73
10
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
T11492 |
GSK2983559 free acid
|
Others; RIP kinase | Apoptosis; NF-κB; Others |
GSK2983559 free acid 是一种有效的特异性受体相互作用蛋白 2 (RIP2) 抑制剂。 GSK2983559 free acid 在阻断人类炎症性肠病外植体样品和体内的许多促炎细胞因子反应方面表现出优异的活性。 | |||
T38576 |
Propargyl-PEG1-THP
Propargyl-PEG1-THP |
||
Propargyl-PEG1-THP is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells. | |||
T9016 |
AI-10-47
1H-Benzimidazole, 2-(2-pyridinyl)-6-(trifluoromethoxy)-AI-10-47 |
Others | Others |
AI-10-47 (1H-Benzimidazole, 2-(2-pyridinyl)-6-(trifluoromethoxy)-AI-10-47) 是 CBFβ-RUNX 结合的小分子抑制剂(IC50:3.2 μM)。 | |||
T38705 |
MS-PEG1-THP
MS-PEG1-THP |
||
MS-PEG1-THP is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells. | |||
T3278 |
Piribedil
EU-4200,Trivastan,ET-495,Trivastal |
Dopamine Receptor; Histone Methyltransferase; Adrenergic Receptor | Chromatin/Epigenetic; GPCR/G Protein; Neuroscience |
Piribedil (Trivastan) 是多巴胺 D2受体激动剂,对 hα1A-肾上腺素受体也显示出拮抗作用。 | |||
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。 | |||
T17088 | THP-SS-PEG1-Boc | Others | Others |
THP-SS-PEG1-Boc is a cleavable ADC linker comprising a one-unit PEG, commonly employed in the synthesis of antibody-drug conjugates (ADCs)[1]. | |||
T10384 |
Farudodstat
ASLAN003 |
Apoptosis; Dehydrogenase; DNA/RNA Synthesis | Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism |
Farudodstat (ASLAN003) 是一种具有口服活性的二氢乳清酸脱氢酶 (DHODH) 抑制剂,对人 DHODH 酶的IC50为 35 nM。它通过激活 AP-1 转录因子来抑制蛋白质合成,可以诱导凋亡,并在急性髓样白血病异种移植小鼠中大大延长其生存期。 | |||
T17089 | THP-SS-PEG1-Tos | Others | Others |
THP-SS-PEG1-Tos is a 1 unit PEG ADC linker that is cleavable. It is employed during the synthesis of antibody-drug conjugates (ADCs)[1]. | |||
T60012 |
HS-243
|
IRAK; MAPK; CDK | Cell Cycle/Checkpoint; Immunology/Inflammation; MAPK; NF-κB |
HS-243 是 IRAK-4 和 IRAK-1 的抑制剂,IC50 分别为 20 和 24 nM。 HS-243 显示出抗炎和抗癌活性。 | |||
T6019 |
Volasertib
BI 6727,伏拉塞替 |
Apoptosis; PLK | Apoptosis; Cell Cycle/Checkpoint |
Volasertib (BI 6727) 是一种具有口服活性的高效ATP 竞争性Polo 样激酶 1 抑制剂。它抑制 PLK2 和 PLK3,IC50分别为 5 和 56 nM。它是二氢蝶呤酮衍生物,有抗肿瘤活性,可诱导有丝分裂停滞和细胞凋亡。 | |||
T7162 |
R1487 Hydrochloride
R1487 (Hydrochloride) |
p38 MAPK; Autophagy | Autophagy; MAPK |
R1487 Hydrochloride (R1487(Hydrochloride)) 是一种可口服的高选择性 p38α 抑制剂,对 p38α 和 p38β 的Kd 值分别为 0.2 nM 和 29 nM。 | |||
T28072L |
MLN-3897 TFA
MLN-3897 TFA(1010731-97-1 Free base) |
CCR | Immunology/Inflammation; Microbiology/Virology |
MLN-3897 TFA 是一种有效的CCR1 拮抗剂,对 125I-MIP-1α 与 THP-1 细胞膜的结合具有抑制作用。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
T36527 |
IL-4-inhibitor-1
|
IL Receptor | Immunology/Inflammation |
IL-4-inhibitor-1 是 IL-4 的抑制剂 (EC50 = 1.81 µM)。 | |||
T60442 |
NLRP3/AIM2-IN-3
|
NOD; AIM2 | Immunology/Inflammation; NF-κB |
NLRP3/AIM2-IN-3 是一种独特的分子,能以物种特异性的方式抑制 NLRP3 和 AIM2 炎性体的激活。它对细胞裂解的 IC50 值为 0.077 ± 0.008 μ M。NLRP3/AIM2-IN-3是一种 NLRP3 和 AIM2 炎症体依赖性细胞裂解的强效抑制剂,对细胞裂解的 IC50 值为 0.077 ± 0.008 μ M。NLRP3/AIM2-IN-3 可抑制 LPS/nigericin 刺激的 THP-1 巨噬细胞的细胞裂解,其 IC50 值为 0.077 ± 0.008 μM。NLRP3/AIM2-IN-3 干扰了 NLRP3 或 AIM2 与桥接蛋白 ASC 的相互作用,抑制了 ASC 的寡聚。 | |||
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。 | |||
T68813 |
NSC-18725
|
||
NSC-18725 is a novel inhibitor of growth of intracellular Mycobacterium tuberculosis, inducing autophagy in differentiated THP-1 macrophages. | |||
T17087 |
THP-SS-alcohol
|
Others | Others |
THP-SS-alcohol is a cleavable linker employed in the synthesis of antibody-drug conjugates (ADCs)[1]. | |||
T19854 |
Evoxine
|
||
Evoxine is a selective inhibitor of CO2-induced immune suppression. It inhibits hypercapnic suppression of interleukin-6 and the chemokine CCL2 expression in human THP-1 macrophages. | |||
