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22

抑制剂 & 化合物

20

天然产物

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Cat. No. Product Name Target Signaling Pathways
T9917 Denosumab

RANKL/RANK NF-κB
Denosumab 是能够结合并抑制RANKL 受体激活因子的人单克隆抗体。它具有抗癌活性,可降髋部、低椎骨以及非椎骨骨折的风险。
T7844 4-IPP

4-Iodo-6-phenylpyrimidine

Others Others
4-IPP (4-Iodo-6-phenylpyrimidine) 是一种巨噬细胞迁移抑制因子 (MIF) 的特异性自杀底物,也是 MIF 的不可逆抑制剂。
T16159 Muramyl dipeptide

MDP

NOD Immunology/Inflammation; NF-κB
Muramyl dipeptide (MDP) 是合成的免疫反应肽,由 N-乙酰壁酸与 L-Ala-D-isoGln 的短氨基酸链相连。它通过MAPK 途径上调 Runx2 基因表达,直接促进成骨细胞分化,通过降低 RANKL/OPG 比值间接抑制破骨细胞分化。它是通过Runx2诱导骨形成的诱导因子,也是NLRP1激动剂。
T13324 VUF11207 fumarate

CXCR; Arrestin Autophagy; GPCR/G Protein; Immunology/Inflammation
VUF11207 fumarate 是一种 CXCR7激动剂和高效CXCR7配体,pKi 为 8.1。它可诱导CXCR7的β-arrestin2募集和随后的内在化,pEC50分别为 8.8 和 7.9。
T62189 sRANKL-IN-1

sRANKL-IN-1 (compound S3) 是一种 sRANKL (soluble RANKL) 的抑制剂。sRANKL-IN-1 能够较强的抑制破骨细胞 (IC50: 0.096 μM,Kd: 34.80 μM)。sRANKL-IN-1 能够用于研究骨质疏松症。
T61531 NFATc1-IN-1

RANKL/RANK NF-κB
NFATc1-IN-1 (also known as compound A04) is a highly effective inhibitor of osteoclast formation induced by RANKL, with an IC50 of 1.57 μM. It exerts its anti-osteoclastogenic effects by attenuating the RANKL-induced nuclear translocation of NFATc1. Due to its remarkable properties, NFATc1-IN-1 holds significant potential for advancing research related to osteoclastic diseases [1].
T77567 BCPA

Others Others
BCPA 是一种无细胞毒性的 Pin1 调节剂。BCPA 可调节破骨细胞活化,减弱 Pin1 蛋白的减少,从而抑制 RANKL 诱导的破骨细胞发生的受体激活物。BCPA 用于研究骨质疏松。
T15718 Latanoprost acid

GPR Endocrinology/Hormones; GPCR/G Protein
Latanoprost acid 是前列腺素受体的选择性激动剂,通过抑制 c-fos/NFATc1 通路抑制 RANKL 诱导的破骨细胞生成和功能。 拉坦前列素酸可用于降低眼内压力的研究。
T2188 Thonzonium Bromide

嘧苯十六铵,通佐溴胺

Proton pump; Antibacterial; Autophagy Autophagy; Membrane transporter/Ion channel; Microbiology/Virology
Thonzonium bromide 是一种单阳离子表面活性剂,在结构上与 Farnesol 相似的抗菌剂。它以剂量依赖的方式抑制质子转运 (EC50=69 μM)。在体外可抑制 RANKL 诱导的破骨细胞形成和骨吸收,并在体内阻止 LPS 诱导的骨丢失。
T27526 Halenaquinone

Halenaquinone is a phosphatidylinositol 3-kinase inhibitor. Halenaquinone specifically inhibits the secondary DNA binding of RAD51. Halenaquinone inhibits RANKL-induced osteoclastogenesis. Halenaquinone induces apoptosis in PC12 cells.
T72008 E09241

E09241 is a novel OPG/RANKL upregulator, increasing OPG expression without affecting RANKL expression, promoting osteoblast differentiation while inhibiting osteoclast differentiation, regulating OPG expression through canonical Wnt/β-catenin signaling.
T80618 Narlumosbart

RANKL/RANK NF-κB
Narlumosbart(JMT103)是一种IgG4κ型抗体,专一性靶向核因子-κB 配体受体激活剂(RANKL)。
T71479 Kahweol oleate

