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43

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
T12079 ML604440

Proteasome Proteases/Proteasome; Ubiquitination
ML604440 是一种特异性的、有效的、细胞可渗透的蛋白酶体 β1i (LMP2) 亚基抑制剂,能够破坏 MHC I 类细胞表面表达,IL-6 分泌以及 naïve T helper 向 17 T helper 细胞的分化。它可以改善实验性结肠炎和 EAE 疾病。
T5310 TR-14035

MDK-1191

Integrin Cytoskeletal Signaling
TR-14035 (MDK-1191) 是一种具有口服活性的 α4β7/α4β1整合素双重抑制剂,对 α4β7和 α4β1作用的 IC50值分别为 7 和 87 nM,可用于炎症和自体免疫疾病的研究。
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。
T80678 (S)-AK-242

(-)-Resatorvid,(S)-Resatorvid,AK-242 (S enantiomer),(-)-AK-242

Others Others
(S)-AK-242 ((S)-Resatorvid) 是一种细胞因子抑制剂,可用于治疗心脏病、自身免疫性疾病、炎症性疾病。
T4644 Tapinarof

GSK2894512,Benvitimod,苯烯莫德,WBI 1001

AhR; Aryl Hydrocarbon Receptor Immunology/Inflammation; Metabolism
Tapinarof (Benvitimod) 是一种从发光杆菌中提取的天然产物,可消除炎症。它是芳烃受体 (AhR) 激动剂,EC50为 13 nM。
T38078 TLR7/8-IN-1

TLR7/8-IN-1

TLR Immunology/Inflammation
TLR7/8-IN-1,是一种结晶态TLR7/TLR8抑制剂,对于自身免疫性疾病研究具有重要价值[1]。
T62858 hGPR91 antagonist 3

GPR Endocrinology/Hormones; GPCR/G Protein
hGPR91 antagonist 3 是一种具有口服活性、有效性和选择性的 hGPR91 拮抗剂。hGPR91 antagonist 3 可用于研究高血压、自身免疫性疾病和视网膜血管生成方面的疾病。
T78525 IRG1-IN-1

Others Others
IRG1-IN-1为衣康酸衍生物,具有抑制免疫反应基因1(IRG1)活性的能力,适用于癌症、炎症及自身免疫性疾病的研究领域。
T68043 Ciamexon

Ciamexone,BM 41332,BM41332,BM-41332

Others Others
Ciamexon (Ciamexone) 是一种新型的免疫调节剂,在自身免疫性疾病的实验模型中具有良好的效果,几乎没有显示出细胞毒性。Ciamexon 可用于研究内分泌眼病和糖尿病,在短时间给药后眼科疾病得到轻微改善。
T73695 Canakinumab

ACZ 885,Ilaris

IL Receptor Immunology/Inflammation
Canakinumab (ACZ885) 是一种重组人靶向 IL-1β 单克隆抗体。Canakinumab 显示出对人类和绒猴 IL-1β 具有抑制作用, IC50 值为分别为 43.6 和 40.8 pM。Canakinumab 具有抗炎活性,通过中和 IL-1β 信号来抑制与自身免疫性疾病相关的炎症。Canakinumab 可用于治疗痛风和冠状动脉疾病。
T3701 MCC950

CP-456773

NOD Immunology/Inflammation; NF-κB
MCC950 (CP-456773) 是NLRP3的选择性抑制剂,能够作用于BMDMs(IC50:7.5 nM) 和 HMDMs(IC50:8.1 nM)。
T39327 Amdizalisib

Amdizalisib,HMPL-689

Amdizalisib is a PI3K inhibitor and used for the research of inflammatory disease, autoimmune disease or cancer.
TP1362 Angiogenin (108-122)

Angiogenin 108-122

Angiogenin (108-122) is an angiogenin peptide. Angiogenin (108-122) acts as a therapeutic agent for the prophylaxis and/or treatment of cancer, an infectious disease, a fibrotic disease, an inflammatory disease, a neurodegenerative disease, an autoimmune
T79816 S1P1 agonist 6

LPL Receptor GPCR/G Protein
S1P1 agonist 6 (Compound I) 是一种可以通过阻断淋巴细胞迁移来减弱免疫反应的S1P1激动剂,常用于研究自身免疫性疾病的免疫抑制剂。
T10835L Cletoquine oxalate

