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23

抑制剂 & 化合物

5

天然产物

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Cat. No. Product Name Target Signaling Pathways
T5863 Indinavir sulfate

L735524 sulfate,MK-639 sulfate,硫酸茚地那韦

SARS-CoV; HIV Protease Microbiology/Virology; Proteases/Proteasome
Indinavir sulfate (L735524 sulfate) 是一种 HIV 蛋白酶抑制剂。它抑制 HIV-1 蛋白酶,IC50 值为 0.41 nM,Ki 值为 0.24 nM。它也是SARS-CoV 3CLpro 抑制剂,IC50为 1.71 μM。
T4665 Temsavir

BMS626529

HIV Protease Microbiology/Virology; Proteases/Proteasome
Temsavir (BMS626529) 是一种新型附着抑制剂,靶向 HIV-1 gp120 并阻止其与 CD4+ T 细胞结合。
T37587 ML 209

ROR Metabolism
ML-209 是一种视黄酸相关的孤儿受体 RORγ 拮抗剂 (IC50= 1.1 μM)。ML-209 抑制 HEK293t 细胞中 RORγt 转录活性(IC50= 300 nM)。ML-209 不抑制细胞中 RORα。ML-209 对鼠 Th17 细胞分化具有选择性抑制,而不影响幼稚 CD4+ T 细胞分化为 Th1 和调节性 T 细胞。
T30077 Anisperimus

LF 150195,LF-150195,LF 15-0195,LF-15-0195,LF15-0195

Caspase Apoptosis; Proteases/Proteasome
Anisperimus (LF 15-0195) 是一种免疫抑制剂,通过促进 DISC 水平的 caspase-8 和 caspase-10 激活来增强激活诱导的 T 细胞死亡,通过促进表达 Foxp3 的调节性 CD4 T 细胞的发育来预防中枢神经系统自身免疫。
T14569 BI8626

E1/E2/E3 Enzyme Ubiquitination
BI8626 是一种泛素连接酶 HUWE1 抑制剂,对 NOD/ShiLtj 小鼠自发性干燥综合征具有保护作用。BI8626 抑制细胞内胆固醇并降低磷酸化 ZAP-70、CD25 和其他激活标志物的表达,抑制 CD4 T 细胞的增殖。
T7739 L-Leucyl-L-Leucine methyl ester hydrochloride

Leu-Leu-ome hydrochloride

Others; Endogenous Metabolite Metabolism; Others
L-Leucyl-L-Leucine methyl ester hydrochloride (Leu-Leu-ome hydrochloride) 是一种人单核细胞或多形核白细胞产生的 L-亮氨酸甲酯的二肽缩合产物,能够选择性消除具有细胞毒性潜能的淋巴细胞,也能够诱导溶酶体途径应激。
T10570 Fostemsavir Tris

BMS-663068 Tris

HIV Protease Microbiology/Virology; Proteases/Proteasome
Fostemsavir Tris (BMS-663068 Tris) 是一种 HIV-1附着抑制剂。
T81403 Priliximab

cM-T412,CEN 000029

Priliximab (CEN 000029) 是一种针对CD4的人源化单克隆抗体。其与T细胞表面CD4的结合作用可引起循环中CD4+T细胞的显著并持久的减少,适用于类风湿性关节炎 (RA) 研究。
T82743 CFP10 (71–85)

CFP10 (71–85) 是具生物活性的肽类,能激活表达不同MHC II类与I类分子的人类CD4+和CD8+ T细胞,诱导IFN-γ产生及CTL活性。(CFP10 71–85).
T78275 Ivuxolimab

Ivuxolimab为针对OX40(亦称CD134TNFRSF4)的激动型单克隆抗体。该抗体针对活化CD4+及CD8+T细胞表面的共刺激受体,具备抗肿瘤能力和潜在免疫刺激作用。
T78291 Tregalizumab

BT-061

Tregalizumab为人源化抗CD4单克隆抗体(IgG1型),体外能选择性激活调节性T细胞(Tregs)功能。适用于研究自身免疫性疾病(因Treg功能不足)及过敏反应。
T83724 TPP-1 hydrochloride

