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31

抑制剂 & 化合物

3

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。
T4031	S1p receptor agonist 1 S1p-receptor-agonist-1	S1P Receptor; LPL Receptor	GPCR/G Protein
	S1p receptor agonist 1 (S1p-receptor-agonist-1) 是有口服活性的S1P 受体激动剂，具有诱导 S1P1 内化的活性，EC50为9.83 nM。它有潜力用于关节炎和实验性自身免疫性脑炎)的相关研究。
T35438	(5E)-7-Oxozeaenol
	(5E)-7-Oxozeaenol is a resorcylic acid lactone that has been found in the fungus MSX 63935 and has enzyme inhibitory and anticancer activities.1,2 It inhibits TGF-β-activated kinase 1 (TAK-1; IC50 = 1.3 μM).1 (5E)-7-Oxozeaenol inhibits proliferation of MCF-7, H460, SF-268, HT-29, and MDA-MB-435 human cancer cells with IC50 values of 4.9, 1.2, 5.6, 4.4, and 5.5 μM, respectively.2 \|1. Fakhouri, L., El-Elimat, T., Hurst, D.P., et al. Isolation, semisynthesis, covalent docking and transforming growt...
T76200	STIEEQAKTFLDKFNHEAEDLFYQSSLASWN
	STIEEQAKTFLDKFNHEAEDLFYQSSLASWN 是与血管紧张素转换酶 2 (ACE2) 相关的肽，适用于研究 ACE2 功能。
T14924	Cenerimod ACT-334441	S1P Receptor	GPCR/G Protein
	Cenerimod (ACT-334441) 是一种具有口服活性、选择性和高效性的磷酸鞘氨醇 1 受体（S1P1）激动剂（EC50：1 nM）。Cenerimod 对多种 S1P 的亚型具有抑制作用，可用于研究鼠类实验性自身免疫性脑脊髓炎 (EAE)和鼠类硬皮病。
T33514	MSC 2032964A MSC-2032964A,MSC2032964A	ASK	Apoptosis
	MSC 2032964A 是一种有效的选择性 ASK1 抑制剂 (IC50 = 93 nM)，具有口服生物利用度和脑渗透性。它在小鼠 EAE 模型中抑制神经炎症，并在培养的小鼠星形胶质细胞中阻断 LPS 诱导的 ASK1 和 p38 磷酸化。
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)。
T7657L	MOG peptide (35-55) , mouse, rat acetate Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat acetate,MOG peptide (35-55) , mouse, rat acetate (149635-73-4 Free base)	Others	Others
	Myelin Oligodendrocyte Glycoprotein (MOG) peptide (35-55) , mouse, rat acetate 是MOG peptide (35-55)衍生物。 MOG peptide (35-55)是髓鞘少突胶质细胞糖蛋白 (MOG) 免疫原肽的一部分。MOG peptide (35-55) 特异性作用于 CD4+ T 细胞，能够给诱导实验性自身免疫性脑脊髓炎 (EAE) 动物模型。MOG peptide (35-55) , mouse, rat acetate(149635-73-4 Free base)是MOG peptide (35-55)衍生物。 MOG peptide (35-55)是髓鞘少突胶质细胞糖蛋白 (MOG) 免疫原肽的一部分，可用于研究与免疫相关的疾病。
T82424	Experimental allergic encephalitogenic peptide (human)
	Experimental allergic encephalitogenic peptide (human) 为EAE多肽类化合物，能够诱导豚鼠发生脑脊髓炎。
T30529	BMS-520
	BMS-520 is a potent, selective S1P1 agonist that has shown impressive efficacy when administered orally in a rat model of arthritis and in a mouse model of experimental autoimmune encephalomyelitis (EAE) with multiple sclerosis.
T78031	MOG peptide (35-55)
	MOG peptide (35-55) 是一段特定的髓鞘少突胶质细胞糖蛋白 (MOG) 免疫原肽的35至55氨基酸序列。该肽段具有针对CD4+T细胞的特异性活性，并可用于诱导实验性自身免疫性脑脊髓炎 (EAE) 的动物模型。
TP1282	PLP (139-151) PLP 139-151
