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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
T9020	GSK620	Epigenetic Reader Domain	Chromatin/Epigenetic
	GSK620 是一种有口服活性的泛BD2抑制剂，在人全血中表现出抗炎表型，有良好的广谱选择性、可开发性和体内口服药代动力学。它对 BET-BD2 家族蛋白具有高度选择性，其选择性超过所有其他 BET 溴结构域 200 倍以上。
T3144	BML-284 Wnt agonist 1	Wnt/beta-catenin	Cytoskeletal Signaling; Stem Cells
	BML-284 (Wnt agonist 1) 是细胞通透性 Wnt 信号激活剂，能够诱导 TCF 依赖的转录活性(EC50>700 nM)。
T3206	NKL 22 Histone Deacetylase Inhibitor IV,PAOA	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	NKL 22 (Histone Deacetylase Inhibitor IV) 是一种有效的选择性组蛋白脱乙酰基酶(HDAC) 抑制剂，对 HDAC2/4/5/7/8 具有选择性，抑制HDAC1和HDAC3的IC50值分别为 199 和 69 nM。它可改善亨廷顿氏病转基因小鼠的疾病表型和转录异常。
T8820	BML-284 hydrochloride BML-284 HCL,Wnt agonist 1 HCL	Wnt/beta-catenin	Cytoskeletal Signaling; Stem Cells
	BML-284 hydrochloride (Wnt agonist 1 HCL) 是细胞通透性 Wnt 信号激活剂。它能够诱导 TCF 依赖的转录活性(EC50>700 nM)。
T22276	Bis(maltolato)oxovanadium(IV) 双(麦芽醇)氧钒(IV),BMOV,Bis maltolato oxovanadium,Bis(maltolato)oxovanadium (IV),bis maltolato oxo vanadium,Bis(maltolato)oxovanadium (IV)	Phosphatase; Others	Metabolism; Others
	Bis(maltolato)oxovanadium(IV) (BMOV) 是一种有效的胰岛素增敏剂，也是一种有效的、竞争性的、可逆的、口服具有活性的光谱蛋白酪氨酸磷酸酶 (PTP) 抑制剂。它抑制HCPTPA，PTP1B，HPTPβ和SHP2的IC50分别为 126 nM，109 nM，26 nM 和 201 nM。
T15168	DRF-1042	Others	Others
	DRF-1042 acts to inhibit DNA topoisomerase I. DRF-1042 displays perfect anticancer activity against a panel of human cancer cell lines including multi-drug resistance (MDR) phenotype.
T5170	KHS101 hydrochloride 盐酸KHS101	FGFR; Microtubule Associated	Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	KHS101 hydrochloride 能够选择性的诱导神经元分化表型，能够与转化酸性含螺旋蛋白发生相互作用。
T77379	Bexmarilimab FP-1305	Others	Others
	Bexmarilimab (FP-1305) 是一种高效的人源化抗 CLEVER-1 IgG4 抗体，其 IC50 值为 4.51 nM。Bexmarilimab 能够促使肿瘤相关巨噬细胞表型 M2 到 M1 的免疫转换。Bexmarilimab 可用于研究癌症。
T63049	CHD1Li 6.11	Others	Others
	CHD1Li 6.11 是一种致癌 CHD1L 的有效抑制剂，能够作用于 cat-CHD1L 重组蛋白 (IC50: 3.3 μM)。CHD1Li 6.11 是一种口服具有活力的抗肿瘤剂，明显减少由分离的准间充质细胞 (M 表型) 产生的 CRC 异种移植物的肿瘤体积，这些细胞具有增强的致瘤特性。
T9682	AZD-4877 AZD4877	Apoptosis; Kinesin	Apoptosis; Cytoskeletal Signaling
	AZD-4877 是一种高效的纺锤体驱动蛋白 (Eg5) 抑制剂，对其 IC50 值为 2 nM。 AZD-4877 是 Ispinesib 的另一种构型，能够抑制细胞有丝分裂，诱导形成单极纺锤体表型，介导细胞凋亡(Apoptosis)。 AZD-4877 具有抗肿瘤活性，对循环外周血单核细胞 (PBMC)有抑制作用。
T11134	DZ2002	Others	Others
	DZ2002 是一种口服有效的、可逆的、低细胞毒性的 III 型 SAHH 抑制剂 (Ki=17.9 nM)，具有较好的免疫抑制活性。DZ2002 能通过逆转各种细胞类型的促纤维化表型来防止实验性皮肤纤维化的发展。DZ2002 可用于自身免疫性疾病，如狼疮综合征和系统性硬化症的研究。
T27537	Hexafluoro
	Hexafluoro is an inhibitor of DRP1 phosphorylation. Honokiol DCA stimulates a phenotype suggestive of respiration through mitochondrial normalization and demonstrates activity in Vemurafenib-resistant melanoma in vivo.
T27551	Honokiol DCA Honokiol Bis-Dichloroacetate
	Honokiol DCA is an inhibitor of DRP1 phosphorylation. Honokiol DCA stimulates a phenotype suggestive of respiration through mitochondrial normalization and demonstrating activity in Vemurafenib-resistant melanoma in vivo.
