HIV
抑制剂选择性比较
HIV产品
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S1009 |
Dactolisib (BEZ235)Dactolisib (BEZ235, NVP-BEZ235) 是一种双重ATP竞争性 PI3K 和 mTOR 抑制剂,在无细胞试验中,抑制 p110α/γ/δ/β 和 mTOR(p70S6K) 的 IC50 分别为 4 nM /5 nM /7 nM /75 nM /6 nM。 在 3T3TopBP1-ER 细胞中抑制 ATR,IC50 为 21 nM,而对 Akt 和 PDK1 的抑制作用很弱。Dactolisib可诱导自噬并抑制HIV-1的复制。Phase 2。 |
![]() ![]() Three-dimensional responses of MCF7/IGF-1R cells to TAM (1 μM), E2 and IGF-1. Compared to parental MCF7 cells (a), MCF7/IGF-1R cells (b) in three-dimensional (3D) culture formed bigger acini in response to IGF-1 stimulation and displayed significant TAM resistance when treated with TAM (1 μM) + E2 + IGF-1, which was removable by kinase inhibitors BMS-536924, U0126 and BEZ235 (c). Cells (10,000/well) were seeded in 96-well plates. Acini were formed on 100% Matrigel and cultured for 14 days in starving medium containing 2% Matrigel and 5% charcoal/dextran-stripped fetal bovine serum with the treatments as indicated. Concentrations used: TAM (1 μM), E2 (1 nM) and IGF-1 (100 ng/mL). Confocal image original magnification, × 20. Red, rhodamine phalloidin (actin). Blue, Hoechst blue stain. Results are representative of two individual experiments. |
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S1208 |
Doxorubicin (Adriamycin) HClDoxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl是一种抗生素类试剂,可抑制DNA topoisomerase II,并在肿瘤细胞中诱导DNA损伤、线粒体自噬和凋亡。Doxorubicin 可降低 AMPK的基础磷酸化。Doxorubicin 可应用于HIV感染病人的联合治疗,但是在免疫治疗中有将HBV重活化的风险。 |
![]() ![]() Cell viabilities with increasing concentrations of cisplatin (CP) and doxorubicin (DOXO) under normoxic and hypoxic condition for 48 hours were determined by MTT assay. IC50 values are presented as the means ?SDs (n=4) and * denotes p<0.05. |
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S1230 |
Flavopiridol (L86-8275)Flavopiridol (L86-8275, Alvocidib, NSC 649890, HMR-1275) 与ATP竞争性抑制CDKs,包括CDK1、CDK2、CDK4、CDK6和CDK9的IC50范围为20-100 nM。作用于CDK1、2、4、6、9比作用于CDK7更具有选择性。Flavopiridol最初被发现能抑制EGFR和PKA。Flavopiridol可诱导自噬和内质网应激反应。Flavopiridol可阻滞HIV-1的复制。Phase 1/2。 |
![]() ![]() (C) In vivo treatment of Tg:Pomc-Pttg;Pomc-eGFP embryos with small-molecule CDK inhibitors (50 μM) or 0.2% DMSO as control from 18 to 40 hpf. One hundred to one hundred fifty embryos were treated with each compound. Representative images of live embryos are shown with gross morphology (Right) and pituitary Pomc-GFP-positive cells at higher magnification (Left) at 40 hpf. Embryos exposed to flavopiridol developed early developmental defect before pituitary POMC cell ontogeny occurs. (D) Relative expression of pituitary Pomc-eGFP fluorescence analyzed using Volocity 5.2 software (Improvision; mean ±SE of relative expression, n = 7). (E) R-roscovitine specifically suppresses expansion of pituitary POMC cells overexpressing zPttg from 18 to 48 hpf. Double transgenic Tg:Pomc-Pttg;Prl-RFP embryos were generated by breeding Tg:Pomc-Pttg fish with a previously generated PRL-RFP transgenic line, in which RFP was targeted to pituitary lactotrophs by a zebrafish Prolactin promoter (34). Representative fluorescent microscopy of pituitary POMC-eGFP (a and b) and PRL-RFP (c and d) expression in live Tg:Pomc-Pttg; Pomc-eGFP and Tg:Pomc-Pttg;Prl-RFP embryos treated with 0.2% DMSO (a and c) or 50 μM R-roscovitine (b and d). (F) Relative expression of pituitary POMC-eGFP or PRL-RFP fluorescence were analyzed (mean ±SE of relative expression; n = 10). Results represent one of three similar experiments;*P < 0.02 and **P < 0.000005. (Scale bar, 50 μm.) |