	PLP (139-151) is amino acid residue residue 139 to 151 of myelin proteolipid protein (PLP). This peptide is used to induce relapsing-remitting (RR)-EAE model.
T63206	SR12418
	SR12418 是一种特异性的 REV-ERB 合成配体，能够作用于 REV-ERBα (IC50: 68 nM) 和 REV-ERBβ (IC50: 119 nM)，可用于研究实验性自身免疫性脑脊髓炎 (EAE) 和结肠炎。
T81734	Myelin Basic Protein (1-11)
	Myelin Basic Protein (1-11) 是髓鞘碱性蛋白 (MBP) 的一个致脑炎表位，并且常用于诱导实验性自身免疫性脑脊髓炎 (EAE)。
T69066	Forphenicine
	Forphenicine is a bacterial metabolite that has been found in S. fulvoviridis and an inhibitor of alkaline phosphatase (IC50 = 0.036 µg/ml for the chicken intestine enzyme). It inhibits the growth of HL-60 leukemia cells when used at a concentration of 10 µM. Forphenicine (50 and 500 µg/animal) increases survival in a guinea pig model of experimental autoimmune encephalomyelitis (EAE).
T82621	D359-0396	NOD-like Receptor (NLR)	Immunology/Inflammation
	D359-0396 是一种口服活性的 NLRP3 炎性体抑制剂，能有效抑制巨噬细胞焦亡（pyroptosis）以及 IL-1β 的释放，并阻止 NLRP3 和 ASC 的寡聚化，抑制 GSDMD 的裂解。该化合物在动物模型中能减轻小鼠的 EAE 症状，并提高感染性休克后的小鼠存活率。
T82020	J5 peptide Myelin basic protein (85-99) antagonist
	J5 peptide是MBP抑制剂，竞争性阻断MBP85-99与HLA-DR2的结合。该肽段能减轻PLP139-151/MBP85-99诱导的小鼠实验性自身免疫性脑脊髓炎(EAE)。J5 peptide主要用于研究炎症和免疫疾病。
T68408	AMG-1
	AMG-1 is a specific CRAC channel inhibitor. AMG-1 blocks the function of effector T cells, but not regulatory T cells in vitro and it attenuates the progression and severity of EAE in vivo.
T73336	Ketotifen 酮替芬,HC 20-511
	Ketotifen (HC 20-511)为第二代口服活性非竞争性组胺1(H1)受体阻滞剂兼肥大细胞稳定剂，能体外阻断6-磷酸葡萄糖酸脱氢酶(6-PGD)。其对SARS-CoV-2及流感病毒(Influenza virus)展现出抗病毒活性，适用于自身免疫性脑脊髓炎(EAE)与哮喘发作预防研究。
T39110	MOG (35-55), human
	MOG (35-55), human, a constituent of central nervous system myelin, is distinguishable from mMOG (35-55) due to a proline-to-serine substitution at position 42. It possesses immunogenic properties and is partially cross-reactive with mMOG35–55. However, MOG (35-55), human does not induce encephalitogenic effects, and only elicits minimal clinical signs of EAE (experimental autoimmune encephalomyelitis) in comparison to the rodent peptide.
T80682	γ-Fibrinogen 377-395 TFA
	γ-Fibrinogen377-395 TFA 是纤维蛋白原衍生抑制肽，具有纤维蛋白原表位特性。该化合物能在体外抑制小胶质细胞激活、阻断纤维蛋白与Mac-1相互作用，并在小鼠体内抑制实验性自身免疫性脑脊髓炎(EAE)。该肽适用于多发性硬化症(MS)及其他血脑屏障损伤和小胶质细胞激活相关的神经炎症疾病研究。
T65390	Fluvoxketone
	Fluvoxketone is trifluoromethyl-substituted aryl ketone compound useful as an intermediate in the synthesis of Fluvoxamine, which is a selective serotonin reuptake inhibitor. In the synthesis of Fluvoxamine, the ketone carbonyl of Fluvoxketone is elaborated to an oxime.In vitro，the inhibitory effect of fluvoxamine on actin polymerization was concentration dependent, and its IC50 was approximately 30 μM.In vivo，fluvoxamine treated EAE rats showed a decrease in IFN-γ serum levels and an increase i...