T70367	SNU-BP
	SNU-BP is an agonist of PPAR-gamma, inhibiting lipopolysaccharide (LPS)-induced NO production and pro-inflammatory cytokines. SNU-BP potentiates interleukin-4-induced arginase-1 expression, and promotes microglial polarization toward an M2 anti-inflammatory phenotype.
T68582	Tonantzitlolone
	Tonantzitlolone is a natural agonist of tprc1/4/5 channels, also acting as a dual pkcα and pkcθ activator, inducing an insulin resistant phenotype by inhibiting irs1 and the pi3k/akt pathway, activating the heat shock factor 1 (hsf1) transcription factor driving glucose dependency
T38502	IGF-1R inhibitor-2
	IGF-1R inhibitor-2 (example 121) is a compound that inhibits the insulin-like growth factor-1 receptor (IGF-1R). By downregulating the IGF-1R, it has the potential to reverse the transformed phenotype of tumor cells and make them more susceptible to apoptosis.
T79590	Anti-neuroinflammation agent 1	NOD-like Receptor (NLR)	Immunology/Inflammation
	Anti-neuroinflammation agent 1 为一种效力显著的抗神经炎症药物，能有效调节BV2小胶质细胞从M1表型向M2表型极化。
T21317	Avanbulin BAL27862,BAL-27862,BAL 27862
	Avanbulin is a potent inhibitor of tubulin polymerization with antitumor activity. It elicits a unique microtubule (MT) phenotype, distinct from colchicine, paclitaxel, and vinblastine has broad in vitro anti-proliferative activity against a diverse range
T69782	GS-9822
	GS-9822 is a novel LEDGIN, an inhibitor that targets the binding pocket of LEDGF/p75 which is a cellular cofactor that substantially contributes to HIV integration site selection, displaying a block-and-lock phenotype in cell culture.
T72430	L-Kynurenine sulfate
	L-Kynurenine sulfate 是一种芳香烃受体AHR 激动剂，可激活 AHR 导向的初始T 细胞极化至抗炎 Treg 表型。
T40099	ALV2
	ALV2 is a potent and selective Helios degrader compound that binds to the CRBN protein, exhibiting an IC50 value of 0.57 μM. Helios, a zinc-finger transcription factor, plays a crucial role in preserving a stable T reg cell phenotype within the inflammatory tumor microenvironment.
T68737	XR9051
	XR9051 is as a potent modulator of P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) following a synthetic chemistry programme based on a natural product lead compound. XR9051 was shown to be a potent inhibitor of the binding of the cytotoxic to P-glycoprotein (EC50 = 1.4 +/- 0.5 nM). XR9051 reverses the MDR phenotype through direct interaction with P-glycoprotein.
T61072	ERD03
	ERD03 是EXOSC3–RNA 相互作用的强效破坏剂，其Kd 值为 17±7 μM。ERD03 诱导斑马鱼胚胎 PCH1B 样表型，可用于脑神经失调的研究。
T79184	FKBP51F67V-selective antagonist Ligand2	FKBP	Apoptosis; Autophagy; Immunology/Inflammation
	FKBP51F67V-selective antagonist Ligand2（示例3-3）是针对杏仁核中由FKBP51 F67V过表达引起的焦虑表型的有效逆转剂。本物质特异性地结合到FKBP51 F67V，与野生型FKBP51及FKBP52无亲和力。
T68227	BMS-214662 HCl