Kahweol oleate is emi-syntetic derivative of kahweol, a natural product found in coffee beans. It exhibits a wide variety of biological activities, including inhibiting RANKL-induced osteoclast generation, inducing cell cycle arrest and apoptosis in oral squamous cell carcinoma cells, preventing aflatoxin B1 induced DNA adduct formation, and suppressing H2O2-induced DNA damage and oxidative stress.
T69205 GGTI-2166

GGTI-2166 is a geranylgeranyl transferase I inhibitor. GGTI-2166 inhibit the pOC formation induced by RANKL or TNF-alpha in cultures of both mouse marrow-derived macrophage-colony-stimulating factor (M-CSF) dependent monocytes (MD cells) and the mouse monocyte cell line RAW 264.7 (RAW cells). GGTI-2166 inhibited TRAP activity induced by RANKL or TNF-alpha in both cell cultures and prevented the incorporation of [3H]all-trans geranylgeraniol into prenylated proteins in RAW cells.
T68642 Kahweol palmitate

Kahweol palmitate is a semi-synthetic derivative of kahweol, a natural product found in coffee beans. It exhibits a wide variety of biological activities, including inhibiting RANKL-induced osteoclast generation, inducing cell cycle arrest and apoptosis in oral squamous cell carcinoma cells, preventing aflatoxin B1-induced DNA adduct formation, and suppressing H2O2-induced DNA damage and oxidative stress.
T73061 Amakusamine

Amakusamine以IC50值为10.5 μM,抑制NF-κB配体受体激活剂(RANKL)在RAW264.7细胞中诱导的多核破骨细胞形成。
T81171 SH491

SH491(Compound 33)是一款抗骨质疏松药物。该化合物能够抑制RANKL诱导的骨髓源性单核细胞(BMM)分化为破骨细胞(IC50: 11.8 nM)。同时,SH491降低了破骨细胞形成的相关标记基因(TRAP、CTSK、MMP-9和ATPase v0d2)以及相应蛋白(TRAP、CTSK、MMP-9)的表达。
T71480 Kahweol linoleate

Kahweol linoleate is a semi-syntetic derivative of kahweol, a natural product found in coffee beans. It exhibits a wide variety of biological activities, including inhibiting RANKL-induced osteoclast generation, inducing cell cycle arrest and apoptosis in oral squamous cell carcinoma cells, preventing aflatoxin B1 induced DNA adduct formation, and suppressing H2O2-induced DNA damage and oxidative stress.
T71478 Kahweol stearate

Kahweol stearate is a semi-synthetic derivative of kahweol, a natural product found in coffee beans. It exhibits a wide variety of biological activities, including inhibiting RANKL-induced osteoclast generation, inducing cell cycle arrest and apoptosis in oral squamous cell carcinoma cells, preventing aflatoxin B1-induced DNA adduct formation, and suppressing H2O2-induced DNA damage and oxidative stress.
T68641 Kahweol Acetate

Kahweol Acetate is a semi-synthetic derivative of kahweol, a natural product found in coffee beans. It exhibits a wide variety of biological activities, including inhibiting RANKL-induced osteoclast generation, inducing cell cycle arrest and apoptosis in oral squamous cell carcinoma cells, preventing aflatoxin B1 induced DNA adduct formation, and suppressing H2O2-induced DNA damage and oxidative stress.
T19848 Cyclosporin B

7-L-Alanine-cyclosporin A,Antibiotic S 7481F2

Cyclosporin B is an immunosuppressant that has revolutionized organ transplantation through its use in the prevention of graft rejection. Cyclosporin B displays antiviral properties, inhibiting the entry of hepatitis B into hepatocytes. Cyclosporin B also
T78816 Anti-osteoporosis agent-4

NF-κB NF-κB
Anti-osteoporosis agent-4 (Compound 11h) 在生物医学领域中表现为有效抑制原代破骨细胞的分化,减弱RANKL诱导的破骨细胞生成,并展示出强抑制作用,具有 IC50 值为358.29 nM。此外,该化合物还能抑制关键的 PI3K/AKT 和 IκBα/NF-κB 信号通路激活,表明其在防治骨质疏松症中的潜在应用价值。

