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33

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T13783	MT-4	Others	Others
	MT-4 可阻断肿瘤细胞和肿瘤niche 表面的TG2/FN 复合体。 MT-4抑制卵巢癌(OC)细胞与腹膜的黏附。
T7519	RS-127445 hydrochloride 4-(4-氟-1-萘基)-6-(1-甲基乙基)-2-嘧啶胺盐酸盐,RS 127445,MT 500	5-HT Receptor	GPCR/G Protein; Neuroscience
	RS-127445 hydrochloride (MT 500) 是一种可口服的，高亲和力选择性5-HT2B 受体拮抗剂，pKi 为 9.5，比作用于其他受体和离子通道的选择性高 1000 倍。
T9104	TJ191	Apoptosis	Apoptosis
	TJ191 是一种选择性抗癌试剂，靶向低 TβRIII 表达的恶性T 细胞白血病/淋巴瘤细胞，可研究癌症。
T11465	Lenacapavir GS-6207	Others; HIV Protease	Microbiology/Virology; Others; Proteases/Proteasome
	Lenacapavir (GS-6207) 是一种有效的靶向衣壳的 HIV 复制抑制剂。 Lenacapavir 在 MT-4 细胞中显示出抗 HIV 活性，EC50 为 100 pM。
T61395	Mt KARI-IN-4
	Mt KARI-IN-4 (compound 5c) is a highly effective inhibitor of Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI), demonstrating a Ki value of 5.48 μM. Additionally, Mt KARI-IN-4 displays inhibitory properties against Mtb H37Rv, with a minimum inhibitory concentration (MIC) of 0.78 μM. Importantly, this compound exhibits low levels of cytotoxicity, as evident from its half-maximal inhibitory concentration (IC 50 ) value of over 72 μg/mL against human embryonic kidney cells (HEK) [1...
TQ0174	Mavorixafor AMD-070	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	Mavorixafor (AMD-070) 是一种有效的特异性 CXCR4 拮抗剂，对 CXCR4 125I-SDF 结合的 IC50 值为 13 nM。 Mavorixafor 在 MT-4 细胞 (IC50 = 1 nM) 和 PBMC (IC50 = 9 nM) 中抑制 T-tropic HIV-1 (NL4.3 株) 的复制。
T67833	HIV-1 inhibitor-54	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	HIV-1 inhibitor-54 是一种有效的 HIV-1 抑制剂，在 MT-4 细胞中对 WT HIV-1 (菌株 IIIB) x 显示出抗 HIV 活性（EC50 ： 32 nM）。HIV-1 inhibitor-54 可用于研究病毒感染。
T10141	4'-Ethynyl-2'-deoxyadenosine	Others	Others
	4'-Ethynyl-2'-deoxyadenosine (4'-E-dA) is a nucleoside reverse transcriptase (RT) inhibitor. It is potent against drug-resistant HIV variants (EC50: 98 nM in MT-4 cells for anti-HIV-1 activity).
T7208	AMD 3465 hexahydrobromide GENZ-644494 (hexahydrobromide)	HIV Protease; CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	AMD 3465 hexahydrobromide (GENZ-644494 (hexahydrobromide)) 是一种 CXCR4受体拮抗剂，具有潜在的抗癌和抗 HIV 活性。
T29393	3'-Deoxy-4-thiothymidine Thymidine, 3'-deoxy-4-thio-,Ddthds
	3'-Deoxy-4-thiothymidine can moderately active in protecting HIV-induced cytopathogenicity of MT-2 and CEM cells.
T15045	D77	Others	Others
	D77 is anti-HIV-1 inhibitor. D77 inhibits HIV-1(IIIB) replication by EC50 value of 23.8 μg/ml in MT-4 cell (5.03 μg/ml for C8166 cells).
T10296	Mavorixafor trihydrochloride AMD-070 trihydrochloride	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	Mavorixafor trihydrochloride is a selective and orally available CXCR4 antagonist (IC50: 13 nM against CXCR4 125I-SDF binding) and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs (IC50s: 1 and 9 nM).