T80683	γ-Fibrinogen 377-395
	γ-Fibrinogen377-395是一种衍自纤维蛋白原的抑制性肽段，也被认为是纤维蛋白原的表位之一。它能在体外抑制小胶质细胞的激活并阻断纤维蛋白与Mac-1的交互作用；此外，在小鼠体内能够抑制实验性自身免疫性脑脊髓炎(EAE)的发展。因此，γ-Fibrinogen377-395对于多发性硬化症(MS)以及其他与血脑屏障损伤和小胶质细胞活化相关的神经炎症性疾病的研究具有潜在的应用价值。
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...
T83690	[Leu144, Arg147]-PLP (139-151) TFA [Leu144, Arg147] Proteolipid Peptide (139-151),H-His-Ser-Leu-Gly-Lys-Leu-Leu-Gly-Arg-Pro-Asp-Lys-Phe-OH
	[Leu144,Arg147]-PLP (139-151)是髓鞘脂蛋白(PLP)的一种突变肽段，包含位于144和147位置的色氨酸到亮氨酸以及组氨酸到精氨酸的替换。使用[Leu144, Arg147]-PLP (139-151)（50 µg）乳化于完全弗氏佐剂(CFA)免疫后，能增加小鼠脾脏中的IL-4水平。它在体外抑制Th1细胞激活，但在体内不抑制，其中它诱导调节性T细胞的产生。用[Leu144, Arg147]-PLP (139-151)预免疫可以延迟由脑炎肽PLP (178-191)、髓磷脂少突细胞蛋白(MOG) (92-106)或髓鞘基础蛋白(MBP)在小鼠中诱导的实验性自身免疫性脑炎(EAE)的发病。
T36015	PDMP (hydrochloride)
	PDMP is a ceramide analog first prepared in a search for inhibitors of glucosylceramide synthase. PDMP has two adjacent chiral centers (C1 and C2) allowing for the formation of four possible isomers. PDMP contains all four of these stereoisomers. PDMP inhibits glucosylceramide synthase by 90% when used at a concentration of 0.8 μM in MDCK cell homogenates, however, the ability to inhibit glucosylceramide synthase has been found to reside in the D-threo (1R,2R) enantiomer. The D-threo PDMP enanti...
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...
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。
T83688	R 715 TFA [Ac-Lys-[D-βNal7,Ile8]des-Arg9]-BK,Ac-Lys-Arg-Pro-Pro-Gly-Phe-Ser-D2Nal-Ile-OH
	R 715是一种布拉迪肾上腺素B1受体拮抗剂。它抑制在表达布拉迪肾上腺素B1受体的孤立人类脐带中由布拉迪肾上腺素引发的收缩（pA2 = 8.49）。R 715（200、400及600 µg/kg）通过尾部闪烁测试减少了由链脲佐菌素（STZ）诱导的糖尿病神经病变小鼠模型中尾部撤回的潜伏期。它还在以髓磷脂少突胶质细胞糖蛋白（MOG）（35-55）（MOG35-55）抗原肽诱导的实验性自体免疫性脑炎（EAE）小鼠模型中，通过每天1 mg/kg的剂量减少了后肢无力和瘫痪的发病率，改善对称步态，并减少脊髓炎症灶点数、神经元脱髓鞘以及病灶单核细胞侵袭。R 715（0.01 nmol/动物，脑室内）能在自发性高血压大鼠中降低平均动脉血压并增加心率。
T36296	BIO5192 hydrate
	BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels[1][2]. The combination of BIO5192 hydrate (1 mg/kg; i.v.) and Plerixafor (5 mg/kg; s.c.) exert an additive effect on progenitor mobilization[1].BIO5192 hydrate (30 mg/kg; s.c; bid; during days...
T38106	JC-171
	JC-171 is a selective NLRP3 inflammasome inhibitor, with an IC50 of 8.45 μM for inhibiting LPS/ATP-induced interleukin-1β (IL-1β) release from J774A.1 macrophages[1]. JC-171 (0-100 μM) blocks NLRP3 inflammasome activation and IL-1β production in primary macrophages dose dependently[1]. ...