化合物

Denosumab
Cat.No: T9917
Synonym:
Target: RANKL/RANK
4-IPP
Cat.No: T7844
Synonym: 4-Iodo-6-phenylpyrimidine
Target: Others
Muramyl dipeptide
Cat.No: T16159
Synonym: MDP
Target: NOD
VUF11207 fumarate
Cat.No: T13324
Synonym:
Target: CXCR, Arrestin
sRANKL-IN-1
Cat.No: T62189
Synonym:
Target:
NFATc1-IN-1
Cat.No: T61531
Synonym:
Target: RANKL/RANK
BCPA
Cat.No: T77567
Synonym:
Target: Others
Latanoprost acid
Cat.No: T15718
Synonym:
Target: GPR
Thonzonium Bromide
Cat.No: T2188
Synonym: 嘧苯十六铵,通佐溴胺
Target: Proton pump, Antibacterial, Autophagy
Halenaquinone
Cat.No: T27526
Synonym:
Target:
E09241
Cat.No: T72008
Synonym:
Target:
Narlumosbart
Cat.No: T80618
Synonym:
Target: RANKL/RANK
Kahweol oleate
Cat.No: T71479
Synonym:
Target:
GGTI-2166
Cat.No: T69205
Synonym:
Target:
Kahweol palmitate
Cat.No: T68642
Synonym:
Target:
Amakusamine
Cat.No: T73061
Synonym:
Target:
SH491
Cat.No: T81171
Synonym:
Target:
Kahweol linoleate
Cat.No: T71480
Synonym:
Target:
Kahweol stearate
Cat.No: T71478
Synonym:
Target:
Kahweol Acetate
Cat.No: T68641
Synonym:
Target:
Cyclosporin B
Cat.No: T19848
Synonym: 7-L-Alanine-cyclosporin A,Antibiotic S 7481F2
Target:
Anti-osteoporosis agent-4
Cat.No: T78816
Synonym:
Target: NF-κB
Cat. No. Product Name Target Signaling Pathways
T5528 Cyanidin Chloride

Antioxidant oxidation-reduction
Cyanidin Chloride 是一种花青素的亚类,具有抗氧化和抗癌活性。它能够抑制破骨细胞形成,羟基磷灰石吸收和 NF-κB 配体 (RANKL) 诱导的破骨细胞标记基因表达的受体激活。
T0683 Mevastatin

Compactin,ML236B,美伐他汀

Apoptosis; Antibacterial; Antibiotic; HMG-CoA Reductase; Autophagy; Lipid Apoptosis; Autophagy; Metabolism; Microbiology/Virology
Mevastatin (ML236B) 是他汀类 HMG-CoA 还原酶抑制剂。它是一种降脂药,可诱导细胞凋亡,将癌细胞阻滞在 G0/G1期。它还可增加内皮型一氧化氮合酶的 mRNA 和蛋白质水平。它有抗肿瘤活性,用于心血管疾病的研究。
TN1215 (2S)-2'-Methoxykurarinone

2'-甲氧基苦参黄素,2'-Methoxykurarinone,2'-O-Methylkurarinone

Akt; Antifection Cytoskeletal Signaling; Microbiology/Virology; PI3K/Akt/mTOR signaling
(2S)-2'-Methoxykurarinone 是一种分离自苦参根中的化合物,具有抗炎、解热、抗糖尿病和抗肿瘤活性。它对人髓系白血病 HL-60 细胞具有细胞毒活性。它能够下调 RANKL 信号,抑制破骨细胞形成和骨吸收。
T2789 Scutellarin

黄岑素,野黄芩苷,Breviscapin,Breviscapinun,Breviscapine,Scutellarein-7-glucuronide

Akt; HIV Protease; STAT Cytoskeletal Signaling; JAK/STAT signaling; Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells
Scutellarin (Scutellarein-7-glucuronide) 是从黄芩中分离的黄酮,可抑制破骨细胞中 RANKL 介导的 MAPK 和 NF-κB 信号通路,并下调 HCC 细胞中的 STAT3/Girdin/Akt 信号通路。
TN2143 3,7,4'-Trihydroxyflavone

Resokaempferol,5-Deoxykampferol

DNA DNA Damage/DNA Repair
3,7,4'-Trihydroxyflavone(5-Deoxykampferol) 是从黄檀心材中分离得到的一种具有 DNA 断链活性的黄酮类化合物,可抑制 NF-κB 配体 (RANKL) 受体激活剂诱导的 RAW 264.7 细胞和骨髓巨噬细胞中的破骨细胞分化、肌动蛋白环形成和骨吸收。
T5770 Alisol B