T15776	Loviride R 89439	Others	Others
	Loviride is a non-nucleoside reverse transcriptase inhibitor (IC50: 0.3 µM). Loviride inhibits HIV-1, HIV-2 and SIV replication in MT-4 cells. It is used for reverse transcriptase from HIV-1.
T62353	HIV-1 inhibitor-33
	HIV-1 inhibitor-33 (compound 5n) 是一种有效的、选择性的 HIV-1 抑制剂，作用于 HIV-1 (EC50: 8.6 nM)、MT-4 细胞 (CC50: 18 μM)。HIV-1 inhibitor-33 能够用于研究艾滋病。
T63499	HIV-1 inhibitor-28
	HIV-1 inhibitor-28 是高效的、选择性的HIV-1抑制剂，对野生型 HIV-1 的EC50=58 nM，对野生型 HIV-1 逆转录的IC50=3.37 μM，对 MT-4 细胞有相对较低的毒性，其CC50= 38.6 μM。HIV-1 inhibitor-28 能够用于研究艾滋病。
T71009	Dolutegravir SR Isomer
	Dolutegravir SR Isomer is an isomeric derivative of Dolutegravir -- a second generation HIV-1 integrase strand transfer inhibitor. Dolutegravir has been shown to potently inhibit HIV replication in cells such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4 cells infected with a self-inactivating PHIV lentiviral vector.
T63113	HIV-1 inhibitor-21
	HIV-1 inhibitor-21 (compound 9b) 是一种 HIV-1 非核苷逆转录酶 (RT) 的有效抑制剂，作用于 HIV-1 RT (IC50: 0.55 μM)。HIV-1 inhibitor-21 能够抑制野生型 HIV-1 (EC50: 12.7 nM) 和突变病毒株 K103N (EC50: 10.4 nM) 的逆转录，且细胞毒性相对较低(对 MT-4 的 CC50: 10.2 μM)。
T62782	HIV-1 inhibitor-34
	HIV-1 inhibitor-34 (compound 5q) 是一种有效的、选择性的 HIV-1 抑制剂，作用于 HIV-1 (EC50: 6.4 nM)、MT-4 细胞 (CC50: 16 μM)。HIV-1 inhibitor-34 能够用于研究艾滋病。
T63813	HIV-1 inhibitor-39
	HIV-1 inhibitor-39 是 HIV-1 的有效抑制剂 (EC50>112.88 μM)。 HIV-1 inhibitor-39 具有抗 RT (HIV-1 逆转录酶) 作用 (IC50: 15.75 μM)。HIV-1 inhibitor-39 对 MT-4 细胞表现出细胞毒性 (CC50: 112.9 μM)。
T74664	KTX-582
	KTX-582为一有效IRAK4降解剂，DC50对IRAK4及Ikaros分别为4 nM与5 nM。KTX-582能诱导MYD88MTDLBCL细胞凋亡(apoptosis)，在淋巴瘤模型中有效促进体内肿瘤消退。
T70881	Dolutegravir RR Isomer
	Dolutegravir RR Isomer is an isomer of Dolutegravir -- a second generation HIV-1 integrase strand transfer inhibitor. Dolutegravir has been shown to potently inhibit HIV replication in cells such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4 cells infected with a self-inactivating PHIV lentiviral vector.
T36659	Boromycin
	Boromycin is a boron-containing macrolide antibiotic that has been found in Streptomyces. Boromycin inhibits growth of B. subtilis (MIC = 0.05 μg/ml) and induces efflux of potassium ions from B. subtilis without affecting Na+/K+-ATPase activity. It decreases the synthesis of protein, RNA, and DNA in B. subtilis when used at a concentration of 0.05 μg/ml. It inhibits the growth of B. halodurans (MIC = 10 ng/ml) and inhibits the futalosine pathway of menaquinone synthesis in B. halodurans. Boromyc...
T37750	Benanomicin B (formate)
	Benanomicin B is a microbial metabolite that has been found inActinomycetesand has antifungal, fungicidal, and antiviral activities.1,2It is active against a variety of mammalian and plant pathogenic fungi, includingC. albicans,T. mentagrophytes,C. neoformans, andP. oryzae(MICs = 1.56-50 μg/ml).1Benanomicin B inhibits HIV-1 viral infection in MT-4 cells in a concentration-dependent manner.2 1.Takeuchi, T., Hara, T., Naganawa, H., et al.New antifungal antibiotics, benanomicins A and B from an act...