Targeting PD-L1 Peptide

TPP-1是一种针对程序化细胞死亡蛋白1(PD-1)及其配体PD-1配体(PD-L1)之间蛋白-蛋白相互作用的肽抑制剂。它在无细胞实验中结合到PD-L1(Kd = 94.67 nM)。TPP-1 (20 µM)能逆转PD-L1在抗CD3激活的人类CD4+ T细胞中所引起的干扰素γ(IFN-γ)水平的下降。在使用HL-60白血病细胞与抗CD3激活的人类CD4+ T细胞共培养并在植入前预处理时,以4 mg/kg的剂量给药,可减少小鼠异种移植模型中的肿瘤体积。
T40590 NY-ESO-1 (87-111)

NY-ESO-1 (87-111) is a pan-MHC class II-restricted peptide that interacts with various HLA-DR and HLA-DP4 molecules, inducing activation of CD4+ T cells with Th1-type and Th-2/Th0-type responses, when presented in conjunction with HLA-DR and HLA-DP4 molecules.
T70065 JNJ-61803534

JNJ-61803534 是一种有效的、具有口服活性 RORγt 反向激动剂,IC50为 9.6 nM。JNJ-61803534 具有抗炎活性。JNJ-61803534Th17 分化条件下抑制人 CD4+ T 细胞产生 IL-17A。
T81308 RDN2150

RDN2150(Compound 25)为一种ZAP-70抑制剂,IC50值为14.6 nM。该化合物通过与ZAP-70的C346残基共价结合,有效抑制CD25和CD69的表达,进而阻断CD4+T细胞的活化。RDN2150可作为银屑病研究中的潜在工具。
T83846 HOXB7 (8-25) TFA

Homeobox B7 (8-25)

HOXB7 (8-25) 是 homeobox B7 (HOXB7) 的肽段,是细胞增殖的主要调控因子和肿瘤基因途径的激活剂。通过 HOXB7 (8-25) 肽脉冲的树突状细胞展示抗原,这些树突状细胞来源于分离的人类外周血单核细胞(PBMCs),刺激CD4+辅助T细胞的激活和IFN-γ的产生,从而引发特异性和多向性肿瘤反应性的抗肿瘤反应。
T37874 Feglymycin

Feglymycin is a 13-amino acid peptide originally isolated from Streptomyces that has antibacterial and antiviral activities. It is active against Gram-positive bacteria (MICs = 32-64 μg/ml) and inhibits HIV viral replication in H9 cells (IC50 = ~5 μM). Feglymycin is also active against clinical isolates of HIV-1 from clades A-D, A/E, and G (EC50s = 0.5-6.7 μM). It interacts with gp120 and inhibits HIV-1 NL4.3 binding to human soluble CD4 (EC50 = 4.4 μM) and to CD4+ SupT1 T cells by 74.5% when us...
T25109 ARN-6039

ARN 6039,ARN6039

ARN-6039 is an orally available inverse agonist of RORγ for Autoimmune Neuroinflammatory Demyelinating Disease. The activity of ARN-6039 against RORγ was demonstrated in a RORγ-activated IL-17A Prom/LUCPorter assay in HEK 293 cells (360 nM) and in IL-17 r
T36998 7β,27-dihydroxy Cholesterol

7β,27-DHC,7β,27-dihydroxy Cholesterol

7β,27-dihydroxy Cholesterol is an oxysterol and agonist of retinoic acid receptor-related orphan receptor γ (RORγ) and RORγt. [1] It activates RORγ- or RORγt-dependent signaling with EC50 values of 691 and 1,045 nM, respectively, in reporter assays using HEK293T cells expressing the recombinant human receptors. 7β,27-dihydroxy Cholesterol is selective for RORγ and RORγt over a panel of eight additional nuclear receptors at 30 &#181M. It increases IL-17A production in Th17-polarized isolated hum...
T36034 CAY10774

