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6
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T28178 |
NLRP3-IN-9
INF-4E,INF 4E,INF4E |
NOD | Immunology/Inflammation; NF-κB |
NLRP3-IN-9 (INF-4E) 是 NLRP3 ATPase 和 caspase-1 的抑制剂。 NLRP3-IN-9 通过不可逆地捕获硫醇亲核体发挥作用,以时间和浓度依赖性方式防止 ATP 和尼日利亚菌素触发的人 THP-1 细胞焦亡。 | |||
T9645 |
CU-115
N-(4-(3,5-bis(trifluoromethyl)phenoxy)phenyl)-2-fluoro-6-iodobenzamide |
TLR | Immunology/Inflammation |
CU-115 是一种有效的,选择性的 TLR8 拮抗剂。CU-115对 TLR8 和 TLR7的 IC50分别为1.04 µM 和=>50 µM。THP-1 细胞中,CU-115 减少了 R-848 激活的 TNF-α 和 IL-1β 的产生。 | |||
T3502 |
C29
|
TLR | Immunology/Inflammation |
C29 是 Toll 样受体 2 抑制剂,可阻断 hTLR2/1 和 hTLR2/6 信号,IC50值分别为 19.7 和 37.6 μM。 | |||
T63140 |
LSD1-IN-20
|
Histone Demethylase | Chromatin/Epigenetic |
LSD1-IN-20 是一种有效的 LSD1/G9a 双重抑制剂,其 Ki 值分别为 0.44 和 0.68 μM。LSD1-IN-20 在体外实验中对 THP-1 白血病细胞和 MDA-MB-231 乳腺癌细胞显示出抗增殖活性,72 h 时 IC50 分别为 0.51 和 1.60 μM。 | |||
T4062 |
CAY10602
|
Sirtuin | Chromatin/Epigenetic; DNA Damage/DNA Repair |
CAY10602 是一种SIRT1激活剂,可剂量依赖性地抑制 THP-1 细胞中脂多糖对 TNF-α 的 NF-κB 依赖性诱导。 | |||
T1764 |
Adezmapimod
PB 203580,4-(4-氟苯基)-2-(4-甲基亚磺酰基苯基)-5-(4-吡啶基)-1H-咪唑,RWJ 64809,SB203580 |
Mitophagy; p38 MAPK; Autophagy | Autophagy; MAPK |
Adezmapimod (SB 203580) 是一种 p38 MAPK 抑制剂 (IC50=0.3-0.5 μM),具有选择性和 ATP 竞争性。Adezmapimod 具有自噬和线粒体自噬的激活活性。Adezmapimod 显示出比 PKB、LCK 和 GSK-3β 高 100 倍以上的选择性。 | |||
T61405 | LSD1-IN-14 | ||
LSD1-IN-14, a powerful and specific inhibitor of LSD1 (with an IC50 value of 0.89 μM), effectively suppresses the growth of A549 and THP-1 cells and promotes the apoptosis of tumor cells [1]. | |||
T28269 |
ORY-1001 free base
RG 6016,ORY-1001,ORY 1001,ORY1001,RG-6016,RG6016 |
||
ORY-1001 is a KDM1A inhibitor (IC50 <20nM) with high selectivity against related FAD dependent aminoxidases (MAO-A/B, IL4I1, KDM1B >100uM, SMOX 7uM). Treatment of THP-1 (MLL-AF9) cells with ORY-1001, results in a time/dose dependent me2H3K4 accumulation a | |||
T74718 |
STING modulator-5
|
||
STINGmodulator-5(compound 38)为THP-1和外周血单个核细胞(PBMC)的拮抗剂,其在THP-1上的pIC50值为8.9,在PBMC上的pIC50值为8.1。此化合物适用于免疫性疾病研究。 | |||
T63854 | Cathepsin C-IN-3 | ||
Cathepsin C-IN-3 是组织蛋白酶 C (Cat C) 的有效抑制剂 (IC50: 61.79 nM),也能抑制 THP-1 细胞 (IC50: 101.5 nM) 和 U937 细胞 (IC50: 86.5 nM)。 | |||
T38328 |
CU-32
|
||
CU-32 is an inhibitor of cyclic GMP-AMP (cGAMP) synthase (cGAS; IC50= 0.45 μM).1It reduces DNA-, but not Sendai virus-, induced dimerization of IFN regulatory factor 3 in THP-1 cells, indicating selectivity for the cGAS DNA sensing pathway over the RIG-I-MAVS RNA sensing pathway. It is also selective for cGAS over toll-like receptors (TLRs) at 50 μM. CU-32 decreases IFN-stimulatory DNA-induced production of IFN-β in THP-1 cells when used at concentrations of 10, 30, and 100 μM. 1.Padilla-Salinas... | |||