RANKL/RANK NF-κB
Alisol B 是一种具有用于骨科疾病研究潜力的化合物,通过分化破骨细胞发挥其功能。
T6S0923 Hypericin

Hypericine,金丝桃素,Cyclosan

Apoptosis; Antiviral; Influenza Virus; Tyrosine Kinases; Antibacterial; PKC Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; Immunology/Inflammation; Microbiology/Virology; Tyrosine Kinase/Adaptors
Hypericin (Cyclosan) 是贯叶连翘的提取物,有抗菌、抗病毒、抗肿瘤和抗抑郁作用。
T3849 Kinsenoside

金线莲苷,(+)-Kinsenoside

Apoptosis; Nrf2 Apoptosis; Immunology/Inflammation
Kinsenoside ((+)-Kinsenoside) 是从金盏花属植物中分离得到的主要活性成分,以 Nrf2 依赖的方式保护髓核细胞在氧化应激下的生存能力,防止细胞凋亡、衰老和线粒体功能障碍。它显示出显着的抗肝毒性和抗炎活性。
T2755 Rhoifolin

野漆树苷,Apigenin-7-O-rhamnoglucoside,Apigenin 7-O-neohesperidoside,Rhoifoloside

Others; p38 MAPK; NF-κB; transporter; IGF-1R; Autophagy Autophagy; MAPK; Metabolism; NF-κB; Others; Tyrosine Kinase/Adaptors
Rhoifolin (Apigenin 7-O-neohesperidoside) 是从琯溪蜜柚叶子分离的一种黄酮糖苷。它通过 RANKL 诱导的NF-κB 和MAPK 途径改善钛颗粒刺激的骨溶解并减少破骨细胞生成。它通过增强脂联素分泌,胰岛素受体-β的酪氨酸磷酸化和GLUT4易位有助于治疗糖尿病并发症。
T5720 Boldine

1,10-Dimethoxy-2,9-dihydroxyaporphine,波尔定碱,波尔定,ex Peumus boldus

RANKL/RANK NF-κB
Boldine (1,10-Dimethoxy-2,9-dihydroxyaporphine) 是一种阿扑吗啡异喹啉生物碱,从山苍子根中提取获得,具有抗氧化、抗炎和细胞保护的活性。它能够抑制破骨细胞生成,并利用下调 OPG/RANKL/RANK 信号途径,改善骨破坏。它可用于研究类风湿性关节炎。
TN1712 Gossypin

NF-κB; S6 Kinase MAPK; NF-κB; PI3K/Akt/mTOR signaling
Gossypin 是一种从Hibiscus vitifolius 中分离得到的黄酮,能够抑制NF-κB 和 NF-κB 的调节基因表达。在小鼠原代骨髓细胞和 RAW264.7 细胞中,它也可抑制 RANKL 诱导的破骨细胞形成。它具有抗氧化、抗炎、抗癌、抗衰老、抗糖尿病和保护肝脏的活性。
T5S2129 Sciadopitysin

TNF; NF-κB Apoptosis; NF-κB
Sciadopitysin 是一种双黄酮类化合物,来自银杏叶片中。它通过抑制NF-κB 活化并降低c-Fos 和NFATc1的表达来抑制 RANKL 诱导的破骨细胞生成和骨丢失。
TN3209 3′,4′,7-Trihydroxyflavone 

ATPase; Others; p38 MAPK; NF-κB MAPK; Membrane transporter/Ion channel; NF-κB; Others
3',4',7-Trihydroxyflavone 是分离自蚕豆荚的黄酮苷元化合物。
T38799 2,3-Bis(3-indolylmethyl)indole

2,3-Bis(3-indolylmethyl)indole exhibits concentration-dependent inhibition of RANKL-induced osteoclastogenesis, actin ring formation, and bone resorption.
T83151 Ajudecunoid A

Ajudecunoid A, 一种从Ajuga decumbens分离的天然产物,具有抑制RANKL诱导的破骨细胞生成的活性。
T83033 Anti-osteoporosis agent-2

Anti-osteoporosis agent-2 (Compound 10)为抗骨质疏松剂,能抑制RANKL诱导的破骨细胞分化。
T16846 Sauristolactam