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S2003 |
Maraviroc (UK-427857)Maraviroc (UK-427857)是一种CCR5拮抗剂,作用于MIP-1α,MIP-1β和RANTES,无细胞试验中IC50分别为3.3 nM,7.2 nM和5.2 nM。Maraviroc可应用于治疗HIV感染。 |
![]() ![]() CCR5 antagonists block FBS-induced breast cancer cell invasion. 3D reconstruction of FBS-induced invasion into collagen gels by Hs578T (A) or SUM-159 (C) breast cancer cells in presence of CCR5 antagonists (100 nmol/L). The corresponding quantifications (mean ±SEM, n = 3) and analysis (Bonferronit test) are displayed in B and D. |
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S2679 |
Flavopiridol (L86-8275) HClFlavopiridol HCl (L86-8275, NSC 649890, Alvocidib, HMR-1275, DSP-2033)与ATP竞争性抑制CDKs,作用于CDK1,CDK2,CDK4和CDK6,无细胞试验中IC50为~40 nM。作用于CDK1/2/4/6比作用于CDK7选择性高7.5倍。Flavopiridol最初被发现可抑制EGFR和PKA。Flavopiridol HCl 可诱导自噬和内质网应激反应。Flavopiridol HCl 可阻止HIV-1的复制。Phase 1/2。 |
![]() ![]() Comparative efficacy of anticancer therapies (Flavopiridol, vincristine, daunorubicin, et al.) in NMC vs non-NMC cell lines. Mean IC50 (± s.e.m.) of the indicated agents in three NMC (PER-403, PER-624, and PER-704) and two non-NMC cell lines (PER-535 and SAOS2), ***P<0.001, unpaired t-test, corrected for multiple testing. |
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E0005New |
Enfuvirtide AcetateEnfuvirtide Acetate (T20 Acetate, DP178 Acetate) 是一种 HIV 融合 抑制剂,对 MT-2 细胞中的 HIV-1IIIB感染 和 M7 细胞中的 HIV-1Bal 感染的 ic50 分别为 13.63 nM 和 30.21 nM。 |
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S1209 |
Fluorouracil (5-Fluorouracil, 5-FU)Fluorouracil (5-Fluorouracil, 5-FU, NSC 19893) 是DNA/RNA合成抑制剂,在肿瘤细胞中通过抑制胸苷酸合成酶(TS)而干扰核苷酸合成。Fluorouracil 可诱导细胞凋亡并可用于治疗HIV。 |
![]() ![]() DNA-PKcs suppression mediated ROS production and GSH content in HepG2 cells exposed to CDDP and 5-Fu. a DNA-PKcs inhibition promoted ROS production in HepG2 cells treated with indicated concentrations of CDDP and 5-Fu. DCFH-DA fluorescent analysis was performed to assess the ROS level. Data presented were mean ?SD of three independent experiments.
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S1117 |
Triciribine (NSC 154020)Triciribine (NSC 154020, VD-0002, vqd-002, API-2, TCN) 是一种DNA synthesis抑制剂,也抑制PC3细胞系中的Akt和CEM-SS,H9,H9IIIB,U1细胞中的HIV-1,IC50分别为130 nM和20 nM;对PI3K/PDK1没有抑制作用;作用于缺乏腺苷激酶的细胞,活性降低5000倍。Phase 1/2。 |
![]() ![]() Effect of triciribine on the migration of (A) FaDu and (B) Hep2 cells. The cells were treated with 5 µM triciribine for different periods of time. *P<0.05 vs. control. Hpf, high-power field. |
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S3013 |
Plerixafor (AMD3100) 8HClPlerixafor (AMD3100, JM 3100) 8HCl 是Plerixafor的盐酸盐,是CXCR4趋化因子受体拮抗剂,作用于CXCR4和CXCL12介导调节的趋化性,IC50分别为44 nM和5.7 nM。Plerixafor 可应用为抗HIV的药物。 |
![]() ![]() BLI of NSG mice engrafted with BV173, treated with no therapy (control), plerixafor: 1 mg/kg IP daily, ESKM 100 ug twice weekly, and a combination of ESKM and plerixafor. (A) Logarithmic plot of BLI of leukemia growth measured weekly. Error bars are 5-95% confidence intervals. There was a small but not significant difference between ESKM and combination treated group. (B) End of therapy (day 34) BLI.