Desethylhydroxychloroquine oxalate

Others Others
Cletoquine oxalate (Desethylhydroxychloroquine oxalate) is a major active metabolite of Hydroxychloroquine. Cletoquine has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune disea
T79094 Bromodomain inhibitor-12 (edisylate)

Epigenetic Reader Domain Chromatin/Epigenetic
Bromodomain inhibitor-12 edisylate(example 303)为bromodomain抑制剂,适用于自身免疫与炎症疾病研究。
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
TP1320 Angiogenin (108-122) TFA (112173-49-6 free base)

Angiogenin (108-122) TFA

Angiogenin (108-122) TFA is an angiogenin peptide.Angiogenin (108-122) acts as a therapeutic agent for the prophylaxis and/or treatment of cancer, an infectious disease, a fibrotic disease, an inflammatory disease, a neurodegenerative disease, an autoimmu
T70870 AC430

AC430 is a potent and specific small molecule inhibitor of janus kinase 2 (JAK2), which has been implicated as a target for therapy in both oncology and autoimmune disease. AC430 is currently being developed by Ambit. In preclinical studies, AC430 has exhibited potency against JAK2 and V617F mutated JAK2 in cell-based models that is at least equivalent to, and in most cases superior to, competing JAK2 inhibitors. In preclinical oncology and autoimmune models, AC430 is well tolerated and has sign...
T75026 PROTAC TYK2 degradation agent1

PROTACs PROTAC
PROTACTYK2 degradation agent1为亚型选择性TYK2降解剂,表现出杰出的TYK2降解活性,其DC50为14 nM,适用于自身免疫性疾病研究。
T79815 c-Fms-IN-14

c-Fms Tyrosine Kinase/Adaptors
c-Fms-IN-14 (Example 76),作为一种c-Fms抑制剂,其IC50为4 nM,主要用于癌症和自身免疫性疾病的研究。
T73262 C5aR-IN-3

C5aR-IN-3 是一种有效的 C5aR 抑制剂。C5a 水平升高与自身免疫性疾病和炎症性疾病等疾病有关。C5aR-IN-3 具有研究炎症性疾病的潜力。
T32825 L-Mevalonic acid

(S)-Mevalonic acid

Others Others
L-Mevalonic acid ((S)-Mevalonic acid) 是胆固醇的远源前体,是甲羟戊酸途径的代谢产物,可用于研究自身免疫性疾病、动脉粥样硬化和阿尔茨海默病。
T81752 MP-PEG8-Val-Lys-Gly-7-MAD-MDCPT

MP-PEG8-Val-Lys-Gly-7-MAD-MDCPT为喜树碱-接头化合物,属于抗体偶联活性分子(drug-linker conjugate for ADC)部分。该化合物在癌症及自身免疫性疾病研究中显示出研究潜力。
T76280 Dalazatide

Dalazatide (ShK-186)是一种针对Kv1.3钾通道的特异性肽抑制剂,用于研究多种自身免疫性疾病,包括多发性硬化症(MS)、红斑狼疮、银屑病、类风湿性关节炎、1型糖尿病及炎症性肠病。
T74650 JPE-1375

JPE-1375 是一种补体C5a 受体 1 (C5aR1) 拮抗剂。JPE-1375 能有效抑制小鼠体内多形核白细胞动员 (EC50=6.9 µM) 和降低TNF 水平 (EC50=4.5 µM)。JPE-1375 可用于自身免疫性和炎性疾病的研究。
T76981 Tibulizumab

Tibulizumab (LY 3090106),一种四价双特异性单克隆抗体,针对 B 细胞激活因子 (BAFF) 与IL-17A,其 Kd 值分别为 60 pM 与 14 pM。该化合物适用于自身免疫性疾病的研究。
T76935 Briakinumab

Briakinumab (ABT-874) 是一种全人抗 IL-12/23p40单克隆抗体。Briakinumab 靶向并中和 IL-12和 IL-23。Briakinumab 可用于类风湿性关节炎、炎症性肠病和多发性硬化症的研究。
T76280L Dalazatide TFA

Dalazatide (ShK-186) TFA 是特异性 Kv1.3 钾通道肽抑制剂,适用于研究多发性硬化症 (MS)、红斑狼疮、银屑病、类风湿性关节炎、1型糖尿病及炎症性肠病等自身免疫性疾病。
T73115 (S)-HH2853