T62659 | Cathepsin C-IN-4 | ||
Cathepsin C-IN-4 是一种组织蛋白酶 C (Cat C) 的有效抑制剂 (IC50: 65.6 nM)。Cathepsin C-IN-4 对 THP-1 (IC50: 203.4 nM)和 U937 (IC50: 177.6 nM) 细胞具有抑制作用。 | |||
T38329 |
CU-76
|
||
CU-76 is an inhibitor of cyclic GMP-AMP synthase (cGAS; IC50= 0.24 μM).1It reduces DNA-, but not Sendai virus-, induced dimerization of IFN regulatory factor 3 in THP-1 cells, indicating selectivity for the cGAS DNA sensing pathway over the RIG-I-MAVS RNA sensing pathway. CU-76 decreases IFN-stimulatory DNA-induced production of IFN-β in THP-1 cells when used at concentrations of 10, 30, and 100 μM. 1.Padilla-Salinas, R., Sun, L., Anderson, R., et al.Discovery of small-molecule cyclic GMP-AMP sy... | |||
T83901 |
BDW568
|
||
BDW568是一种刺激素干扰素基因(STING)的激动剂,同时是BDW-OH的前药形式。在使用THP-1细胞的报告基因测定中,它能诱导STING转录活性(EC50 = 7.6 µM)。BDW568(50 µM)在THP-1细胞中诱导TANK结合激酶1(TBK1)和IFN调节因子3(IRF3)的磷酸化。 | |||
T14909 |
CCX140
3-三氟甲基-4-氯-N-[2-[7H-吡咯并[2,3-D]嘧啶-4-羰基]-5-甲基-3-吡啶基]苯磺酰胺,CCX140-B |
CCR | Immunology/Inflammation; Microbiology/Virology |
CCX140 (CCX140-B) 是 CCR2 的拮抗剂。 | |||
T16614 |
Propargyl-PEG4-acid
|
Others | Others |
Propargyl-PEG4-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-IAP PROTACs Ibrutinib -based PROTAC 2 and an analogue PROTAC 3. PROTAC 3 causes BTK degradation with a DC50 of 200 nM in THP-1 cells[1]. | |||
T78068 |
O-allylvanillin
|
Others | Others |
O-allylvanillin为o-烯丙基查尔酮衍生物,呈现抗癌活性。该化合物对THP-1、HL60、Hep-G2、MCF-7细胞系生长抑制作用显著,其IC50值依次为74.76 μM、63.52 μM、90.99 μM、90.11 μM。 | |||
T9552 |
BAZ1A-IN-1
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
BAZ1A-IN-1 是BAZ1A(含溴结构域蛋白)抑制剂(Kd:0.52 μM)。它对低表达BAZ1A 的癌细胞表现出弱活性或无活性,但对高表达BAZ1A 的癌细胞系显示出良好的抗生存作用。 | |||
T63088 |
NOD2 antagonist 1
|
||
NOD2 antagonist 1 (compound 32) 是一种有效的、选择性的 NOD2 拮抗剂 (IC50: 5.23 μM)。NOD2 antagonist 1 在 THP-1 细胞,对 Muramyl dipeptide (MDP) 诱导的 IL-8 分泌表现出抑制作用。NOD2 antagonist 1 在 PBMCs 细胞,可以抑制 MDP 诱导的 IL-6、IL-10 和 TNF-α 的水平升高。 | |||
T72615 | STING modulator-4 | ||
STINGmodulator-4 是一种竞争性的 STING 调节剂,对 R232HSTING 的 Ki 为 0.0933 μM。STINGmodulator-4 在 THP-1 细胞中对 p-IRF3 的 EC50为 >10 μM。 | |||
T63716 | LSD1-IN-18 | ||
LSD1-IN-18 是有效的、非共价的、选择性的 LSD1 抑制剂 (Ki:0.156 μM; KD: 0.075 μM)。LSD1-IN-18 在 THP-1 白血病细胞和 MDA-MB-231 乳腺癌细胞中表现出抗增殖效果,其IC50(72 h) 分别为 0.16 和 0.21 μM。 | |||
T38159 |
STING Agonist 12b
|
||
