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26

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T2567	Etonogestrel 3-Oxodesogestrel,3-keto-Desogestrel,依托孕烯,Nexplanon,Implanon	Estrogen Receptor/ERR; Estrogen/progestogen Receptor; Progesterone Receptor; Endogenous Metabolite	Endocrinology/Hormones; Metabolism; Others
	Etonogestrel (Implanon) 是孕激素去氧孕烯的生物活性代谢物，与靶器官中的孕酮受体和雌激素受体高亲和力地结合，可诱导FKBP51mRNA 和蛋白表达。它是一种甾体孕激素，用作激素避孕药。
T5409	AZD3229	c-Kit	Tyrosine Kinase/Adaptors
	AZD3229 是一种突变型酪氨酸激酶受体抑制剂，可用于胃肠道间质瘤的研究。
T10803	CHMFL-KIT-033	c-Kit	Tyrosine Kinase/Adaptors
	CHMFL-KIT-033 是一种有效的选择性 c-KIT 抑制剂，对胃肠道间质瘤中的 c-KIT T670I 突变体的 IC50 值为 45 nM。
T1776L	Plerixafor octahydrochloride 盐酸普乐沙福,JM3100 octahydrochloride,Plerixafor 8HCl (AMD3100 8HCl),Plerixafor 8HCl,SID791 octahydrochloride,AMD 3100 octahydrochloride,JM 3100 8HCl	Virus Protease; HIV Protease; CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	Plerixafor octahydrochloride (JM3100 octahydrochloride) 是一种选择性的CXCR4拮抗剂，IC50为 44 nM。Plerixafor 是一种具有造血干细胞动员活性的双环霉素。
T8402	Regorafenib Hydrochloride 瑞戈非尼盐酸盐,BAY73-4506 hydrochloride	Raf; VEGFR; c-RET; PDGFR; Autophagy	Angiogenesis; Apoptosis; Autophagy; MAPK; Tyrosine Kinase/Adaptors
	Regorafenib Hydrochloride (BAY73-4506 hydrochloride) 是一种新型口服多激酶抑制剂，可抑制血管生成、基质和致癌受体酪氨酸激酶，具有强大的临床前抗肿瘤活性。它靶向作用于 VEGFR1/2/3、PDGFRβ、Kit、RET 和 Raf-1，IC50值分别为 13/4.2/46、22、7、1.5 和 2.5 nM。
T4605	NT157	IGF-1R; STAT	JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors
	NT157 是一种口服生物可利用的间充质-上皮转化 (MET) TKI，主要针对具有 METex14 跳跃突变的特定 NSCLC 患者开发。
T1776	Plerixafor 普乐沙福,JM3100,AMD 3100,AMD-3329	Virus Protease; HIV Protease; CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	Plerixafor (AMD-3329) 是一种趋化因子受体拮抗剂，可阻断基质细胞衍生因子与细胞受体 CXCR4 的结合。它也是 CXCR7 的变构激动剂，是免疫刺激剂和造血干细胞动员剂，还抑制HIV-1和HIV-2的复制，EC50为 1-10 nM。
T17208	USL311	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	USL311 是选择性 CXCR4拮抗剂，可防止基质细胞衍生因子 1（SDF-1 或 CXCL12）与 CXCR4 结合。它抑制 CXCR4 活化并减少表达 CXCR4 的肿瘤细胞的增殖和迁移，具有抗肿瘤活性。
T16686	Pyr10	TRP/TRPV Channel	Membrane transporter/Ion channel
	Pyr10 是吡唑衍生物，是TRPC3通道的选择性抑制剂。Pyr10抑制卡巴可刺激的TRPC3转染的 HEK293 细胞中的 Ca2+流入。它具有区分受体操纵的TRPC3和天然基质相互作用分子 1 (STIM1)/Orai1 通道的能力。
T16104	ML-9	Myosin; Akt	Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	ML-9 是 Akt 激酶的一种选择性强效抑制剂，可抑制肌球蛋白轻链激酶 (MLCK) 和基质相互作用分子1(STIM1) 活性。它通过刺激自噬小体的形成并抑制其降解来诱导自噬。它抑制 MLCK，PKA 和 PKC 活性，Ki 值分别为 4、32 和 54 μM。
T77697	BML-278 BML278,BML 278	Sirtuin; Histone Methyltransferase	Chromatin/Epigenetic; DNA Damage/DNA Repair
	BML-278 是一种 SIRT1 激活剂，EC150 值为 1 μM。BML-278 增加父本和母本原核中的 H3K9 甲基化并抑制 H3K9 乙酰化，可用于改善早期胚胎发育。BML-278 促使原代人间充质细胞的细胞周期停止在 G1/S 期，可用于延缓衰老。BML-278 减少 U937 细胞中的微管蛋白乙酰化，增加小鼠 C2C12 成肌细胞的线粒体密度。
T70062	Osteoprotegerin
