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20

抑制剂 & 化合物

3

天然产物

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Cat. No. Product Name Target Signaling Pathways
T63453 HIV-1 protease-IN-1

HIV-1 protease-IN-1HIV-1 蛋白酶的有效抑制剂 (IC50: 90 pM)。HIV-1 protease-IN-1 对 B-HIV 具有抗病毒活性 (EC50: 89 nM)。HIV-1 protease-IN-1 能够作用于 C-HIV 毒株 ZM246 (EC50: 13.59 nM) 以及 C-HIVIndie (EC50: 8.23 nM)。
T74939 HIV protease-IN-1

HIVprotease-IN-1 (compound 1·succinate) 是一种有效的HIV 蛋白酶 (HIV protease) 非肽抑制剂,可用于艾滋病的研究。
T63733 HIV-1 protease-IN-6

HIV-1 protease-IN-6 (compound 17d) 是 HIV-1 蛋白酶 (HIV-1 protease) 的有效抑制剂 (IC50: 21 pM, Ki: 4.7 pM)。HIV-1 protease-IN-6 对 DRV (darunavir) 耐药病毒突变体具有显著的抗病毒效果 (antiviral activity),抑制强度甚至超过对野生型病毒。
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-1HIV-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。
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]。
T79537 HIV-1 protease-IN-12

HIV Protease Microbiology/Virology; Proteases/Proteasome
HIV-1protease-IN-12 (compound 35b)为HIV-1蛋白酶抑制剂,具有0.51 nM的IC50值,同时对HIV耐药变体也具有抑制作用。
T79493 HIV-1 protease-IN-10

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
HIV-1protease-IN-10(化合物2)显示出对HIV-1潜伏期的逆转活性,IC50值为0.22 μM。该化合物通过与PKCδC1b结构域结合展现活性,IC50值为0.69 μM。此外,HIV-1protease-IN-10对于酯酶介导的水解表现出稳定性。
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。
T63949 HIV-1 protease-IN-2

HIV-1 protease-IN-2 是 HIV-1 protease 的有效抑制剂 (IC50: 2.53 nM)。HIV-1 protease-IN-2 对 DRV (达芦那韦)敏感或耐药性 HIV-1 突变体均表现出抗病毒效果。
T79536 HIV-1 protease-IN-11

HIV Protease Microbiology/Virology; Proteases/Proteasome
HIV-1protease-IN-11 (compound 34a) 为一抗HIV-1蛋白酶抑制剂,其IC50值为0.41 nM,并对抗耐药变异表现出显著活性。
T74942 HIV-1 protease-IN-7

HIV Protease Microbiology/Virology; Proteases/Proteasome
HIV-1protease-IN-7(化合物 16)作为一种HIV-1蛋白酶抑制剂,具有良好的口服活性,表现出优异的抑制效能(IC50=3.52 nM,EC50=37 nM)。
T79295 HIV-1 protease-IN-9

HIV Protease Microbiology/Virology; Proteases/Proteasome
HIV-1protease-IN-9 (compound 5b)为HIV-1蛋白酶抑制剂,具有0.028 nM的Ki值和66.8 nM的IC50,表现出显著的抗病毒活性。
T3335 Darunavir Ethanolate

地瑞那韦乙醇盐,UIC 94017,Darunavir Ethanolate,TMC114,达芦那韦乙醇

HIV Protease Microbiology/Virology; Proteases/Proteasome
Darunavir Ethanolate (UIC 94017) 是一种HIV 蛋白酶抑制剂,可以用于 HIV/AIDS 的相关研究。对野生型 HIV-1 蛋白酶的Ki 值为1 nM。
T76603 HIV-IN petide

HIV-IN petide 是HIV-1蛋白酶 (Ki=50 nM) 的竞争性抑制剂。
T70491 XM 323

XM 323 is an inhibitor of clinical isolates of HIV-1 in vitro and represents a novel class of non-peptidyl inhibitors of HIV-1 protease.
T28306 PD 099560

PD099560,PD-099560

PD 099560 is a non-peptide inhibitor of HIV-1 protease, a significant target enzyme in AIDS research.
T28811 SM111

SM 111,SM-111

SM111 inhibits in vitro replication of HIV-1, including strains resistant to reverse transcriptase, licensed protease, and integrase inhibitors, without major cellular toxicity.
T39345 Lopinavir Metabolite M-1

Lopinavir Metabolite M-1, an active metabolite derived from Lopinavir, effectively inhibits the HIV protease enzyme with a Ki value of 0.7 pM. Additionally, in vitro studies have revealed notable antiviral properties associated with Lopinavir Metabolite M-1.
T74990 ICeD-2