(S)-HH2853 是一种 PYRIDINO 五元芳环化合物,一种有效的 EZH1/2双重抑制剂,对 EZH2_Y641F 的IC50为 <100 nM。(S)-HH2853有潜力用于抗肿瘤或自身免疫性疾病的研究。
T39129 BMS-986143

BMS-986143 是一种口服有效的、可逆的BTK 抑制剂,IC50为 0.26 nM,具有自身免疫性疾病的研究潜力。BMS-986143 还抑制 TEC、BLK、BMX、TXK FGR、YES1、ITK,IC50分别为 3 nM、5 nM、7 nM、10 nM、15 nM、19 nM、21 nM。
T70899 Vidofludimus hemicalcium

4sc-101 hemicalcium,SC12267 hemicalcium,4sc-101 hemicalcium ; SC12267 hemicalcium

Vidofludimus (4sc-101 ; SC12267) hemicalcium 是一种口服有效的二氢乳清酸脱氢酶 (DHODH) 的抑制剂,也是法尼醇 X 受体 (FXR) 调节剂。Vidofludimus hemicalcium 作为一种免疫调节剂,可用于研究自身免疫性疾病,如炎症性肠病 (IBD)。Vidofludimus hemicalcium 还可通过靶向FXR 用于脂肪肝的研究。
T60909 SSAO inhibitor-3

SSAO inhibitor-3 (Compound 2) 可用于研究动脉粥样硬化、糖尿病及其并发症、肥胖症、中风、慢性肾病、视网膜病变、慢性阻塞性肺病 (COPD)、自身免疫性疾病、多发性硬化等。SSAO inhibitor-3 是一种氨基脲敏感性胺氧化酶 (SSAO) 的抑制剂,对人 AOC1 和SSAO 的IC50分别为 0.1-10 μM 和 <10 nM 。
T60640 SSAO inhibitor-2

SSAO inhibitor-2 (Compound 1) 可用于动脉粥样硬化、糖尿病及其并发症、肥胖、中风、慢性肾病、视网膜病变、慢性阻塞性肺病 (COPD)、自身免疫性疾病、多发性硬化等的研究。SSAO inhibitor-2 是氨基脲敏感性胺氧化酶 (SSAO) 抑制剂,其对人 SSAO 和 MAO-A 的IC50分别为 <10 nM 和 10-100 μM。
T37554 Oleyl Anilide

AcylCoA:cholesterol acyltransferase (ACAT) is an intracellular cholesteryl ester synthase tied closely to the absorption of dietary cholesterol. Oleyl analide (OA) is a weak inhibitor of acylCoA:cholesterol acyltransferase (ACAT) with an IC50 of 26 μM. OA and the related glyceride dioleoyl phenylamino propane 1,2-diol have been linked to a syndrome of eosinophilia, excessive T-cell activation, and elevated interleukin-4 (IL-4), soluble IL-2R, and IL-5. The clinical consequences are an acute pulm...
T72017 6(5H)-Phenanthridinone

6(5H)-Phenanthridinone is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2. It decreases radiation-induced PARP activity and proliferation of RDM4 murine lymphoma cells. 6(5H)-Phenanthridinone reduces NF-κB-induced transcription of the genes encoding TNF-α, IL-2, and IFN-γ in rat lymphocytes. In vivo, 6(5H)-phenanthridinone reduces spinal cord expression of inducible nitric oxide synthase (iNOS), IL-1β, TNF-α, IL-2, and IFN-γ and reduces disease score in a rat model of experimenta...
T36486 Benpyrine

Benpyrine is a highly specific and orally active TNF-α inhibitor with a KD value of 82.1 μM. Benpyrine tightly binds to TNF-α and blocks its interaction with TNFR1, with an IC50 value of 0.109 μM. Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research[1]. Benpyrine (5-20 μM; 14 hours; RAW264.7 cells) pretreatment results in a dose-dependent decrease in the phosphorylation of IκBα in RAW264.7 cells (stimulated with 10 ng/mL TNF-α or 1 μg/mL LPS). Benpyrine abo...
T80973 TNF-α-IN-8