	Osteoprotegerin is a soluble secreted member of the tumor necrosis factor receptor superfamily, inhibiting osteoclastogenesis by interrupting the signaling between stromal cells and osteoclastic progenitor cells, leading to excess accumulation of bone and cartilage.
T71894	AZD3229 Tosylate
	AZD3229 Tosylate is a highly potent inhibitor targeting mutant forms of the pan-KIT enzyme, with a primary application in the treatment of gastrointestinal stromal tumors (GISTs).
T22859	Imatinib hydrochloride	Others	Others
	Imatinib is a multi-target inhibitor of v-Abl, c-Kit, and PDGFR (IC50: 0.6 μM, 0.1 μM, and 0.1 μM, respectively). Imatinib is used to treat chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs), and a number of other malignancies.
T16103	ML-9 Free Base	Others	Others
	ML-9 (free base) suppresses MLCK, PKA, and PKC activity (Ki: 4, 32, and 54 μM, respectively). ML-9 (free base) is a selective and effective inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK), and stromal interaction molecule 1 (STIM1) acti
T40908	KLD-12
	KLD-12, a 12-residue self-assembling peptide, displays properties that promote chondrogenic differentiation of bone marrow stromal cells (BMSCs). Moreover, KLD-12 hydrogel can effectively fill full-thickness osteochondral defects in their original location, leading to improved cartilage repair.
T82851	BMP2-derived peptide
	BMP2-derived peptide为BMP-2第73至92位氨基酸序列的功能性基序，具有促进骨髓基质细胞(BMSCs)成骨分化及骨再生的作用。
T76327	CTCE-0214
	CTCE-0214 是一种 CXCR4(chemokine CXC receptor 4) 激动剂，是 SDF-1α 肽类似物。CTCE-0214 具有抗炎活性，可用于炎症败血症和系统性炎症综合征的研究。
T82507	Ecleralimab CSJ-117,NVP-CSJ117
	Ecleralimab (CSJ-117; NVP-CSJ117) 是一种 Fab-IgG1-λ2 类型的单克隆抗体，专一性靶向胸腺基质淋巴生成素（TSLP）。该抗体主要采用 CHO（Chinese Hamster Ovary）细胞表达系统生产。
T68861	MS-0022
	MS-0022 is a SMO antagonist. MS-0022 showed effective Hh signaling pathway inhibition at the level of SMO in the low nM range, and Hh pathway inhibition downstream of Suppressor of fused (SUFU) in the low µM range. MS-0022 reduced growth in the tumor cell lines PANC-1, SUIT-2, PC-3 and FEMX in vitro. MS-0022 is a treatment led to a transient delay of tumor growth that correlated with a reduction of stromal Gli1 levels in SUIT-2 xenografts in vivo.
T69288	CEP-7055
	CEP-18770 is an orally bioavailable synthetic P2 threonine boronic acid inhibitor of the chymotrypsin-like activity of the proteasome, with potential antineoplastic activity. Proteasome inhibitor CEP 18770 represses the proteasomal degradation of a variety of proteins, including inhibitory kappaBalpha (IkappaBalpha), resulting in the cytoplasmic sequestration of the transcription factor NF-kappaB; inhibition of NF-kappaB nuclear translocation and transcriptional up-regulation of a variety of cel...