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S1189 |
Aprepitant (MK-0869)Aprepitant (MK-0869, L-754030)是一种有效的选择性 neurokinin-1 receptor 拮抗剂,IC50为0.1 nM。Aprepitant 可降低炎症因子的表达水平,包括 G-CSF、IL-6、IL-8 和 TNFα。Aprepitant 可抑制人巨噬细胞 HIV 的感染。 |
![]() ![]() HepT1, HepG2, and HuH6 cells were treated with increasing doses of aprepitant or SP [100 nM] and Western blot analysis was performed for the apoptotic markers PARP, Caspase-3, and BID. |
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S7015 |
Birinapant (TL32711)Birinapant (TL32711)是一种SMAC模拟拮抗剂,对cIAP1最有效,无细胞试验中Kd为<1 nM,对XIAP作用较弱。Birinapant可帮助诱导HIV-1感染的细胞凋亡。Phase 2。 |
![]() ![]() Western blot analysis of XIAP and cIAP1 expression and PARP cleavage in H460, A549 and 34LU cells pre-treated with vorinostat or entinostat for 6h followed by the SMAC mimetic birinapant for 24h. |
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S1400 |
Tenofovir (GS 1278) Disoproxil FumarateTenofovir Disoproxil Fumarate (GS-1278, Tenofovir DF)属于一类抗逆转录病毒药物,其通过与天然底物脱氧腺苷5’-三磷酸盐竞争以及整合到DNA后终止DNA链抑制HIV reverse transcriptase活性。 |
![]() ![]() Human PBMCs containing indicated concentrations of Tenofovir disoproxil fumarate were inoculated with 5 ng mock-exposed or semen-exposed R5-HIV-luciferase, or 50 ng R5-HIV-luciferase as infectivity matched control. Infection rates were determined 3 days post inoculation.
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S1704 |
Emtricitabine (BW 1592)Emtricitabine (BW1592, FTC)是一种新型的核苷剂,对人类免疫缺陷病毒HIV和HBV具有抑制活性。是逆转录酶抑制剂,在细胞中的半衰期为39 h。 |
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S8030 |
Plerixafor (AMD3100)Plerixafor (AMD3100, JM 3100, SID791)是一种趋化因子受体拮抗剂,作用于CXCR4和CXCL12介导的趋化性,无细胞试验中IC50分别为44 nM和5.7 nM。Plerixafor 可抑制human immunodeficiency virus (HIV)复制。 |
![]() ![]() BLI of NSG mice engrafted with BV173, treated with no therapy (control), plerixafor: 1 mg/kg IP daily, ESKM 100 ug twice weekly, and a combination of ESKM and plerixafor. (A) Logarithmic plot of BLI of leukemia growth measured weekly. Error bars are 5-95% confidence intervals. There was a small but not significant difference between ESKM and combination treated group. (B) End of therapy (day 34) BLI.
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S1896 |
Hydroxyurea (NSC-32065)Hydroxyurea (NSC-32065, NCI-C04831, Hydroxycarbamide)是一种抗肿瘤药,通过抑制核苷二磷酸还原酶 ribonucleoside diphosphate reductase 而抑制DNA合成。 Hydroxyurea 可激活凋亡和自噬,并可用于治疗HIV感染。 |
![]() ![]() Lethally irradiated C57BL/6 recipient mice were injected with a 1:1 mixture of GFP+JAK2(V671F) and wild-type bone marrow cells. Five weeks later, mice were treated with vehicle (C), hydroxyurea (H; 30 mg/kg twice daily IP), ruxolitinib (R; 30 mg/kg twice daily oral gavage), BMN673 (B; 0.33 mg/kg IV), H+R, H+B, R+B, and H+R+B for 3 weeks. Percentage of GFP+JAK2(V617F) was measured in (panel B) bone marrow cells, (panel C) splenocytes, and (panel D) peripheral blood leukocytes; (panel E) number of GFP+JAK2(V617F) Lin−Sca1+c-Kit+ (LSK) cells per 106 bone marrow cells was calculated, too. *P < .05, **P < .05, and ***P < .05 when compared with control, single treatment, and double treatment, respectively, from 6 to 7 mice using the Student t test.