T18847 | THP-PEG4-Pyrrolidine(N-Me)-CH2OH | Others | Others |
THP-PEG4-Pyrrolidine(N-Me)-CH2OH, a PEG-based PROTAC linker, facilitates the synthesis of PROTAC K-Ras Degrader-1[1]. | |||
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]. | |||
T18853 |
Tos-PEG4-THP
|
Others | Others |
Tos-PEG4-THP is a polyethylene glycol (PEG) derivative utilized as a linker in the synthesis of PROTAC K-Ras Degrader-1, a potential therapeutic compound for targeted degradation of K-Ras protein [1]. | |||
T18846 |
THP-PEG4-Pyrrolidine(N-Boc)-CH2OH
|
Others | Others |
THP-PEG4-Pyrrolidine(N-Boc)-CH2OH is a polyethylene glycol (PEG) based PROteolysis TArgeting Chimera (PROTAC) linker, employed for the synthesis of PROTAC K-Ras Degrader-1, as documented in reference [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。 | |||
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... | |||
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。 | |||
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)。 | |||
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。 | |||
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。 | |||
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... | |||
T17084 |
THP-PEG6-OH
|
Others | Others |
THP-PEG6-OH is a polyethylene glycol (PEG)-based PROTAC linker, utilized in the synthesis of PROTACs[1]. It is also a non-cleavable three-unit PEG linker for antibody-drug conjugates (ADCs)[2]. | |||
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]. | |||
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。 | |||
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。 | |||
T28072 |
MLN-3897
AVE9897,AVE 9897,CCR1 antagonist 10,AVE-9897 |
CCR | Immunology/Inflammation; Microbiology/Virology |
MLN-3897 (CCR1 antagonist 10) 是一种具有口服活性的 CCR1 拮抗剂,对于 125I-MIP-1α 与 THP-1 细胞膜的结合,Ki 为 2.3 nM。 MLN-3897 抑制 Akt 信号转导和 MM 细胞存活和增殖。 | |||
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。 | |||
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。 | |||
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。 | |||
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). | |||
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。 | |||
T74803 | Levonadifloxacin | ||
Levonadifloxacin ((S)-(-)-Nadifloxacin; WCK 771),作为一种宽谱抗葡萄球菌药物,对甲氧西林敏感金黄色葡萄球菌(MSSA)及对甲氧西林耐药金黄色葡萄球菌(MRSA)显示出显著的抗菌活性,并能有效减少THP-1单核细胞对MRSA和MSSA菌株的吞噬。 | |||
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。 | |||
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) |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2P2870 |
Damascenone
trans-damascenone,Beta-Damascenone,大马烯酮,大马酮 |
Others; NF-κB; Endogenous Metabolite | Metabolism; NF-κB; Others |
Damascenone (trans-damascenone) 是一种 E-和 Z-异构体大马士革酮的混合物,源于 Epipremnum pinnatum 的具有抗炎特性的特性化合物。 | |||
T9218 |
Andrograpanin
19-HYDROXY-8(17),13-LABDADIEN-16,15-OLIDE,新穿心莲内酯苷元 |
p38 MAPK | MAPK |
Andrograpanin (19-HYDROXY-8(17),13-LABDADIEN-16,15-OLIDE) 是来自穿心莲的一种天然产物,具有抗炎和抗感染活性。 | |||
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。 | |||
TN5593 | Euphohelioscopin A | ||
Euphohelioscopin A, an activator of protein kinase C (PKC), it inhibits proliferation and induces differentiation of the myeloid leukemia cell lines THP-1 and HL-60. Euphohelioscopin A has anti-inflammary activity, it exhibits moderate inhibitory activity | |||
T72742 |
(-)-Pinocembrin
(-)-乔松素 |
||
(-)-Pinocembrin 对 H37Ra 结核分枝杆菌展示了抗菌活性,无论是休眠还是活跃期,其 IC50 值分别为1.11 mg/mL 和 1.21 mg/mL。作为一种抗增殖剂,(-)-Pinocembrin 对于 THP-1、A549、Panc-1、HeLa 和 MCF7 细胞系,IC50 值范围为 1.88 至 11.00 mg/mL。 | |||
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 。 |