ICeD-2 是一种细胞死亡诱导剂,可诱导HIV-1感染的细胞死亡。 ICeD-2 介导的HIV-1感染细胞杀伤依赖于HIV-1蛋白酶活性。ICeD-2 可有效阻断二肽基肽酶DPP8和DPP9对 Gly-Pro-AMC 的水解。ICeD-2 显示 PBMC 中 DPP9 的强稳定性。
T76512 Ac-Ser-Gln-Asn-Tyr-Pro-Val-Val-NH2

Ac-Ser-Gln-Asn-Tyr-Pro-Val-Val-NH2 是 HIV-1蛋白酶的肽底物。Ac-Ser-Gln-Asn-Tyr-Pro-Val-Val-NH2 在肽水解测定法作为可变底物,用于量化蛋白酶的抑制作用。

化合物

HIV-1 protease-IN-1
Cat.No: T63453
Synonym:
Target:
HIV protease-IN-1
Cat.No: T74939
Synonym:
Target:
HIV-1 protease-IN-6
Cat.No: T63733
Synonym:
Target:
HIV-1 protease-IN-8
Cat.No: T78950
Synonym:
Target: HIV Protease
HIV-1 protease-IN-4
Cat.No: T74488
Synonym:
Target:
HIV-1 protease-IN-12
Cat.No: T79537
Synonym:
Target: HIV Protease
HIV-1 protease-IN-10
Cat.No: T79493
Synonym:
Target: PKC
HIV-1 protease-IN-5
Cat.No: T64112
Synonym:
Target:
HIV-1 protease-IN-2
Cat.No: T63949
Synonym:
Target:
HIV-1 protease-IN-11
Cat.No: T79536
Synonym:
Target: HIV Protease
HIV-1 protease-IN-7
Cat.No: T74942
Synonym:
Target: HIV Protease
HIV-1 protease-IN-9
Cat.No: T79295
Synonym:
Target: HIV Protease
Darunavir Ethanolate
Cat.No: T3335
Synonym: 地瑞那韦乙醇盐,UIC 94017,Darunavir Ethanolate,TMC114,达芦那韦乙醇
Target: HIV Protease
HIV-IN petide
Cat.No: T76603
Synonym:
Target:
XM 323
Cat.No: T70491
Synonym:
Target:
PD 099560
Cat.No: T28306
Synonym: PD099560,PD-099560
Target:
SM111
Cat.No: T28811
Synonym: SM 111,SM-111
Target:
Lopinavir Metabolite M-1
Cat.No: T39345
Synonym:
Target:
ICeD-2
Cat.No: T74990
Synonym:
Target:
Ac-Ser-Gln-Asn-Tyr-Pro-Val-Val-NH2
Cat.No: T76512
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
TN1059 Ganoderic acid B

IL Receptor; HIV Protease; JAK; STAT Angiogenesis; Chromatin/Epigenetic; Immunology/Inflammation; JAK/STAT signaling; Microbiology/Virology; Proteases/Proteasome; Stem Cells
Ganoderic acid B 是从灵芝中分离的一种三萜类天然产物。它是端粒酶抑制剂,抑制 Epstein-Barr 病毒抗原的活化。它是 HIV-1 蛋白酶抑制剂。
TMA1012 Ganoderiol F

Androgen Receptor; HIV Protease; Autophagy Autophagy; Endocrinology/Hormones; Microbiology/Virology; Proteases/Proteasome
Ganoderiol F has anti-inflammatory, cytotoxic and anti-HIV activity, it inhibits activity of topoisomerases in vitro, and it inhibits human immunodeficiency virus-1 protease with IC(50) values of 20-40 microM. It induced HO-1 expression, activation of the mitogen-activated protein kinase EKR and up-regulation of cyclin-dependent kinase inhibitor p16 and suppressed lipopolysaccharide (LPS)-induced nitric oxide (NO) production.
TN1660 Ganoderic acid C1

灵芝酸 C1,灵芝酸C1

IL Receptor; TNF; NF-κB; MAPK; COX; HIV Protease; DNA/RNA Synthesis Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Immunology/Inflammation; MAPK; Microbiology/Virology; Neuroscience; NF-κB; Proteases/Proteasome
Ganoderic acid C1 是分离自 G. lucidum 中的天然产物,能够抑制小鼠巨噬细胞TNF-α 的生成。

天然产物

Ganoderic acid B
Cat.No: TN1059
Synonym:
Target: IL Receptor, HIV Protease, JAK, STAT
Ganoderiol F
Cat.No: TMA1012
Synonym:
Target: Androgen Receptor, HIV Protease, Autophagy
Ganoderic acid C1
Cat.No: TN1660
Synonym: 灵芝酸 C1,灵芝酸C1
Target: IL Receptor, TNF, NF-κB, MAPK, COX, HIV Protease, DNA/RNA Synthesis
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