CAY10774 is an inhibitor of the protein-protein interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 (IC50= 15 nM in a homologous time-resolved fret (HTRF) assay).1It increases the activation of Jurkat cells expressing PD-1 in co-culture with artificial antigen-presenting cells (aAPCs) expressing PD-L1 (EC50= 6.6 μM in a reporter assay). CAY10774 increases surface expression of PD-1 on primary human CD4+and CD8+T cells co-cultured with aAPCs. 1.Konieczny, M., Musielak, B., Koc...
T64280 ODN 2216

ODN 2216 是一种 TLR9 (toll-like receptor 9) 配体或激动剂,能够诱导产生大量的 IFN-α 和 IFN-β。ODN 2216 可以利用 pDC (浆细胞样 DC) 诱导 IFN-α,以及利用 DC (树突状细胞) 产生IL-12 (p40)。ODN 2216 能够间接的、在 IFN-α/β 介导下刺激外周血单核细胞 (PBMC) 产生 IFN-γ。ODN 2216 可以激活 NK 细胞,诱导 IFN-γ 产生 TCR 触发的 CD4+T 细胞。
T35995 Ferrichrome (iron-free)

Ferrichrome (iron-free) 是一种异羟肟酸盐铁载体,可由各种真菌产生(包括 U. sphaerogena),促进这些生物体对铁的螯合和吸收,还被细菌用作异源铁载体,包括铜绿假单胞菌和副溶血性弧菌。 Ferrichrome (iron-free) (0.8 μM) 可以抑制由刀豆球蛋白 A 诱导的小鼠脾脏单核细胞增殖,并减少刀豆球蛋白 A 刺激的 CD4+ T 细胞的数量。它还以浓度依赖性方式抑制过氧化氢对 LDL 的血红素催化氧化。
T83910 S1PL-IN-31

Sphingosine-1-Phosphate Lyase Inhibitor 31,S1PL Inhibitor 31,S1P Lyase Inhibitor 31

S1PL-IN-31是一种鞘氨醇-1-磷酸(S1P)裂解酶的抑制剂(IC50 = 210 nM),同时也是Smoothened(Smo)受体的对抗剂(IC50 = 440 nM)。在体内,S1PL-IN-31 (每天2 mg/kg)能够防止实验性自身免疫性脑炎(EAE)模型大鼠中,由髓鞘少突胶质细胞糖蛋白(MOG)肽段MOG29-152诱发的颈部及胸部淋巴细胞渗透和神经肌肉虚弱。该化合物降低了大鼠的淋巴细胞总数及CD4+ T细胞、CD8+ T细胞和B细胞的水平。S1PL-IN-31 (每天3及10 mg/kg剂量)在雄性和雌性大鼠心脏和淋巴结中增加了S1P水平,并且在雌性大鼠中降低了心率。

化合物

Indinavir sulfate
Cat.No: T5863
Synonym: L735524 sulfate,MK-639 sulfate,硫酸茚地那韦
Target: SARS-CoV, HIV Protease
Temsavir
Cat.No: T4665
Synonym: BMS626529
Target: HIV Protease
ML 209
Cat.No: T37587
Synonym:
Target: ROR
Anisperimus
Cat.No: T30077
Synonym: LF 150195,LF-150195,LF 15-0195,LF-15-0195,LF15-0195
Target: Caspase
BI8626
Cat.No: T14569
Synonym:
Target: E1/E2/E3 Enzyme
L-Leucyl-L-Leucine methyl ester hydrochloride
Cat.No: T7739
Synonym: Leu-Leu-ome hydrochloride
Target: Others, Endogenous Metabolite
Fostemsavir Tris
Cat.No: T10570
Synonym: BMS-663068 Tris
Target: HIV Protease
Priliximab
Cat.No: T81403
Synonym: cM-T412,CEN 000029
Target:
CFP10 (71–85)
Cat.No: T82743
Synonym:
Target:
Ivuxolimab
Cat.No: T78275
Synonym:
Target:
Tregalizumab
Cat.No: T78291
Synonym: BT-061
Target:
TPP-1 hydrochloride
Cat.No: T83724
Synonym: Targeting PD-L1 Peptide
Target:
NY-ESO-1 (87-111)
Cat.No: T40590
Synonym:
Target:
JNJ-61803534
Cat.No: T70065
Synonym:
Target:
RDN2150
Cat.No: T81308
Synonym:
Target:
HOXB7 (8-25) TFA
Cat.No: T83846
Synonym: Homeobox B7 (8-25)
Target:
Feglymycin
Cat.No: T37874
Synonym:
Target:
ARN-6039
Cat.No: T25109
Synonym: ARN 6039,ARN6039
Target:
7β,27-dihydroxy Cholesterol
Cat.No: T36998
Synonym: 7β,27-DHC,7β,27-dihydroxy Cholesterol
Target:
CAY10774
Cat.No: T36034
Synonym:
Target:
ODN 2216
Cat.No: T64280
Synonym:
Target:
Ferrichrome (iron-free)
Cat.No: T35995
Synonym:
Target:
S1PL-IN-31
Cat.No: T83910
Synonym: Sphingosine-1-Phosphate Lyase Inhibitor 31,S1PL Inhibitor 31,S1P Lyase Inhibitor 31
Target:
Cat. No. Product Name Target Signaling Pathways
T6S1885 Benzoylmesaconine