STING agonist 12b is an agonist of stimulator of interferon genes (STING).1It binds to STING (Kd= 26.4 μM) and induces interferon reporter gene expression in cells expressing human or mouse STING (EC50s = 7.45 and 10.23 μM, respectively). STING agonist 12b (40 μM) induces expression of TNF-a, IL-6, IP-10, and IL-1b in THP-1 cells. 1.Hou, S., Lan, X.-j., Li, W., et al.Design, synthesis and biological evaluation of acridone analogues as novel STING receptor agonistsBioorg. Chem.95103556(2020) | |||
T35701 |
FSL-1 TFA
|
||
FSL-1 TFA, a bacterial-derived toll-like receptor 2/6 (TLR2/6) agonist, enhances resistance to experimental HSV-2 infection[1]. FSL-1 TFA induces MMP-9 production through TLR2 and NF-κB/AP-1 signaling pathways in monocytic THP-1 cells[2]. FSL-1 significantly reduces HSV-2 replication in human vaginal epithelial cells (EC)[1].FSL-1 induces significant resistance to experimental genital HSV-2 infection through elaboration of a specific cytokine response profile[1].FSL-1 (50 ng/mL, 24 hours) induce... | |||
T38162 | STING18 | ||
STING18 is a competitive ligand of stimulator of interferon genes (STING; IC50 = 0.068 μM in a radioligand binding assay).1 It inhibits cGAMP-induced IFN-β production (IC50 = 11 μM) but does not stimulate IFN-β production (EC50 = >30 μM) in THP-1 cells. |1. Siu, T., Altman, M.D., Baltus, G.A., et al. Discovery of a novel cGAMP competitive ligand of the inactive form of STING. Med. Chem. Lett. 10(1), 92-97 (2019). | |||
T72614 | STING modulator-3 | ||
STINGmodulator-3 是一种 STING 抑制剂。在闪烁接近实验中,STINGmodulator-3 抑制 R232STING 的 Ki 值为 43.1 nM。STINGmodulator-3 对 THP-1 细胞的 IRF-3 激活和 TNF-β诱导无影响。 | |||
T9655 |
NBC 6
|
||
NLRP3-IN-NBC6 是一种有效的选择性 NLRP3炎性小体抑制剂 ,IC50为574 nM,其作用独立于 Ca2+。NLRP3-IN-NBC6 抑制 Nigericin 诱导的 THP-1 细胞炎症反应和 Imiquimod 诱导的 LPS-primed 的骨髓源性巨噬细胞 (BMDMs) 释放 IL-1β。 | |||
T36221 |
2-chloro Palmitic Acid
|
||
2-chloro Palmitic acid is a monochlorinated form of palmitic acid . It is produced in a myeloperoxidase (MPO) and time-dependent manner in neutrophils stimulated by phorbol 12-myristate 13-acetate . 2-chloro Palmitic acid (10 μM) induces neutrophil extracellular trap (NET) formation (NETosis) in human neutrophils, increasing DNA release from neutrophils, colocalization of MPO with extracellular DNA (ecDNA), and trapping of E. coli. It increases COX-2 protein levels in human coronary artery endot... | |||
T61945 |
hGGPPS-IN-1
|
||
hGGPPS-IN-1 是 C-2 取代的噻吩并嘧啶基双膦酸盐 (C2-ThP-BPs) 的类似物,对人类香叶基香叶基焦磷酸合成酶 (hGGPPS) 具有有效的抑制作用。hGGPPS-IN-1 可选择性诱导多发性骨髓瘤 (MM) 细胞凋亡 (apoptosis)。hGGPPS-IN-1在体内表现出抗骨髓瘤活性。 | |||
T63315 | IRAK4-IN-19 | ||
IRAK4-IN-19 是白介素 1 受体相关激酶 4 (IRAK4) 的有效抑制剂 (IC50: 4.3 nM)。IRAK4-IN-19 能够阻碍 THP 和 DC 细胞中 LPS 诱导的 IL23 产生,抑制关节炎模型大鼠的关节炎发展。IRAK4-IN-19 能够用于研究关节炎疾病。 | |||