	BMS-214662 is a Farnesyltransferase inhibitor , is also a nonsedating benzodiazepine derivative with potential antineoplastic activity. BMS-214662 inhibits the enzyme farnesyltransferase and the post-translational farnesylation of number of proteins involved in signal transduction, which may result in the inhibition of Ras function and apoptosis in susceptible tumor cells. This agent may reverse the malignant phenotype of H-Ras-transformed cells and has been shown to be active against tumor cell...
T70287	BMS-186511
	BMS-186511 is a Farnesyltransferase (FT) inhibitor with potential anticancer activity. BMS-186511 is a bisubstrate analogue inhibitor of FT, would inhibit the malignant growth properties of a cell line established from malignant schwannoma of an NF1 patient. Following treatment with BMS-186511 , ST88-14 cells became flat, nonrefractile, were contact-inhibited, and lost their ability to grow in soft agar. BMS-186511 was found to specifically inhibit FT, but not geranylgeranyltransferase I, a clos...
T83948	Sakura 6
	Sakura 6是一种合成的5-HT转运体(SERT)结合肽，促进SERT与神经元型一氧化氮合酶的相互作用，降低SERT活性和细胞表面的SERT，增加自我抑制，减少突触5-HT释放并降低背侧绕束核的放电。在抑郁症小鼠模型中诱导急性抑郁表型。
T69618	XR3054
	XR3054 is a novel inhibitor of farnesyl protein transferase (FPTase). XR3054 inhibited the proliferation of the prostatic cancer cell lines LnCAP and PC3 and the colon carcinoma SW480 and HT1080 (IC50 values of 12.4, 12.2, 21.4 and 8.8 microM, respectively) but was relatively inactive when tested against a panel of breast carcinoma cell lines. The activity did not relate to the presence of mutant or wild-type ras in the cell lines tested. In conclusion XR3054 inhibits ras farnesylation, MAP kina...
T63608	P-gp inhibitor 5
	P-gp inhibitor 5 是 P 糖蛋白 (P-gp) 的有效抑制剂，在 1.25 μM 和 2.5 μM 时 P-gp 抑制倍数分别为 2.5 和 3.0。P-gp inhibitor 5 对某些癌细胞表现出抗增殖效果。P-gp inhibitor 5 能够恢复细胞对 Vincristine 和 Paclitaxel 的敏感性，进而逆转 ABCB1/Flp-InTM-293 和 KBvin 的多药耐药 (MDR) 表型。
T37579	GW 1929 hydrochloride
	Highly selective orally active peroxisome proliferator-activated receptor (PPAR)γ agonist (pEC50 values are 8.05, < 4 and < 4 for human PPARγ, PPARα and PPARδ receptors respectively). Decreases glucose, fatty acid and triglyceride levels following oral administration in vivo. Brown et al (1999) A novel N-aryl tyrosine activator of peroxisome proliferator-activated receptor-γ reverses the diabetic phenotype of the Zucker diabetic fatty rat. Diabetes 48 1415 PMID:10389847 \|Nugent et al (2001) Pote...
T35604	Osteocalcin (1-49) (human) (trifluoroacetate salt)
	Osteocalcin (1-49) is a non-collagenous peptide that is secreted by osteoblasts and odontoblasts and comprises 1-2% of the total protein in bone. Secretion of osteocalcin (1-49) is stimulated by 1,25-dihydroxy vitamin D and plasma levels increase in diseases that induce dysregulated bone turnover such as osteoporosis, Paget's disease, and primary hyperparathyroidism. Osteocalcin (1-49) is positively correlated with insulin sensitivity and negatively correlated with high blood glucose levels in w...