T37749	Benanomicin A
	Benanomicin A is a microbial metabolite that has been found inActinomycetesand has antifungal, fungicidal, and antiviral activities.1,2It is active against a variety of mammalian and plant pathogenic fungi, includingC. albicans,T. mentagrophytes,C. neoformans,P. oryzae, andA. niger(MICs = 3.13-50 μg/ml).1Benanomicin A inhibits HIV-1 viral infection in MT-4 cells in a concentration-dependent manner.2 1.Takeuchi, T., Hara, T., Naganawa, H., et al.New antifungal antibiotics, benanomicins A and B fr...
T63962	HIV-1 inhibitor-29
	HIV-1 inhibitor-29 是 HIV-1 的有效抑制剂，能够作用于 HIV-1 IIIB (EC50: 2.18 μM)。HIV-1 inhibitor-29 对 F227L/V106A 株表现出较高的抗耐药性，其 EC50 值为 0.974 μM。HIV-1 inhibitor-29 对 MT-4 细胞显示出较低的细胞毒性，其 CC50 值为 211 μM。HIV-1 inhibitor-29 能够用于研究艾滋病。
T62430	HIV-1 inhibitor-24
	HIV-1 inhibitor-24 (compound S-12a) 是一种 HIV-1 逆转录 (HIV-1 RT) 的高效抑制剂 (IC50: 9.5 nM)。HIV-1 inhibitor-24 对野生型 HIV-1 表现出较高的抗病毒效果，其 EC50 值为 1.6 nM，且细胞毒性较低 (对 MT-4 细胞的 CC50 值为 9.07 μM)。HIV-1 inhibitor-24 在小鼠中 2 g/kg 剂量下具有良好的耐受性，并具有明显的心血管安全性。
T78925	HIV-1 inhibitor-58
	HIV-1inhibitor-58（Compound 10c）是一款抗逆转录病毒活性的广谱非核苷逆转录酶抑制剂，有效抑制MT-4细胞中的HIV-1 WT株IIIB以及NNRTI耐药菌株，如K103N和E138K（EC50 < 50 nM）。此外，HIV-1inhibitor-58对CYP2C9与CYP2C19也表现出抑制作用（IC50分别为2.06 μM与1.91 μM），适用于HIV感染研究。
T11693L	IT1t dihydrochloride	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	IT1t dihydrochloride 抑制 CXCL12/CXCR4 相互作用，IC50 为 2.1 nM。 IT1t dihydrochloride 是 CXCR4 的拮抗剂。
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...
T83769	TC 14012 hydrochloride H-Arg-Arg-Nal-Cys-Tyr-Cit-Lys-D-Cit-Pro-Tyr-Arg-Cit-Cys-Arg-NH2
	TC 14012是一种化学肽模拟的拮抗剂，针对趋化因子(C-X-C motif)受体4（CXCR4；IC50 = 2.9 nM）和CXCR7激动剂。它能在表达CXCR7的HEK293T细胞中诱导β-arrestin招募（EC50 = 350 nM）。TC 14012可减少HIV在MT-4细胞中的细胞病理效应（EC50 = 0.4 nM），并以CXCR4依赖的方式抑制HIV在体外进入（IC50 = 19.3 nM）。它还能抑制由趋化因子(C-X-C motif)配体12（CXCL12）在MDA-MB-231乳腺癌细胞和人脐静脉内皮细胞（HUVECs）中诱导的迁移，当使用浓度范围从10到1,000 nM时。在通过左前降（LAD）冠状动脉结扎诱导的急性心肌梗死小鼠模型中，TC 14012（10 mg/kg）能减少梗死面积。
T62431	HIV-1 inhibitor-25
	HIV-1 inhibitor-25 (compound R-12a) 是一种 HIV-1 逆转录 (HIV-1 RT) 的高效抑制剂 (IC50: 0.1061 nM)。HIV-1 inhibitor-25 对野生型 HIV-1 表现出较高的抗病毒效果，其 EC50 值为 13.6 nM，且细胞毒性较低 (对 MT-4 细胞的 CC50 值为 33.13 μM)。HIV-1 inhibitor-25 也能够抑制 HIV-1 突变株 (L100I, K103 N, Y181C, Y188L, E138K, F227L+V106A)，EC50=0.1961 ~ 5.8136 μM。HIV-1 inhibitor-25 能够用于研究艾滋病。
T14208	AMD 3465 GENZ-644494	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM). However, it has no effect on CCR5-using (R5) viruses. AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC
T11693	IT1t	Others	Others
	IT1t inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM. is a potent CXCR4 antagonist.