T62950 | IRAK4-IN-18 | ||
IRAK4-IN-18 是一种白介素 1 受体相关激酶 4 (IRAK4) 的有效抑制剂 (IC50: 15 nM)。IRAK4-IN-18 能够抑制 THP 和 DC 细胞中 LPS 诱导的 IL23 产生,阻断关节炎模型大鼠的关节炎发展。IRAK4-IN-18 可用于研究关节炎疾病。 | |||
T83775 |
STING Agonist 12L
Stimulator of Interferon Genes Agonist 12L |
||
STING激动剂12L是一种刺激干扰素基因(STING)的激动剂。它与野生型STING结合(IC50 = 1.15 µM),以及STING的R232、AQ和Q变体(IC50分别为1.06、0.61和1.12 µM),并在THP-1和RAW 264.7细胞中诱导报告基因表达(EC50分别为0.38和12.94 µM)。STING激动剂12L (5 µM)在THP-1细胞中诱导IFNB1、CXCL10和IL6 mRNA的表达。在体内,STING激动剂12L (10 mg/kg)提高了血浆IFN-β水平,并且在B16/F10小鼠黑色素瘤模型中减少了肿瘤体积和肺转移灶的数量。 | |||
T36859 |
C16 Globotriaosylceramide (d18:1/16:0)
C16 Globotriaosylceramide (d18:1/16:0) |
||
C16 globotriaosylceramide is an endogenous sphingolipid found in mammalian cell membranes that is synthesized from C16 lactosylceramide . C16 globotriaosylceramide acts as a receptor for Shiga toxin in B cell-derived Raji cells and THP-1 monocytes. It accumulates in endothelial cells, pericytes, vascular smooth muscle cells, renal epithelial cells, dorsal ganglia neuronal cells, and myocardial cells in patients with Fabry disease. C16 globotriaosylceramide is also upregulated in plasma of patien... | |||
T72989 |
hGGPPS-IN-3
|
Apoptosis | Apoptosis |
hGGPPS-IN-3(Compound 13h)是一种针对人类香叶基香叶基焦磷酸合成酶(hGGPPS)的有效抑制剂,属于C-2取代的噻吩并嘧啶基双膦酸盐(C2-ThP-BPs)衍生物。该化合物能够诱导多发性骨髓瘤(MM)细胞具有选择性地进入凋亡(apoptosis),并且在体内展现了对抗骨髓瘤的活性。 | |||
T38160 |
STING Agonist 1a
|
||
STING agonist 1a is an agonist of stimulator of interferon genes (STING).1It induces expression of an IRF-inducible SEAP reporter gene in a cell-based assay (EC50= 16.77 μM). STING agonist 1a (12.5-100 μM) induces expression of IFN-β, IL-6, and chemokine (C-X-C motif) ligand 10 (CXCL10) in THP-1 cells, an effect that can be reversed by STING knockout or the STING inhibitor H-151 . 1.Hou, H., Yang, R., Liu, X., et al.Discovery of triazoloquinoxaline as novel STING agonists via structure-based vir... | |||
T83710 |
Gastric Inhibitory Peptide (22-51) (human) TFA
GIP (22-51),Glucose-dependent Insulinotropic Peptide (22-51) |
||
胃抑制肽(GIP) (22-51) 是一种具有30个氨基酸的前动脉硬化肽,对应于GIP前体蛋白proGIP的第22至51个氨基酸残基,已在人类血浆中发现。在1 µM的浓度下使用,该肽能引起在巨峰细胞分化的THP-1细胞和分离的人类主动脉内皮细胞中IκB-α的降解和NF-κB的核转移。在体内,GIP (22-51) 增加了ApoE-/-小鼠的动脉粥样硬化病变面积和斑块形成。 | |||
T37439 |
C18 Globotriaosylceramide (d18:1/18:0)
|
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C18 globotriaosylceramide is an endogenous sphingolipid found in mammalian cell membranes that is synthesized from lactosylceramide . It inhibits aggregation of human neutrophils induced by phorbol 12-myristate 13-acetate (PMA; 10008014) when used at a concentration of 1 μM. C18 globotriaosylceramide acts as a receptor for Shiga toxin in B cell-derived Raji cells and THP-1 monocytes. It accumulates in the brain, heart, kidney, liver, lung, and spleen in a mouse model of Fabry disease, a lysosoma... | |||