T68306	INCB16562
	INCB16562 is a novel, selective, and orally bioavailable small-molecule inhibitor of JAK1 and JAK2 markedly selective over JAK3. Treatment of myeloma cells with INCB16562 potently inhibited interleukin-6 (IL-6)-induced phosphorylation of STAT3. INCB16562 abrogated the protective effects of recombinant cytokines or bone marrow stromal cells and sensitized myeloma cells to cell death by exposure to dexamethasone, melphalan, or bortezomib. Oral administration of INCB16562 antagonized the growth of ...
T69081	KRH-1636
	KRH-1636 is an orally active, selective and extremely potent CXC chemokine receptor 4 antagonist. KRH-1636 exhibits a potent and selective anti-HIV-1 activity. KRH-1636 efficiently blocked replication of various T cell line-tropic (X4) HIV type 1 (HIV-1) in MT-4 cells and peripheral blood mononuclear cells through the inhibition of viral entry and membrane fusion via the CXC chemokine receptor (CXCR)4 coreceptor but not via CC chemokine receptor 5. KRH-1636 also inhibits binding of the CXC chem...
T83880	C18 Ceramide-1-phosphate (d18:1/18:0) ammonium Ceramide-1-phosphate (d18:1/18:0),N-octadecanoyl-D-erythro-Sphingosine-1-phosphate,C18 Ceramide-1-phosphate,C18 C1P,CerP(d18:1/18:0),N-stearoyl-D-erythro-Sphingosine-1-phosphate
	C18 Ceramide-1-phosphate (d18:1/18:0) 是一种在鼠皮肤中发现的长链ceramide-1-phosphate。它能在0.5至5 µM的浓度范围内促进分离的小鼠骨髓来源的多能间充质细胞和人脐静脉内皮细胞（HUVECs）的迁移。与胰腺癌干细胞相比，CFPAC-1胰管腺癌细胞中C18 Ceramide-1-phosphate (d18:1/18:0)的水平有所增加。在Langendorff分离的灌流小鼠心脏的离体缺血模型中，心肌中C18 ceramide-1-phosphate (d18:1/18:0)的水平有所增加。
T37265	15(R)-Lipoxin A4 15(R)-Lipoxin A4,AT-Lipoxin A4
	Lipid-derived lipoxins are produced at the site of vascular and mucosal inflammation where they down-regulate polymorphonuclear leukocyte recruitment and function. 15(R)-Lipoxin A4 (15(R)-LXA4) is derived from the aspirin-triggered formation of 15(R)-HETE from arachidonic acid. [1] [2] 15(R)-LXA4 inhibits LTB4-induced chemotaxis, adherence, and transmigration of neutrophils with twice the potency of LXA4 demonstrating activity in the nM range.[2] [3] The anti-inflammatory effects of aspirin may...
T68321	AS1940477
	AS1940477 is p38 MAPK inhibitor. AS1940477 inhibited the enzymatic activity of recombinant p38α and β isoforms but showed no effect against other 100 protein kinases including p38γ and δ isoforms. In human peripheral blood mononuclear cells, AS1940477 inhibited lipopolysaccharide (LPS)- or phytohemagglutinin A (PHA)-induced production of proinflammatory cytokines, including TNFα, IL-1β, and IL-6 at low concentrations (LPS/TNFα, IC(50)=0.45n M; PHA/TNFα, IC(50)=0.40 nM). In addition, equivalent c...

