), demonstrates remarkable activity against the target with an IC50 value of 0.3 μM. Notably, this compound exhibits a wide range of antiviral effects, showcasing its efficacy against various viral strains. Importantly, DDX3-IN-2 exhibits the potential to overcome resistance observed in the context of HIV [1].
T73986	ONX-0914 TFA
	ONX-0914 (PR-957) TFA 为针对免疫蛋白酶体中的LMP7（低分子量多肽-7）的选择性抑制剂，LMP7为类糜蛋白酶亚单位。该化合物通过抑制细胞因子产生，减缓实验性关节炎进展，并已证实为分枝杆菌蛋白酶体的非竞争性不可逆抑制剂（Ki=5.2 μM）。此外，ONX-0914 TFA 能通过HSF-1介导的p-TEFb活化，激活潜伏的HIV-1。
T60799	Peldesine dihydrochloride
	Peldesine (BCX 34) dihydrochloride 是一种有效的，竞争性，可逆和口服活性的嘌呤核苷磷酸化酶 (PNP) 抑制剂，对人，大鼠和小鼠红细胞 (RBC)PNP 的 IC50分别为 36 nM，5 nM 和 32 nM。Peldesine dihydrochloride 还是一种 T 细胞 (T-cell) 增殖抑制剂，IC50为 800 nM。Peldesine dihydrochloride 可用于皮肤 T 细胞淋巴瘤，牛皮癣和 HIV 感染的研究。
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...

化合物

HIV-1 inhibitor-3

Cat.No: T11564

Target: Others

HIV-1 integrase inhibitor 3

Cat.No: T11567

Target: Others

HIV-1 inhibitor-6

Cat.No: T9854

Synonym: 3-Pyridinecarboxamide, 1,4-dihydro-1-methyl-N-(5-nitro-1,2-benzisothiazol-3-yl)-4-oxo-

Target: HIV Protease

Dolutegravir intermediate-1

Cat.No: T11074

Synonym: 1-(2,2-dimethoxyethyl)-5-methoxy-6-methoxycarbonyl-4-oxopyridine-3-carboxylic acid,1-(2,2-dimethoxyethyl)-5-methoxy-6-(methoxycarbonyl)-4-oxo-1,4-dihydropyridine-3-carboxylic acid

Target: HIV Protease

Cat.No: T7700

Synonym: 3-氰基-5-[[3,5-二乙基-1-(2-羟基乙基)-1H-吡唑-4-基]氧基]苯腈,Lersivirine(UK 453061),UK-453061

Target: HIV Protease, Reverse Transcriptase

Cat.No: T6418

Synonym: BMS378806,BMS-806,1-[(2R)-4-苯甲酰基-2-甲基-1-哌嗪基]-2-(4-甲氧基-1H-吡咯并[2,3-B]吡啶-3-基)-1,2-乙二酮

Target: gp120/CD4, HIV Protease

Dideoxyadenosine

Cat.No: T5949

3'-Azido-3'-deoxy-5-methylcytidine

Cat.No: T10133

Target: Antiviral, HIV Protease

Cat.No: T14313

Synonym: AVX754,SPD754

Target: HIV Protease, DNA/RNA Synthesis

Cat.No: T0682

Synonym: GR109714X,BCH-189,拉米夫定

Target: HIV Protease, Reverse Transcriptase

Cat.No: T2279

Synonym: 替唑尼特,Desacetyl-nitazoxanide,TIZ

Target: Antiviral, HIV Protease, Antibacterial, Autophagy

Cat.No: T10603

Target: HIV Protease, HDAC

Cat.No: T24266

HIV-1 inhibitor-17

Cat.No: T64131

HIV-1 inhibitor-18

Cat.No: T63687

HIV-1 integrase inhibitor 10

Cat.No: T72162

Cat.No: T10986

Target: Others

Reverse transcriptase-IN-3

Cat.No: T72203

HIV-1 inhibitor-47

Cat.No: T60342

2’,3’-Dideoxy-3’-fluorocytidine

Cat.No: TNU0208

HIV-1 protease-IN-8

Cat.No: T78950

Target: HIV Protease

Cat.No: T78737

Target: HIV Protease

Cat.No: FL0097

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

Cat.No: T79579

Synonym: 2′,3′-Dideoxyuridine-5′-triphosphate

Target: Reverse Transcriptase

Stavudine sodium

Cat.No: T60356

Abacavir monosulfate

Cat.No: T61679

Cat.No: T74513

Cat.No: T61193

Cat.No: T73986

Peldesine dihydrochloride

Cat.No: T60799

Cat.No: T35762

Cat. No.	Product Name	Target	Signaling Pathways
T16791	Rottlerin Mallotoxin,NSC 56346,粗糠柴苦素,NSC 94525	CaMK; Apoptosis; Others; HIV Protease; PKA; PKC; Autophagy	Apoptosis; Autophagy; Chromatin/Epigenetic; Cytoskeletal Signaling; Microbiology/Virology; Neuroscience; Others; Proteases/Proteasome; Tyrosine Kinase/Adaptors
	Rottlerin (NSC-56346) 是一种从Mallotus Philippinensis 中得到的天然产物，是 PKC 的特异性抑制剂，抑制HIV-1整合和狂犬病病毒感染。它通过活化 caspase 3 诱导细胞凋亡.
T10928	Cytochalasin A	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	Cytochalasin A is a cell-permeable fungal toxin and is an oxidized derivative of cytochalasin B. Cytochalasin A is an inhibitor of HIV-1 protease (IC50 = 3 μM), inhibits actin polymerization and interferes with microtubule assembly by reacting with sulfhy
TN4605	Myriceric acid B	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	Myriceric acid B is a potent HIV-1 entry inhibitor targeting gp41 and can serve as a lead compound for developing novel anti-HIV-1 drug. Myriceric acid B scavenges DPPH free radicals with IC50 value of 21.8 uM, it inhibits aromatase activity with IC50 val

天然产物

Cat.No: T16791

Synonym: Mallotoxin,NSC 56346,粗糠柴苦素,NSC 94525

Target: CaMK, Apoptosis, Others, HIV Protease, PKA, PKC, Autophagy

Cat.No: T10928

Target: HIV Protease

Myriceric acid B

Cat.No: TN4605

Target: HIV Protease

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