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S1848 |
CurcuminCurcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow)是流行的印度香料姜黄的主要姜黄色素,属于姜科(Zingiberaceae)。它是p300 histone acetylatransferase(IC50~25 μM)和Histone deacetylase (HDAC)的抑制剂,能够激活Nrf2 pathway并抑制NF-κB的激活。Curcumin 可诱导线粒体自噬、细胞自噬、凋亡和细胞周期阻滞,并具有抗肿瘤的活性。Curcumin 可通过减少铁死亡介导的细胞死亡来减少横纹肌溶解相关的肾衰竭。Curcumin 对各种人类病原体(如流感病毒,丙型肝炎病毒,HIV等)具有抗感染特性。 |
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S1351 |
Ivermectin (MK-933)Ivermectin (MK-933, IVM) 是一种chloride channel激活剂,用作广谱抗寄生虫药。Ivermectin (MK-933, IVM) 是 P2X4 和 α7 nicotinic acetylcholine receptors (nAChRs) 的特异性正变构效应物。Ivermectin 对 HIV-1 和登革热dengue virus均具有有效的抗病毒活性。Ivermectin 可通过AKT/mTOR信号通路来诱导自噬,并诱导线粒体自噬。 |
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S5144 |
NeferineNeferine ((R)-1,2-Dimethoxyaporphine) 是 Nelumbo nucifera 的天然成分,具有抗肿瘤功效。Neferine 可诱导肾癌细胞凋亡。Neferine 通过激活肌肉细胞中的 Akt/mTOR 通路和 Nrf2 来防止自噬。Neferine 可抑制 NF-κB 的激活。Neferine具有多种治疗作用,例如抗糖尿病,抗衰老,抗微生物,抗血栓形成,抗心律不齐,抗炎甚至抗HIV。 |
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S7311 |
Q-VD-OphQ-VD-OPh (Quinoline-Val-Asp-Difluorophenoxymethylketone)是一种有效的pan-caspase抑制剂,作用于caspases 1, 3, 8和9,IC50范围在25到400 nM之间,有效抑制与细胞凋亡相关的末端caspase激活,底物裂解,及DNA梯状条带形成。Q-VD-OPh 可抑制HIV感染。 |
![]() ![]() UA and Q-VD-Oph attenuated TNF-α-induced unclear translocation of NF-κB (C) and P-STAT3(S727) (D) in BEAS-2B cells.
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S0958 |
Zingibroside R1Zingibroside R1 从 Panax zingiberensis Wu et Feng(五加科)的根茎中分离得到,具有一定的抗 HIV-1 活性。Zingibroside R1 显示对 EAT 细胞摄取 2-脱氧-D-葡萄糖 (2-DG) 的抑制作用,IC50 为 91.3 µM,对 MT-4 细胞的生长具有抑制作用,CC50 为 46.2 µM。 |
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S5959 |
Tenofovir DisoproxilTenofovir Disoproxil (Bis(POC)-PMPA, GS 4331) 是Tenofovir的前药,Tenofovir在细胞内会被代谢成其活性的同化蛋白Tenofovir diphosphate,是 HIV-1 reverse transcriptase 的竞争性抑制剂,并终止其生长DNA链。 |
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S0076 |
ABX464ABX464 (SPL-464)是一种新型的抗HIV的分子,可抑制 HIV-1 的复制,对来自5个不同供体的受刺激的外周血单个核细胞(PBMCs)中的IC50范围为0.1 μM至0.5 μM。 |
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S4861 |
OxindoleOxindole (2-indolone, 2-Oxindole, Indolin-2-one)是芳香族杂环有机化合物,当剂量过量时,可引起镇静、肌无力、低血压和昏迷。 |
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S3500 |
Pentosan Polysulfate SodiumPentosan Polysulfate Sodium (PPS, Elmiron) 是一种口服生物可利用的半合成药物,具有抗炎和促软骨形成的特性。Pentosan Polysulfate Sodium 也具有抗 HIV-1 的活性。 |
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S6676 |
EbselenEbselen (DR 3305, SPI-1005, PZ-51, CCG-39161)是HIV-1复制的小分子衣壳抑制剂,在TR-FRET分析中的IC50为46.1 nM。 |
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S6848 |
3'-Fluoro-3'-deoxythymidine (Alovudine)3'-Fluoro-3'-deoxythymidine (Alovudine, CL 184824, FddThd, FLT, MIV-310)是一种有效的 polymerase γ 和 reverse transcriptase 抑制剂,可用于治疗HIV感染。3'-Fluoro-3'-deoxythymidine (Alovudine) 也是一种 DNA synthesis 的标记,可以用作为胰腺癌化疗的早期反应生物标记物。 |
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S5979 |
2',3'-Dideoxyadenosine2',3'-Dideoxyadenosine (ddA, ddAdo) 是抗人类免疫缺陷病毒药物,可抑制 human immunodeficiency virus (HIV) 和 human hepatitis B virus (HBV) 的复制。 |
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S9064 |
TrilobatinTrilobatin (P-Phlorizin), a natural flavonoid lipid molecule, is an HIV-1 entry inhibitor targeting the HIV-1 Gp41 envelope and exihibits anti-oxidant and anti-inflammatory effect. |
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S4446 |
DimercaprolDimercaprol (Bal, 2,3-Dimercapto-1-propanol, Dithioglycerol) 是一种丙烯醛清除剂,在体外可抑制 HIV-1 tat 的活性、病毒的产生和感染性。 |