化合物

Cat.No: T2567

Synonym: 3-Oxodesogestrel,3-keto-Desogestrel,依托孕烯,Nexplanon,Implanon

Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor, Progesterone Receptor, Endogenous Metabolite

Cat.No: T5409

Target: c-Kit

Cat.No: T10803

Target: c-Kit

Plerixafor octahydrochloride

Cat.No: T1776L

Synonym: 盐酸普乐沙福,JM3100 octahydrochloride,Plerixafor 8HCl (AMD3100 8HCl),Plerixafor 8HCl,SID791 octahydrochloride,AMD 3100 octahydrochloride,JM 3100 8HCl

Target: Virus Protease, HIV Protease, CXCR

Regorafenib Hydrochloride

Cat.No: T8402

Synonym: 瑞戈非尼盐酸盐,BAY73-4506 hydrochloride

Target: Raf, VEGFR, c-RET, PDGFR, Autophagy

Cat.No: T4605

Target: IGF-1R, STAT

Cat.No: T1776

Synonym: 普乐沙福,JM3100,AMD 3100,AMD-3329

Target: Virus Protease, HIV Protease, CXCR

Cat.No: T17208

Target: CXCR

Cat.No: T16686

Target: TRP/TRPV Channel

Cat.No: T16104

Target: Myosin, Akt

Cat.No: T77697

Synonym: BML278,BML 278

Target: Sirtuin, Histone Methyltransferase

Osteoprotegerin

Cat.No: T70062

AZD3229 Tosylate

Cat.No: T71894

Imatinib hydrochloride

Cat.No: T22859

Target: Others

Cat.No: T16103

Target: Others

Cat.No: T40908

BMP2-derived peptide

Cat.No: T82851

Cat.No: T76327

Cat.No: T82507

Synonym: CSJ-117,NVP-CSJ117

Cat.No: T68861

Cat.No: T69288

Cat.No: T68306

Cat.No: T69081

C18 Ceramide-1-phosphate (d18:1/18:0) ammonium

Cat.No: T83880

Synonym: Ceramide-1-phosphate (d18:1/18:0),N-octadecanoyl-D-erythro-Sphingosine-1-phosphate,C18 Ceramide-1-phosphate,C18 C1P,CerP(d18:1/18:0),N-stearoyl-D-erythro-Sphingosine-1-phosphate

15(R)-Lipoxin A4

Cat.No: T37265

Synonym: 15(R)-Lipoxin A4,AT-Lipoxin A4

Cat.No: T68321

Cat. No.	Product Name	Target	Signaling Pathways
T5751	Tigogenin	Others	Others
	Tigogenin 是甾体皂甙元，普遍用于甾体类药物的合成。它能够阻碍小鼠骨髓基质细胞脂肪细胞分化，促使成骨细胞的分化。
T3674	Hydroxysafflor yellow A 藏红花,羟基红花黄色素A,HSYA,Safflomin A	TGF-beta/Smad	Stem Cells
	Hydroxysafflor yellow A (Safflomin A) 是一种黄酮类天然产物，从中药红花中分离得到，具有抗癌作用。
T2820	Glycitin 黄豆黄苷,Glycitein-7-β-O-glucoside,Glycitein 7-O-β-glucoside	Others; Influenza Virus; Antibacterial	Microbiology/Virology; Others
	Glycitin (Glycitein 7-O-β-glucoside) 是一种从豆类中分离出来的天然异黄酮，有抗菌，抗病毒和雌激素作用，还有促进骨髓基质细胞和成骨细胞的增殖和抑制骨转换的生物学功能。
T3524	Halofuginone hydrobromide 卤夫酮溴氢酸盐,Tempostatin,RU-19110 (hydrobromide),Stenorol,常山酮溴酸盐	Others; Calcium Channel; DNA/RNA Synthesis; Sodium Channel; Parasite; TGF-beta/Smad	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Others; Stem Cells
	Halofuginone hydrobromid 是Febrifugine 的衍生物，是竞争性脯氨酰-tRNA 合成酶抑制剂。它是 I 型胶原合成的特异性抑制剂，并通过抑制TGF-β活性可减轻骨关节炎。它具有抗疟疾、抗炎、抗癌、抗纤维化作用。

天然产物

Cat.No: T5751

Target: Others

Hydroxysafflor yellow A

Cat.No: T3674

Synonym: 藏红花,羟基红花黄色素A,HSYA,Safflomin A

Target: TGF-beta/Smad

Cat.No: T2820

Synonym: 黄豆黄苷,Glycitein-7-β-O-glucoside,Glycitein 7-O-β-glucoside

Target: Others, Influenza Virus, Antibacterial

Halofuginone hydrobromide

Cat.No: T3524

Synonym: 卤夫酮溴氢酸盐,Tempostatin,RU-19110 (hydrobromide),Stenorol,常山酮溴酸盐

Target: Others, Calcium Channel, DNA/RNA Synthesis, Sodium Channel, Parasite, TGF-beta/Smad

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