Saurolactam

Others Others
Sauristolactam inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis and has the potential to inhibit osteoclast differentiation. Sauristolactam, a natural aristolactam isolated from aerial portions of Saururus Chi
T27711 Kahweol Eicosanate

J002075,J 002075,J-002075

Kahweol Eicosanate is a semi-syntetic derivative of kahweol. Kahweol Eicosanate exhibits a wide variety of biological activities, including inducing cell cycle arrest and apoptosis in oral squamous cell carcinoma cells, inhibiting RANKL-induced osteoclast
T79932 Eudebeiolide B

Plebeiolide D

NF-κB NF-κB
Eudebeiolide B,一种自荔枝草分离得的化合物,能通过调控RANKL诱导的NF-κB、c-Fos及钙信号来抑制破骨细胞的生成,适用于研究与破骨细胞相关的疾病。
TN2775 2-Methoxystypandrone

MMP; BCL; IκB/IKK; GSK-3; TNF; NOS; NF-κB; Wnt/beta-catenin; COX; JAK; STAT Angiogenesis; Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; Immunology/Inflammation; JAK/STAT signaling; Neuroscience; NF-κB; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells
2-Methoxystypandrone displays an immunomodulatory effect in a cellular model, it blocks inflammatory responses by impairing NF-κB signaling to limit the inflammation and oxidative stress for preservation of BBB integrity. 2-Methoxystypandrone concomitant

天然产物

Cyanidin Chloride
Cat.No: T5528
Synonym:
Target: Antioxidant
Mevastatin
Cat.No: T0683
Synonym: Compactin,ML236B,美伐他汀
Target: Apoptosis, Antibacterial, Antibiotic, HMG-CoA Reductase, Autophagy, Lipid
(2S)-2'-Methoxykurarinone
Cat.No: TN1215
Synonym: 2'-甲氧基苦参黄素,2'-Methoxykurarinone,2'-O-Methylkurarinone
Target: Akt, Antifection
Scutellarin
Cat.No: T2789
Synonym: 黄岑素,野黄芩苷,Breviscapin,Breviscapinun,Breviscapine,Scutellarein-7-glucuronide
Target: Akt, HIV Protease, STAT
3,7,4'-Trihydroxyflavone
Cat.No: TN2143
Synonym: Resokaempferol,5-Deoxykampferol
Target: DNA
Alisol B
Cat.No: T5770
Synonym:
Target: RANKL/RANK
Hypericin
Cat.No: T6S0923
Synonym: Hypericine,金丝桃素,Cyclosan
Target: Apoptosis, Antiviral, Influenza Virus, Tyrosine Kinases, Antibacterial, PKC
Kinsenoside
Cat.No: T3849
Synonym: 金线莲苷,(+)-Kinsenoside
Target: Apoptosis, Nrf2
Rhoifolin
Cat.No: T2755
Synonym: 野漆树苷,Apigenin-7-O-rhamnoglucoside,Apigenin 7-O-neohesperidoside,Rhoifoloside
Target: Others, p38 MAPK, NF-κB, transporter, IGF-1R, Autophagy
Boldine
Cat.No: T5720
Synonym: 1,10-Dimethoxy-2,9-dihydroxyaporphine,波尔定碱,波尔定,ex Peumus boldus
Target: RANKL/RANK
Gossypin
Cat.No: TN1712
Synonym:
Target: NF-κB, S6 Kinase
Sciadopitysin
Cat.No: T5S2129
Synonym:
Target: TNF, NF-κB
3′,4′,7-Trihydroxyflavone 
Cat.No: TN3209
Synonym:
Target: ATPase, Others, p38 MAPK, NF-κB
2,3-Bis(3-indolylmethyl)indole
Cat.No: T38799
Synonym:
Target:
Ajudecunoid A
Cat.No: T83151
Synonym:
Target:
Anti-osteoporosis agent-2
Cat.No: T83033
Synonym:
Target:
Sauristolactam
Cat.No: T16846
Synonym: Saurolactam
Target: Others
Kahweol Eicosanate
Cat.No: T27711
Synonym: J002075,J 002075,J-002075
Target:
Eudebeiolide B
Cat.No: T79932
Synonym: Plebeiolide D
Target: NF-κB
2-Methoxystypandrone
Cat.No: TN2775
Synonym:
Target: MMP, BCL, IκB/IKK, GSK-3, TNF, NOS, NF-κB, Wnt/beta-catenin, COX, JAK, STAT
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