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S8512 |
Cenicriviroc (TAK-652)Cenicriviroc (CVC, TAK-652, TBR-652) 是一种有效的、口服活性的 CC chemokine receptor 2 (CCR2) 和 CCR5 的双效抑制剂。Cenicriviroc 还可抑制 HIV-1 和 HIV-2 并具有有效的抗炎和抗感染活性。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S1009 |
Dactolisib (BEZ235)Dactolisib (BEZ235, NVP-BEZ235) 是一种双重ATP竞争性 PI3K 和 mTOR 抑制剂,在无细胞试验中,抑制 p110α/γ/δ/β 和 mTOR(p70S6K) 的 IC50 分别为 4 nM /5 nM /7 nM /75 nM /6 nM。 在 3T3TopBP1-ER 细胞中抑制 ATR,IC50 为 21 nM,而对 Akt 和 PDK1 的抑制作用很弱。Dactolisib可诱导自噬并抑制HIV-1的复制。Phase 2。 |
![]() ![]() Three-dimensional responses of MCF7/IGF-1R cells to TAM (1 μM), E2 and IGF-1. Compared to parental MCF7 cells (a), MCF7/IGF-1R cells (b) in three-dimensional (3D) culture formed bigger acini in response to IGF-1 stimulation and displayed significant TAM resistance when treated with TAM (1 μM) + E2 + IGF-1, which was removable by kinase inhibitors BMS-536924, U0126 and BEZ235 (c). Cells (10,000/well) were seeded in 96-well plates. Acini were formed on 100% Matrigel and cultured for 14 days in starving medium containing 2% Matrigel and 5% charcoal/dextran-stripped fetal bovine serum with the treatments as indicated. Concentrations used: TAM (1 μM), E2 (1 nM) and IGF-1 (100 ng/mL). Confocal image original magnification, × 20. Red, rhodamine phalloidin (actin). Blue, Hoechst blue stain. Results are representative of two individual experiments. |
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S1208 |
Doxorubicin (Adriamycin) HClDoxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl是一种抗生素类试剂,可抑制DNA topoisomerase II,并在肿瘤细胞中诱导DNA损伤、线粒体自噬和凋亡。Doxorubicin 可降低 AMPK的基础磷酸化。Doxorubicin 可应用于HIV感染病人的联合治疗,但是在免疫治疗中有将HBV重活化的风险。 |
![]() ![]() Cell viabilities with increasing concentrations of cisplatin (CP) and doxorubicin (DOXO) under normoxic and hypoxic condition for 48 hours were determined by MTT assay. IC50 values are presented as the means ?SDs (n=4) and * denotes p<0.05. |
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S1230 |
Flavopiridol (L86-8275)Flavopiridol (L86-8275, Alvocidib, NSC 649890, HMR-1275) 与ATP竞争性抑制CDKs,包括CDK1、CDK2、CDK4、CDK6和CDK9的IC50范围为20-100 nM。作用于CDK1、2、4、6、9比作用于CDK7更具有选择性。Flavopiridol最初被发现能抑制EGFR和PKA。Flavopiridol可诱导自噬和内质网应激反应。Flavopiridol可阻滞HIV-1的复制。Phase 1/2。 |
![]() ![]() (C) In vivo treatment of Tg:Pomc-Pttg;Pomc-eGFP embryos with small-molecule CDK inhibitors (50 μM) or 0.2% DMSO as control from 18 to 40 hpf. One hundred to one hundred fifty embryos were treated with each compound. Representative images of live embryos are shown with gross morphology (Right) and pituitary Pomc-GFP-positive cells at higher magnification (Left) at 40 hpf. Embryos exposed to flavopiridol developed early developmental defect before pituitary POMC cell ontogeny occurs. (D) Relative expression of pituitary Pomc-eGFP fluorescence analyzed using Volocity 5.2 software (Improvision; mean ±SE of relative expression, n = 7). (E) R-roscovitine specifically suppresses expansion of pituitary POMC cells overexpressing zPttg from 18 to 48 hpf. Double transgenic Tg:Pomc-Pttg;Prl-RFP embryos were generated by breeding Tg:Pomc-Pttg fish with a previously generated PRL-RFP transgenic line, in which RFP was targeted to pituitary lactotrophs by a zebrafish Prolactin promoter (34). Representative fluorescent microscopy of pituitary POMC-eGFP (a and b) and PRL-RFP (c and d) expression in live Tg:Pomc-Pttg; Pomc-eGFP and Tg:Pomc-Pttg;Prl-RFP embryos treated with 0.2% DMSO (a and c) or 50 μM R-roscovitine (b and d). (F) Relative expression of pituitary POMC-eGFP or PRL-RFP fluorescence were analyzed (mean ±SE of relative expression; n = 10). Results represent one of three similar experiments;*P < 0.02 and **P < 0.000005. (Scale bar, 50 μm.) |
