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22

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
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。
T68766	Dp2mT
	Dp2mT is an iron chelator which inhibits HIV-1 transcription.
T68484	2-MT-63
	2-MT 63 is a novel TIE-2 kinase inhibitor that demonstrates unique and improved kinase selectivity compared to other inhibitors known to interact with TIE-2. 2-MT 63 has a good kinase selectivity profile in enzyme assays with >30-fold selectivity (typically much greater) against the tested kinases. Importantly, the profile includes selectivity against other targets of relevance for angiogenesis (KDR, PDGFR, EPHB4).
T61570	Mt KARI-IN-2
	Mt KARI-IN-2 (compound 5b) is a highly effective inhibitor of Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI), with a Ki value of 2.02 μM. This compound also exhibits inhibitory activity against Mtb H37Rv, with a MIC value of 0.78 μM. Moreover, Mt KARI-IN-2 demonstrates low cytotoxicity, as evidenced by a HEK IC 50 greater than 86 μg/mL [1].
T17319	1,2-Bis(2-iodoethoxy)ethane	Others; PROTAC Linker	Others; PROTAC
	1,2-Bis(2-iodoethoxy)ethane 是一种属于 PEG 类的 PROTAC linker，可用于 MT802 和 SJF620 的合成。其中 MT-802 和 SJF620 都是 PROTAC BTK 降解剂，DC50分别为 1 和 7.9 nM。
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.
T29044	UCM 765 UCM-765,UCM765
	UCM 765 is a partial agonist of melatonin MT(2) receptor.
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.
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).
T37455	C18 D-threo Ceramide (d18:1/18:0) C18 D-threo Ceramide (d18:1/18:0)
	C18 D-threoCeramide (d18:1/18:0) is a synthetic ceramide and stereoisomer of C18 ceramide .1It inhibits rat brain mitochondrial ceramidase (mt-CDase) with an IC50value of 16.6 μM.2[Matreya, LLC. Catalog No. 1855] 1.Koolath, S., Murai, Y., Suga, Y., et al.Chiral combinatorial preparation and biological evaluation of unique ceramides for inhibition of sphingomyelin synthaseChirality32(3)308-313(2019) 2.Usta, J., El Bawab, S., Roddy, P., et al.Structural requirements of ceramide and sphingosine bas...
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。
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。
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...
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...
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。
T83707	F9170 TFA
	F9170是一种抗病毒肽，对应HIV-1包膜糖蛋白的789-803氨基酸。它与HIV-1包膜蛋白胞浆尾部的LLP1域结合，并抑制HIV-1 IIIB对MT-2细胞的感染(EC50 = 0.19 µM)。在恒河猴模型的类人猿免疫缺陷病毒(SHIV)感染中，F9170 (3 mg/kg)能降低血浆病毒负荷。
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。
T62305	MtTMPK-IN-2
	MtTMPK-IN-2 (compound 15)为一高效MtbTMPK抑制剂，IC50值达1.1 μM。该化合物对MtbH37Rv表现出抑制活性（MIC = 12.5 μM），同时对人成纤维细胞MRC-5显示出一定细胞毒性（EC50= 6.1 μM）。MtTMPK-IN-2适用于结核病研究。
T70856	3-Oxobetulin Acetate
	3-Oxobetulin acetate is a derivative of the cholesterol biosynthesis inhibitor betulin. It inhibits the growth of P388 murine lymphocytic leukemia cells (EC50 = 0.12 µg/ml), as well as human MCF-7 breast, SF-268 CNS, H460 lung, and KM20L2 colon cancer cells (GI50s = 8, 10.6, 5.2, and 12.7 µg/ml, respectively), but not BxPC-3 pancreas or DU145 prostate cancer cells (GI50s = >10 µg/ml for both). 3-Oxobetulin acetate inhibits replication of X4 tropic recombinant HIV (NL4.3-Ren) in MT-2 lymphoblasto...
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

化合物

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: T68766

Cat.No: T68484

Cat.No: T61570

1,2-Bis(2-iodoethoxy)ethane

Cat.No: T17319

Target: Others, PROTAC Linker

3'-Deoxy-4-thiothymidine

Cat.No: T29393

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

Cat.No: T29044

Synonym: UCM-765,UCM765

Cat.No: T15776

Synonym: R 89439

Target: Others

4'-Ethynyl-2'-deoxyadenosine

Cat.No: T10141

Target: Others

C18 D-threo Ceramide (d18:1/18:0)

Cat.No: T37455

Synonym: C18 D-threo Ceramide (d18:1/18:0)

HIV-1 integrase inhibitor 10

Cat.No: T72162

AMD 3465 hexahydrobromide

Cat.No: T7208

Synonym: GENZ-644494 (hexahydrobromide)

Target: HIV Protease, CXCR

Benanomicin B (formate)

Cat.No: T37750

Cat.No: T37749

Cat.No: T36659

Cat.No: T74664

Cat.No: T83707

HIV-1 inhibitor-24

Cat.No: T62430

Cat.No: T62305

3-Oxobetulin Acetate

Cat.No: T70856

Cat.No: T14208

Synonym: GENZ-644494

Target: HIV Protease

Cat. No.	Product Name	Target	Signaling Pathways
T4S1521	1,4-Dicaffeoylquinic acid 1,4-二咖啡酰奎宁酸,洋蓟素	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	1,4-Dicaffeoylquinic acid 是一种苯丙素类物质，从苍耳子中获得，可以减少 LPS 诱导的 TNF-α 的生成，具有抗炎活性。
T75333	Quinine hemisulfate hydrate
	Quinine hemisulfate hydrate，一种从金鸡纳树皮提取的生物碱，具有抗疟疾效果。作为钾离子通道 (potassium channel) 抑制剂，它能够抑制由电压脉冲触发的MT mSlo3 (KCa5.1) 通道在+100 mV下的电流活动，其IC50值达169 μM。

天然产物

1,4-Dicaffeoylquinic acid

Cat.No: T4S1521

Synonym: 1,4-二咖啡酰奎宁酸,洋蓟素

Target: HIV Protease

Quinine hemisulfate hydrate

Cat.No: T75333

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