化合物

Cat.No: T13783

Target: Others

RS-127445 hydrochloride

Cat.No: T7519

Synonym: 4-(4-氟-1-萘基)-6-(1-甲基乙基)-2-嘧啶胺盐酸盐,RS 127445,MT 500

Target: 5-HT Receptor

Cat.No: T9104

Target: Apoptosis

Cat.No: T11465

Synonym: GS-6207

Target: Others, HIV Protease

Cat.No: T61395

Cat.No: TQ0174

Synonym: AMD-070

Target: CXCR

HIV-1 inhibitor-54

Cat.No: T67833

Target: HIV Protease

4'-Ethynyl-2'-deoxyadenosine

Cat.No: T10141

Target: Others

AMD 3465 hexahydrobromide

Cat.No: T7208

Synonym: GENZ-644494 (hexahydrobromide)

Target: HIV Protease, CXCR

3'-Deoxy-4-thiothymidine

Cat.No: T29393

Synonym: Thymidine, 3'-deoxy-4-thio-,Ddthds

Cat.No: T15045

Target: Others

Mavorixafor trihydrochloride

Cat.No: T10296

Synonym: AMD-070 trihydrochloride

Target: HIV Protease

Cat.No: T15776

Synonym: R 89439

Target: Others

HIV-1 inhibitor-33

Cat.No: T62353

HIV-1 inhibitor-28

Cat.No: T63499

Dolutegravir SR Isomer

Cat.No: T71009

HIV-1 inhibitor-21

Cat.No: T63113

HIV-1 inhibitor-34

Cat.No: T62782

HIV-1 inhibitor-39

Cat.No: T63813

Cat.No: T74664

Dolutegravir RR Isomer

Cat.No: T70881

Cat.No: T36659

Benanomicin B (formate)

Cat.No: T37750

Cat.No: T37749

HIV-1 inhibitor-29

Cat.No: T63962

HIV-1 inhibitor-24

Cat.No: T62430

HIV-1 inhibitor-58

Cat.No: T78925

IT1t dihydrochloride

Cat.No: T11693L

Target: CXCR

Cat.No: T69081

TC 14012 hydrochloride

Cat.No: T83769

Synonym: H-Arg-Arg-Nal-Cys-Tyr-Cit-Lys-D-Cit-Pro-Tyr-Arg-Cit-Cys-Arg-NH2

HIV-1 inhibitor-25

Cat.No: T62431

Cat.No: T14208

Synonym: GENZ-644494

Target: HIV Protease

Cat.No: T11693

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T72533	4-Deoxy-4α-phorbol
	4-Deoxy-4α-phorbol 是在 E. desmondi 中发现的一种四环二萜类物质。4-Deoxy-4α-phorbol 可用于半合成 HIV-1诱导的 MT-4 细胞的细胞病理学效应抑制剂和 4α-山梨醇酯。
T20654	Heparin Certoparin,Bemiparin,Dalteparin,Adomiparin	Thrombin; Endogenous Metabolite; Antibacterial; Autophagy	Autophagy; Metabolism; Microbiology/Virology; Proteases/Proteasome
	Heparin (Adomiparin) 是硫酸粘多糖，常在临床医学上当抗凝剂使用。Heparin 在体内实验中显示出部分抗炎活性。

天然产物

4-Deoxy-4α-phorbol

Cat.No: T72533

Cat.No: T20654

Synonym: Certoparin,Bemiparin,Dalteparin,Adomiparin

Target: Thrombin, Endogenous Metabolite, Antibacterial, Autophagy

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