T37722 |
Diprovocim-1
|
||
Diprovocim-1 is an agonist of the toll-like receptor 1/2 heterodimer.1It induces TNF-α release in THP-1 cells (EC50= 110 pM), an effect that can be inhibited by anti-TLR1 or anti-TLR2 antibodies. Diprovocim-1 (10 mg/kg) increases the production of ovalbumin-specific IgG1 in wild-type, but notTLR2-/-, mice sensitized to ovalbumin.2It also enhances anti-PD-L1 antibody-induced activation of cytotoxic T lymphocytes, reduction of tumor growth, and increases in survival in a B16/F10 murine melanoma mo... | |||
T83856 |
AP-1
|
||
AP-1是一种微型化的蛋白质水解靶向嵌合体(PROTAC),由吲哚美辛(±)连接的间变性淋巴瘤激酶(ALK)配体和E3泛素连接酶配体通过超短连接器相连。在10至300 nM浓度范围内使用时,AP-1能高效降解Karpas-299细胞中高表达的ALK融合蛋白NPM-ALK,此效应可被蛋白酶体抑制剂MG-132阻断。它还能降解在SN-N-SH和NCI H3122细胞中表达的ALK融合蛋白EML4-ALK及含有苯丙氨酸至亮氨酸替换突变(ALKF1174L)的ALK。AP-1对依赖ALK的Karpas-299细胞具有细胞毒性(IC50 = 0.1265 nM),但对非ALK依赖的THP-1细胞无细胞毒性(IC50 = 2,704 nM)。在给药剂量为25, 50, 和100 mg/kg时,能减小NCI H3122小鼠移植瘤模型中的肿瘤体积。 | |||
T36461 |
CAY10748
CAY10748 |
||
CAY10748 is an agonist of stimulator of interferon genes (STING; IC50= 0.3794 μM in a competition binding assay).1It activates STING in STING-expressing, but not STING knockout, THP-1 cells (EC50s = 0.287 and >100 μM, respectively, in a reporter assay). It induces phosphorylation of STING at the serine in position 366, as well as phosphorylation of TBK1 and IFN regulatory factor 3 (IRF3), indicating activation of the STING-TBK1-IRF3 signaling pathway. CAY10748 increases the secretion of IFN-β an... | |||
T35812 |
CAY10591
CAY10591 |
||
Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). Human SIRT1 is the homolog of yeast silent information regulator 2 (Sir2) and has been shown to regulate the activity of the p53 tumor suppressor and inhibit apoptosis. Small molecule activators of SIRT1, such as resveratrol, extend lifespan in yeast and C. elegans in a manner that resembles caloric restriction. CAY10591 has been identified as an activator of the enzyme SIRT1. This com... | |||
TP2109 |
TAT 14
|
Nrf2 | Immunology/Inflammation |
TAT-14 是 由14 个氨基酸组成的多肽,是 Nrf2激活因子,表现出抗炎活性。它通过靶向 Nrf2 上 Keap1 的结合位点而非 Nrf2 mRNA 表达来提高 Nrf2 蛋白水平。 | |||
T36996 |
MSA-2 dimer
|
||