化合物

Cat.No: T12079

Target: Proteasome

S1p receptor agonist 1

Cat.No: T4031

Synonym: S1p-receptor-agonist-1

Target: S1P Receptor, LPL Receptor

(5E)-7-Oxozeaenol

Cat.No: T35438

STIEEQAKTFLDKFNHEAEDLFYQSSLASWN

Cat.No: T76200

Cat.No: T14924

Synonym: ACT-334441

Target: S1P Receptor

Cat.No: T33514

Synonym: MSC-2032964A,MSC2032964A

Target: ASK

Cat.No: T3701

Synonym: CP-456773

Target: NOD

MOG peptide (35-55) , mouse, rat acetate

Cat.No: T7657L

Synonym: Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat acetate,MOG peptide (35-55) , mouse, rat acetate (149635-73-4 Free base)

Target: Others

Experimental allergic encephalitogenic peptide (human)

Cat.No: T82424

Cat.No: T30529

MOG peptide (35-55)

Cat.No: T78031

Cat.No: TP1282

Synonym: PLP 139-151

Cat.No: T63206

Myelin Basic Protein (1-11)

Cat.No: T81734

Cat.No: T69066

Cat.No: T82621

Target: NOD-like Receptor (NLR)

Cat.No: T82020

Synonym: Myelin basic protein (85-99) antagonist

Cat.No: T68408

Cat.No: T73336

Synonym: 酮替芬,HC 20-511

MOG (35-55), human

Cat.No: T39110

γ-Fibrinogen 377-395 TFA

Cat.No: T80682

Cat.No: T65390

γ-Fibrinogen 377-395

Cat.No: T80683

6(5H)-Phenanthridinone

Cat.No: T72017

[Leu144, Arg147]-PLP (139-151) TFA

Cat.No: T83690

Synonym: [Leu144, Arg147] Proteolipid Peptide (139-151),H-His-Ser-Leu-Gly-Lys-Leu-Leu-Gly-Arg-Pro-Asp-Lys-Phe-OH

PDMP (hydrochloride)

Cat.No: T36015

Cat.No: T69600

Cat.No: T83910

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

Cat.No: T83688

Synonym: [Ac-Lys-[D-βNal7,Ile8]des-Arg9]-BK,Ac-Lys-Arg-Pro-Pro-Gly-Phe-Ser-D2Nal-Ile-OH

BIO5192 hydrate

Cat.No: T36296

Cat.No: T38106

Cat. No.	Product Name	Target	Signaling Pathways
T14055	5Z-7-Oxozeaenol FR148083,L783279,LL-Z 1640-2	VEGFR; FLT; MEK; MAPK; PDGFR; Antibiotic; Src	Angiogenesis; MAPK; Microbiology/Virology; Tyrosine Kinase/Adaptors
	5Z-7-Oxozeaenol (FR148083) 是一种天然抗原生动物抑制剂，不可逆的选择性抑制 TAK1和 VEGF-R2，IC50值分别为 8 nM 和 52 nM。
T3426	Bacoside A	MMP; Others; TNF; Dopamine Receptor; NOS; ROS	Apoptosis; GPCR/G Protein; Immunology/Inflammation; Neuroscience; Others; Proteases/Proteasome
	Bacoside A has a possible anticancer activity that could be inducing cell cycle arrest and apoptosis through Notch pathway in GBM in vitro. It exerts cytoprotective efficacy by attenuation of ROS generated through oxidative stress by an increase in the concentration of antioxidant enzymes and sustain membrane integrity which leads to restoring the damage caused by tBHP. Bacoside A can able to inhibit the progression of Experimental Autoimmune Encephalomyelitis (EAE) may be by the inhibition of i...
T78492	D-Mannuronic acid sodium
	D-Mannuronic acid sodium，一种可从Macrocystis pyrifera中分离得到的化合物，显示出在自身免疫性脑脊髓炎(EAE)、佐剂性关节炎(AIA)、肾病综合征以及急性肾小球肾炎的研究中具有潜在应用价值。

天然产物

5Z-7-Oxozeaenol

Cat.No: T14055

Synonym: FR148083,L783279,LL-Z 1640-2

Target: VEGFR, FLT, MEK, MAPK, PDGFR, Antibiotic, Src

Cat.No: T3426

Target: MMP, Others, TNF, Dopamine Receptor, NOS, ROS

D-Mannuronic acid sodium

Cat.No: T78492

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