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S2003 |
Maraviroc (UK-427857)Maraviroc (UK-427857)是一种CCR5拮抗剂,作用于MIP-1α,MIP-1β和RANTES,无细胞试验中IC50分别为3.3 nM,7.2 nM和5.2 nM。Maraviroc可应用于治疗HIV感染。 |
![]() ![]() CCR5 antagonists block FBS-induced breast cancer cell invasion. 3D reconstruction of FBS-induced invasion into collagen gels by Hs578T (A) or SUM-159 (C) breast cancer cells in presence of CCR5 antagonists (100 nmol/L). The corresponding quantifications (mean ±SEM, n = 3) and analysis (Bonferronit test) are displayed in B and D. |
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S2679 |
Flavopiridol (L86-8275) HClFlavopiridol HCl (L86-8275, NSC 649890, Alvocidib, HMR-1275, DSP-2033)与ATP竞争性抑制CDKs,作用于CDK1,CDK2,CDK4和CDK6,无细胞试验中IC50为~40 nM。作用于CDK1/2/4/6比作用于CDK7选择性高7.5倍。Flavopiridol最初被发现可抑制EGFR和PKA。Flavopiridol HCl 可诱导自噬和内质网应激反应。Flavopiridol HCl 可阻止HIV-1的复制。Phase 1/2。 |
![]() ![]() Comparative efficacy of anticancer therapies (Flavopiridol, vincristine, daunorubicin, et al.) in NMC vs non-NMC cell lines. Mean IC50 (± s.e.m.) of the indicated agents in three NMC (PER-403, PER-624, and PER-704) and two non-NMC cell lines (PER-535 and SAOS2), ***P<0.001, unpaired t-test, corrected for multiple testing. |
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E0005New |
Enfuvirtide AcetateEnfuvirtide Acetate (T20 Acetate, DP178 Acetate) 是一种 HIV 融合 抑制剂,对 MT-2 细胞中的 HIV-1IIIB感染 和 M7 细胞中的 HIV-1Bal 感染的 ic50 分别为 13.63 nM 和 30.21 nM。 |
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S1209 |
Fluorouracil (5-Fluorouracil, 5-FU)Fluorouracil (5-Fluorouracil, 5-FU, NSC 19893) 是DNA/RNA合成抑制剂,在肿瘤细胞中通过抑制胸苷酸合成酶(TS)而干扰核苷酸合成。Fluorouracil 可诱导细胞凋亡并可用于治疗HIV。 |
![]() ![]() DNA-PKcs suppression mediated ROS production and GSH content in HepG2 cells exposed to CDDP and 5-Fu. a DNA-PKcs inhibition promoted ROS production in HepG2 cells treated with indicated concentrations of CDDP and 5-Fu. DCFH-DA fluorescent analysis was performed to assess the ROS level. Data presented were mean ?SD of three independent experiments.
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S1117 |
Triciribine (NSC 154020)Triciribine (NSC 154020, VD-0002, vqd-002, API-2, TCN) 是一种DNA synthesis抑制剂,也抑制PC3细胞系中的Akt和CEM-SS,H9,H9IIIB,U1细胞中的HIV-1,IC50分别为130 nM和20 nM;对PI3K/PDK1没有抑制作用;作用于缺乏腺苷激酶的细胞,活性降低5000倍。Phase 1/2。 |
![]() ![]() Effect of triciribine on the migration of (A) FaDu and (B) Hep2 cells. The cells were treated with 5 µM triciribine for different periods of time. *P<0.05 vs. control. Hpf, high-power field. |
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S3013 |
Plerixafor (AMD3100) 8HClPlerixafor (AMD3100, JM 3100) 8HCl 是Plerixafor的盐酸盐,是CXCR4趋化因子受体拮抗剂,作用于CXCR4和CXCL12介导调节的趋化性,IC50分别为44 nM和5.7 nM。Plerixafor 可应用为抗HIV的药物。 |
![]() ![]() BLI of NSG mice engrafted with BV173, treated with no therapy (control), plerixafor: 1 mg/kg IP daily, ESKM 100 ug twice weekly, and a combination of ESKM and plerixafor. (A) Logarithmic plot of BLI of leukemia growth measured weekly. Error bars are 5-95% confidence intervals. There was a small but not significant difference between ESKM and combination treated group. (B) End of therapy (day 34) BLI.