MSA-2 dimer is a selective, orally active non-nucleotide STING agonist (Kd=145 μM) with long-term antitumor and immunogenic activity. MSA-2 dimer is bound to STING as a non-covalent dimer exhibiting higher permeability than cyclic dinucleotide[1]. MSA-2 dimer (60 mg/kg; p.o.; 50 days) inhibits tumor growth and prolongs overall survival[1]. MSA-2 dimer (40 mg/kg; s.c.; 25 days) induces complete tumor regression[1].MSA-2 dimer (60 mg/kg; p.o.; 4 hours) increases proinflammatory cytokine (IFN-β) le... | |||
T28290 |
Pactimibe
CS 505,CS-505,CS505,Pactimibe free base,帕替麦布 |
||
Pactimibe is a ACAT inhibitor. It has anti-atherosclerotic activity. | |||
T28985 |
TMI-1
WAY-171318 |
Apoptosis; MMP | Apoptosis; Proteases/Proteasome |
TMI-1 (WAY-171318) 是一种有效的抑制剂,用于抑制去整合素金属酶17 (ADAM17) 和其他基质金属蛋白酶MMPs。TMI-1 能够有效地抑制LPS 诱导的人原代单核细胞和人全血中TNF-α的分泌。TMI-1 在三阴性 (TN) 和过度表达ERBB2的乳腺肿瘤细胞系中选择性地诱导Caspase 依赖的细胞凋亡。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN1879 |
Lucideric acid A
Lucidenic acid A,赤芝酸A |
MMP; p38 MAPK; JNK | MAPK; Proteases/Proteasome |
Lucideric acid A (Lucidenic acid A) 是分离自灵芝的天然产物,可抑制 PMA 诱导的MMP-9活性,具有抵抗肝癌细胞侵袭的作用。 | |||
T81159 | Sibiricine | ||
Sibiricine(Compound 8),一种从Corydalis crispa药用植物提取的异喹啉类生物碱,对于LPS诱导的THP-1细胞产生的TNF-α显示出显著的抗炎效果。 | |||
T37751 |
Streptazolin
|
||
Streptazolin is a fungal metabolite originally isolated from S. viridochromogenes. It increases NF-κB activity when used at concentrations ranging from 60 to 130 μg/ml, at least in part, via PI3K signaling. Streptazolin enhances TNF-α secretion induced by LPS and enhances IL-8 secretion when used alone or in combination with LPS in THP-1 Blue cells. | |||
TN5238 |
Viscidulin II
|
IL Receptor; TNF | Apoptosis; Immunology/Inflammation |
Viscidulin II can be potential therapeutic agents against P. acnes-induced skin inflammation, it can significantly suppress P. acnes-induced IL-8 and IL-1β production in THP-1 cells, concomitant intradermal injection of viscidulin II with P. acnes can effectively attenuate P. acnes-induced ear swelling, and decrease the production of IL-6 and tumor necrosis factor-α in ear homogenates. | |||
T37442 |
Aspergillin PZ
|
||
Aspergillin PZ is a fungal metabolite originally isolated from A. awamori. It induces morphological deformation of P. oryzae conidia when used at a concentration of 89 nM. Aspergillin PZ is active against S. epidermidis (MIC = 20 μM) but not S. aureus, E. coli, or B. cereus (MICs = >20 μM). It is cytotoxic to HL-60 promyelocytic leukemia cells (IC50 = 56.61 μM) but not THP-1 acute monocytic leukemia or PC3 prostate cancer cells (IC50s = >80 μM). | |||
TN3395 |
Alpinone 3-acetate
|
IFNAR | Immunology/Inflammation |
Alpinone 3-acetate 具有抗炎作用,可抑制12-O-tetradecanophenol 13-acetate 所致小鼠耳部水肿模型的炎症反应。Alpinone 3-acetate 是Alpinone 衍生物 。Alpinone 是一种具有活性的天然化合物,来源于向日葵,具有免疫调节和抗病毒活性 。 |