化合物

Cat.No: T9020

Target: Epigenetic Reader Domain

Cat.No: T3144

Synonym: Wnt agonist 1

Target: Wnt/beta-catenin

Cat.No: T3206

Synonym: Histone Deacetylase Inhibitor IV,PAOA

Target: HDAC

BML-284 hydrochloride

Cat.No: T8820

Synonym: BML-284 HCL,Wnt agonist 1 HCL

Target: Wnt/beta-catenin

Bis(maltolato)oxovanadium(IV)

Cat.No: T22276

Synonym: 双(麦芽醇)氧钒(IV),BMOV,Bis maltolato oxovanadium,Bis(maltolato)oxovanadium (IV),bis maltolato oxo vanadium,Bis(maltolato)oxovanadium (IV)

Target: Phosphatase, Others

Cat.No: T15168

Target: Others

KHS101 hydrochloride

Cat.No: T5170

Synonym: 盐酸KHS101

Target: FGFR, Microtubule Associated

Cat.No: T77379

Synonym: FP-1305

Target: Others

Cat.No: T63049

Target: Others

Cat.No: T9682

Synonym: AZD4877

Target: Apoptosis, Kinesin

Cat.No: T11134

Target: Others

Cat.No: T27537

Cat.No: T27551

Synonym: Honokiol Bis-Dichloroacetate

Cat.No: T70367

Tonantzitlolone

Cat.No: T68582

IGF-1R inhibitor-2

Cat.No: T38502

Anti-neuroinflammation agent 1

Cat.No: T79590

Target: NOD-like Receptor (NLR)

Cat.No: T21317

Synonym: BAL27862,BAL-27862,BAL 27862

Cat.No: T69782

L-Kynurenine sulfate

Cat.No: T72430

Cat.No: T40099

Cat.No: T68737

Cat.No: T61072

FKBP51F67V-selective antagonist Ligand2

Cat.No: T79184

Target: FKBP

Cat.No: T68227

Cat.No: T70287

Cat.No: T83948

Cat.No: T69618

P-gp inhibitor 5

Cat.No: T63608

GW 1929 hydrochloride

Cat.No: T37579

Osteocalcin (1-49) (human) (trifluoroacetate salt)

Cat.No: T35604

Cat. No.	Product Name	Target	Signaling Pathways
T2895	Lupeol Fagarasterol,羽扇豆醇,Monogynol B,Clerodol,(3β,13ξ)-Lup-20(29)-en-3-ol,Farganasterol	Apoptosis; Androgen Receptor; Akt	Apoptosis; Cytoskeletal Signaling; Endocrinology/Hormones; PI3K/Akt/mTOR signaling
	Lupeol (Monogynol B) 是一个活跃的五环三萜，具有抗氧化剂、抗肿瘤和抗炎活性。它是一种雄激素受体抑制剂，可研究癌症，特别是雄激素依赖表型和去势抵抗表型的前列腺癌。
T4831	α,α-Dimethylglycine 2-Aminoisobutyric acid,α-Aminoisobutanoic acid,2-甲基丙氨酸	Others; Endogenous Metabolite	Metabolism; Others
	NSC-16590 (2-Aminoisobutyric acid) 对苍耳子叶中内源性乙烯(ethylene)的产生具有抑制作用。
T60256	2,4,5-Trimethoxybenzoic acid
	2,4,5-Trimethoxybenzoic acid 是一种紫苏提取物中发现的化合物，可抑制 M1 巨噬细胞表型介导的糖尿病炎症反应。

天然产物

Cat.No: T2895

Synonym: Fagarasterol,羽扇豆醇,Monogynol B,Clerodol,(3β,13ξ)-Lup-20(29)-en-3-ol,Farganasterol

Target: Apoptosis, Androgen Receptor, Akt

α,α-Dimethylglycine

Cat.No: T4831

Synonym: 2-Aminoisobutyric acid,α-Aminoisobutanoic acid,2-甲基丙氨酸

Target: Others, Endogenous Metabolite

2,4,5-Trimethoxybenzoic acid

Cat.No: T60256

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