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S1189 |
Aprepitant (MK-0869)Aprepitant (MK-0869, L-754030)是一种有效的选择性 neurokinin-1 receptor 拮抗剂,IC50为0.1 nM。Aprepitant 可降低炎症因子的表达水平,包括 G-CSF、IL-6、IL-8 和 TNFα。Aprepitant 可抑制人巨噬细胞 HIV 的感染。 |
![]() ![]() HepT1, HepG2, and HuH6 cells were treated with increasing doses of aprepitant or SP [100 nM] and Western blot analysis was performed for the apoptotic markers PARP, Caspase-3, and BID. |
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S7015 |
Birinapant (TL32711)Birinapant (TL32711)是一种SMAC模拟拮抗剂,对cIAP1最有效,无细胞试验中Kd为<1 nM,对XIAP作用较弱。Birinapant可帮助诱导HIV-1感染的细胞凋亡。Phase 2。 |
![]() ![]() Western blot analysis of XIAP and cIAP1 expression and PARP cleavage in H460, A549 and 34LU cells pre-treated with vorinostat or entinostat for 6h followed by the SMAC mimetic birinapant for 24h. |
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S1400 |
Tenofovir (GS 1278) Disoproxil FumarateTenofovir Disoproxil Fumarate (GS-1278, Tenofovir DF)属于一类抗逆转录病毒药物,其通过与天然底物脱氧腺苷5’-三磷酸盐竞争以及整合到DNA后终止DNA链抑制HIV reverse transcriptase活性。 |
![]() ![]() Human PBMCs containing indicated concentrations of Tenofovir disoproxil fumarate were inoculated with 5 ng mock-exposed or semen-exposed R5-HIV-luciferase, or 50 ng R5-HIV-luciferase as infectivity matched control. Infection rates were determined 3 days post inoculation.
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S1704 |
Emtricitabine (BW 1592)Emtricitabine (BW1592, FTC)是一种新型的核苷剂,对人类免疫缺陷病毒HIV和HBV具有抑制活性。是逆转录酶抑制剂,在细胞中的半衰期为39 h。 |
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S8030 |
Plerixafor (AMD3100)Plerixafor (AMD3100, JM 3100, SID791)是一种趋化因子受体拮抗剂,作用于CXCR4和CXCL12介导的趋化性,无细胞试验中IC50分别为44 nM和5.7 nM。Plerixafor 可抑制human immunodeficiency virus (HIV)复制。 |
![]() ![]() BLI of NSG mice engrafted with BV173, treated with no therapy (control), plerixafor: 1 mg/kg IP daily, ESKM 100 ug twice weekly, and a combination of ESKM and plerixafor. (A) Logarithmic plot of BLI of leukemia growth measured weekly. Error bars are 5-95% confidence intervals. There was a small but not significant difference between ESKM and combination treated group. (B) End of therapy (day 34) BLI.
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S1896 |
Hydroxyurea (NSC-32065)Hydroxyurea (NSC-32065, NCI-C04831, Hydroxycarbamide)是一种抗肿瘤药,通过抑制核苷二磷酸还原酶 ribonucleoside diphosphate reductase 而抑制DNA合成。 Hydroxyurea 可激活凋亡和自噬,并可用于治疗HIV感染。 |
![]() ![]() Lethally irradiated C57BL/6 recipient mice were injected with a 1:1 mixture of GFP+JAK2(V671F) and wild-type bone marrow cells. Five weeks later, mice were treated with vehicle (C), hydroxyurea (H; 30 mg/kg twice daily IP), ruxolitinib (R; 30 mg/kg twice daily oral gavage), BMN673 (B; 0.33 mg/kg IV), H+R, H+B, R+B, and H+R+B for 3 weeks. Percentage of GFP+JAK2(V617F) was measured in (panel B) bone marrow cells, (panel C) splenocytes, and (panel D) peripheral blood leukocytes; (panel E) number of GFP+JAK2(V617F) Lin−Sca1+c-Kit+ (LSK) cells per 106 bone marrow cells was calculated, too. *P < .05, **P < .05, and ***P < .05 when compared with control, single treatment, and double treatment, respectively, from 6 to 7 mice using the Student t test.