TNF-α-IN-8 (compound I-42) 作为一种TNF-α抑制剂,属于异吲哚-亚胺类化合物,适用于肿瘤、心脏病、骨质疏松、炎症、过敏及自身免疫性疾病的研究。作为点击化学试剂,其Azide基团能与含Alkyne的分子配对,通过铜催化的叠氮-炔环加成反应(CuAAc)产生反应,也可与含DBCO或BCN基团的分子进行菌株促进的炔-叠氮环加成反应(SPAAC)。
T69600 Spermidine-d6

Spermidine-d6 is intended for use as an internal standard for the quantification of spermidine by GC- or LC-MS. Spermidine is an endogenous polyamine. It is formed from putrescine by spermidine synthase. Spermidine (25 µM) inhibits the activity of the human inward-rectifying potassium channel Kir2.3 in a patch-clamp assay. It induces autophagy in HeLa cells when used at a concentration of 100 µM and increases the lifespan of D. melanogaster, yeast, and C. elegans. Spermidine (30 mM in the drinki...
T82907 BDC2.5 Mimotope 1040-63

BDC2.5 Mimotope 1040-63是具有生物活性的肽,广泛应用于1型糖尿病(T1D)研究中的TCR转基因模型(BDC2.5)模拟表位。T1D是一种涉及自身免疫系统对胰岛β细胞的T细胞介导损害的自身免疫性疾病。BDC2.5模拟表位在研究胰岛素产生细胞遭到自身反应性T细胞破坏的过程中,对支持抗原肽实现向胰岛自身抗原特异性T细胞的抗原呈递具有重要作用。
T81609 omega-3 Arachidonic acid ethyl ester

(all-Z)-8,11,14,17-Eicosatetraenoic acid ethyl ester,ω-3 Arachidonic acid ethyl ester

omega-3 Arachidonic Acid ethyl ester 是一种少见的多不饱和脂肪酸,饮食来源稀少。ω-3脂肪酸对婴幼儿生长发育极为重要,能够帮助预防心脏病、血栓、高血压及炎症和自身免疫性疾病。该化合物在人血小板膜中通过抑制花生四烯酰辅酶A合成酶发挥作用,Ki值达到14 μM;同时在小牛脑提取物中也表现出抑制作用,IC50大约5 μM。omega-3 Arachidonic Acid ethyl ester 作为游离酸的亲脂性更强的形式,具备独特的生物活性。
T37419 Zetomipzomib

KZR-616, a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. KZR-616 has the potential for the research of multiple autoimmune diseases[1][2]. KZR-616 also inhibits MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=688 nM). KZR-616 maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells. KZR-616 (250 nM) shows a comparable cytokine inhib...
T36578 Boc-Lys(Ac)-AMC

Commendamide (N-acyl-3-hydroxypalmitoyl-glycine) is a newly discovered GPCR G2A/GPR132 agonist (EC50=11.8 μM) that isolated from Bacteroides vulgatus. [1] G2A/GPR132 belongs to the guanine nucleotide-binding protein (G protein)-coupled receptor (GPCR) superfamily. GPR132/G2A is first reported to be a transcriptional target for BCR-ABL tyrosine kinase attenuating B-cell expansion in vitro and arresting cells at G2 during mitosis. It has been involved in autoimmune disease and atherosclerosis. [1]...