Mesaconine 14-benzoate,苯甲酰新乌头原碱

Others Others
Benzoylmesaconine (Mesaconine 14-benzoate) 是乌头汤最丰富的组分。其中乌头汤可用于研究类风湿性关节炎。
T5681 ETHYL CAFFEATE

咖啡酸乙酯,ETHYL 3,4-DIHYDROXYCINNAMATE

NF-κB; COX; PGE Synthase; NO Synthase Immunology/Inflammation; Neuroscience; NF-κB
Ethyl Caffeate (ETHYL 3,4-DIHYDROXYCINNAMATE) 是从鬼针草分离的一种酚类天然产物,在体外或在小鼠皮肤中抑制NF-κB 活化及其下游炎症介质的诱导型一氧化氮合酶、环氧合酶 2 和前列腺素 E2。
T2S2173 (E)-Naringenin chalcone

Isosalipurpol,柚皮苷查尔酮,Chalconaringenin,trans-2'4'6'4-tetrahydroxychalcone,柚皮素查耳酮

Others Others
Naringenin chalcone (Isosalipurpol) 是一种黄酮醇生物合成的中间体,在查耳酮异构酶的作用下,自发代谢成柚皮素。它具有抗炎和抗过敏活性。
T21441 Prostratin

12-Deoxyphorbol-13-acetate

Prostratin, a protein kinase C activator, has been shown to exhibit promising therapeutic potential against other diseases such as cancer and Alzheimer's disease. Prostratin has the potential to be useful in the treatment of HIV as it could flush viral re
T73402 Flavipin

Flavipin 是一种芳香烃受体(Ahr)激动剂,可诱导小鼠 CD4+T 细胞和 CD11b+巨噬细胞表达 Ahr 下游基因。Flavipin 抑制 Arid5a 在 Il23a3'UTR 上的稳定功能,这是一种新发现的靶 mRNA。Flavipin 具有清除 DPPH 自由基的能力,IC50值为7.2 μM,对α-葡萄糖苷酶具有较强的抑制作用,IC50值为 33.8 μM。

天然产物

Benzoylmesaconine
Cat.No: T6S1885
Synonym: Mesaconine 14-benzoate,苯甲酰新乌头原碱
Target: Others
ETHYL CAFFEATE
Cat.No: T5681
Synonym: 咖啡酸乙酯,ETHYL 3,4-DIHYDROXYCINNAMATE
Target: NF-κB, COX, PGE Synthase, NO Synthase
(E)-Naringenin chalcone
Cat.No: T2S2173
Synonym: Isosalipurpol,柚皮苷查尔酮,Chalconaringenin,trans-2'4'6'4-tetrahydroxychalcone,柚皮素查耳酮
Target: Others
Prostratin
Cat.No: T21441
Synonym: 12-Deoxyphorbol-13-acetate
Target:
Flavipin
Cat.No: T73402
Synonym:
Target:
TargetMol Loading
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