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S1848 |
CurcuminCurcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow)是流行的印度香料姜黄的主要姜黄色素,属于姜科(Zingiberaceae)。它是p300 histone acetylatransferase(IC50~25 μM)和Histone deacetylase (HDAC)的抑制剂,能够激活Nrf2 pathway并抑制NF-κB的激活。Curcumin 可诱导线粒体自噬、细胞自噬、凋亡和细胞周期阻滞,并具有抗肿瘤的活性。Curcumin 可通过减少铁死亡介导的细胞死亡来减少横纹肌溶解相关的肾衰竭。Curcumin 对各种人类病原体(如流感病毒,丙型肝炎病毒,HIV等)具有抗感染特性。 |
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S1351 |
Ivermectin (MK-933)Ivermectin (MK-933, IVM) 是一种chloride channel激活剂,用作广谱抗寄生虫药。Ivermectin (MK-933, IVM) 是 P2X4 和 α7 nicotinic acetylcholine receptors (nAChRs) 的特异性正变构效应物。Ivermectin 对 HIV-1 和登革热dengue virus均具有有效的抗病毒活性。Ivermectin 可通过AKT/mTOR信号通路来诱导自噬,并诱导线粒体自噬。 |
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S5144 |
NeferineNeferine ((R)-1,2-Dimethoxyaporphine) 是 Nelumbo nucifera 的天然成分,具有抗肿瘤功效。Neferine 可诱导肾癌细胞凋亡。Neferine 通过激活肌肉细胞中的 Akt/mTOR 通路和 Nrf2 来防止自噬。Neferine 可抑制 NF-κB 的激活。Neferine具有多种治疗作用,例如抗糖尿病,抗衰老,抗微生物,抗血栓形成,抗心律不齐,抗炎甚至抗HIV。 |
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S7311 |
Q-VD-OphQ-VD-OPh (Quinoline-Val-Asp-Difluorophenoxymethylketone)是一种有效的pan-caspase抑制剂,作用于caspases 1, 3, 8和9,IC50范围在25到400 nM之间,有效抑制与细胞凋亡相关的末端caspase激活,底物裂解,及DNA梯状条带形成。Q-VD-OPh 可抑制HIV感染。 |
![]() ![]() UA and Q-VD-Oph attenuated TNF-α-induced unclear translocation of NF-κB (C) and P-STAT3(S727) (D) in BEAS-2B cells.
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S0958 |
Zingibroside R1Zingibroside R1 从 Panax zingiberensis Wu et Feng(五加科)的根茎中分离得到,具有一定的抗 HIV-1 活性。Zingibroside R1 显示对 EAT 细胞摄取 2-脱氧-D-葡萄糖 (2-DG) 的抑制作用,IC50 为 91.3 µM,对 MT-4 细胞的生长具有抑制作用,CC50 为 46.2 µM。 |
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S5959 |
Tenofovir DisoproxilTenofovir Disoproxil (Bis(POC)-PMPA, GS 4331) 是Tenofovir的前药,Tenofovir在细胞内会被代谢成其活性的同化蛋白Tenofovir diphosphate,是 HIV-1 reverse transcriptase 的竞争性抑制剂,并终止其生长DNA链。 |
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S0076 |
ABX464ABX464 (SPL-464)是一种新型的抗HIV的分子,可抑制 HIV-1 的复制,对来自5个不同供体的受刺激的外周血单个核细胞(PBMCs)中的IC50范围为0.1 μM至0.5 μM。 |
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S4861 |
OxindoleOxindole (2-indolone, 2-Oxindole, Indolin-2-one)是芳香族杂环有机化合物,当剂量过量时,可引起镇静、肌无力、低血压和昏迷。 |
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S3500 |
Pentosan Polysulfate SodiumPentosan Polysulfate Sodium (PPS, Elmiron) 是一种口服生物可利用的半合成药物,具有抗炎和促软骨形成的特性。Pentosan Polysulfate Sodium 也具有抗 HIV-1 的活性。 |
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S6676 |
EbselenEbselen (DR 3305, SPI-1005, PZ-51, CCG-39161)是HIV-1复制的小分子衣壳抑制剂,在TR-FRET分析中的IC50为46.1 nM。 |
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S6848 |
3'-Fluoro-3'-deoxythymidine (Alovudine)3'-Fluoro-3'-deoxythymidine (Alovudine, CL 184824, FddThd, FLT, MIV-310)是一种有效的 polymerase γ 和 reverse transcriptase 抑制剂,可用于治疗HIV感染。3'-Fluoro-3'-deoxythymidine (Alovudine) 也是一种 DNA synthesis 的标记,可以用作为胰腺癌化疗的早期反应生物标记物。 |
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S5979 |
2',3'-Dideoxyadenosine2',3'-Dideoxyadenosine (ddA, ddAdo) 是抗人类免疫缺陷病毒药物,可抑制 human immunodeficiency virus (HIV) 和 human hepatitis B virus (HBV) 的复制。 |
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S9064 |
TrilobatinTrilobatin (P-Phlorizin), a natural flavonoid lipid molecule, is an HIV-1 entry inhibitor targeting the HIV-1 Gp41 envelope and exihibits anti-oxidant and anti-inflammatory effect. |
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S4446 |
DimercaprolDimercaprol (Bal, 2,3-Dimercapto-1-propanol, Dithioglycerol) 是一种丙烯醛清除剂,在体外可抑制 HIV-1 tat 的活性、病毒的产生和感染性。 |
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S8512 |
Cenicriviroc (TAK-652)Cenicriviroc (CVC, TAK-652, TBR-652) 是一种有效的、口服活性的 CC chemokine receptor 2 (CCR2) 和 CCR5 的双效抑制剂。Cenicriviroc 还可抑制 HIV-1 和 HIV-2 并具有有效的抗炎和抗感染活性。 |