化合物

ML604440
Cat.No: T12079
Synonym:
Target: Proteasome
TR-14035
Cat.No: T5310
Synonym: MDK-1191
Target: Integrin
HS-243
Cat.No: T60012
Synonym:
Target: IRAK, MAPK, CDK
(S)-AK-242
Cat.No: T80678
Synonym: (-)-Resatorvid,(S)-Resatorvid,AK-242 (S enantiomer),(-)-AK-242
Target: Others
Tapinarof
Cat.No: T4644
Synonym: GSK2894512,Benvitimod,苯烯莫德,WBI 1001
Target: AhR, Aryl Hydrocarbon Receptor
TLR7/8-IN-1
Cat.No: T38078
Synonym: TLR7/8-IN-1
Target: TLR
hGPR91 antagonist 3
Cat.No: T62858
Synonym:
Target: GPR
IRG1-IN-1
Cat.No: T78525
Synonym:
Target: Others
Ciamexon
Cat.No: T68043
Synonym: Ciamexone,BM 41332,BM41332,BM-41332
Target: Others
Canakinumab
Cat.No: T73695
Synonym: ACZ 885,Ilaris
Target: IL Receptor
MCC950
Cat.No: T3701
Synonym: CP-456773
Target: NOD
Amdizalisib
Cat.No: T39327
Synonym: Amdizalisib,HMPL-689
Target:
Angiogenin (108-122)
Cat.No: TP1362
Synonym: Angiogenin 108-122
Target:
S1P1 agonist 6
Cat.No: T79816
Synonym:
Target: LPL Receptor
Cletoquine oxalate
Cat.No: T10835L
Synonym: Desethylhydroxychloroquine oxalate
Target: Others
Bromodomain inhibitor-12 (edisylate)
Cat.No: T79094
Synonym:
Target: Epigenetic Reader Domain
ARN-6039
Cat.No: T25109
Synonym: ARN 6039,ARN6039
Target:
Angiogenin (108-122) TFA (112173-49-6 free base)
Cat.No: TP1320
Synonym: Angiogenin (108-122) TFA
Target:
AC430
Cat.No: T70870
Synonym:
Target:
PROTAC TYK2 degradation agent1
Cat.No: T75026
Synonym:
Target: PROTACs
c-Fms-IN-14
Cat.No: T79815
Synonym:
Target: c-Fms
C5aR-IN-3
Cat.No: T73262
Synonym:
Target:
L-Mevalonic acid
Cat.No: T32825
Synonym: (S)-Mevalonic acid
Target: Others
MP-PEG8-Val-Lys-Gly-7-MAD-MDCPT
Cat.No: T81752
Synonym:
Target:
Dalazatide
Cat.No: T76280
Synonym:
Target:
JPE-1375
Cat.No: T74650
Synonym:
Target:
Tibulizumab
Cat.No: T76981
Synonym:
Target:
Briakinumab
Cat.No: T76935
Synonym:
Target:
Dalazatide TFA
Cat.No: T76280L
Synonym:
Target:
(S)-HH2853
Cat.No: T73115
Synonym:
Target:
BMS-986143
Cat.No: T39129
Synonym:
Target:
Vidofludimus hemicalcium
Cat.No: T70899
Synonym: 4sc-101 hemicalcium,SC12267 hemicalcium,4sc-101 hemicalcium ; SC12267 hemicalcium
Target:
SSAO inhibitor-3
Cat.No: T60909
Synonym:
Target:
SSAO inhibitor-2
Cat.No: T60640
Synonym:
Target:
Oleyl Anilide
Cat.No: T37554
Synonym:
Target:
6(5H)-Phenanthridinone
Cat.No: T72017
Synonym:
Target:
Benpyrine
Cat.No: T36486
Synonym:
Target:
TNF-α-IN-8
Cat.No: T80973
Synonym:
Target:
Spermidine-d6
Cat.No: T69600
Synonym:
Target:
BDC2.5 Mimotope 1040-63
Cat.No: T82907
Synonym:
Target:
omega-3 Arachidonic acid ethyl ester
Cat.No: T81609
Synonym: (all-Z)-8,11,14,17-Eicosatetraenoic acid ethyl ester,ω-3 Arachidonic acid ethyl ester
Target:
Zetomipzomib
Cat.No: T37419
Synonym:
Target:
Boc-Lys(Ac)-AMC
Cat.No: T36578
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T10835 Cletoquine

Desethylhydroxychloroquine

Parasite; Antifection Microbiology/Virology
Cletoquine 是 Hydroxychloroquine 的主要活性代谢物。 Cletoquine 具有对抗基孔肯雅病毒 (CHIKV) 的能力。 Cletoquine 具有抗疟作用,并具有治疗自身免疫性疾病的潜力。
T3877 Esculentoside A

NF-κB; COX Immunology/Inflammation; Neuroscience; NF-κB
Esculentoside A 是一种三萜皂苷,从商陆根部分离得到。它在具有抗炎活性,对环氧合酶-2 具有选择性抑制活性。它通过抑制NF-κB 和丝裂原活化蛋白激酶信号通路抑制 LPS 诱导的急性肺损伤中的炎症反应。

天然产物

Cletoquine
Cat.No: T10835
Synonym: Desethylhydroxychloroquine
Target: Parasite, Antifection
Esculentoside A
Cat.No: T3877
Synonym:
Target: NF-κB, COX
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