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34

抑制剂 & 化合物

11

天然产物

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Cat. No. Product Name Target Signaling Pathways
T1850 Balicatib

AAE581,巴利卡替

Cysteine Protease Proteases/Proteasome
Balicatib (AAE581) 是组织蛋白酶K 抑制剂,其对组织蛋白酶K 的抑制作用是组织蛋白酶B、L 和S 的抑制性的10到100倍。
T22702 CYM 50769

Neuropeptide W GPCR/G Protein; Neuroscience
CYM 50769是神经肽 B/W 受体 1 的一种选择性拮抗剂。CYM 50769可抑制 NPW-23 诱导的 ATDC5 细胞增殖。CYM 50769在软骨内骨形成方面有研究价值。
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。
T7566 GRGDSPK

EMD 56574

Others Others
GRGDSPK (EMD 56574) 是一种包含精氨酸-甘氨酸-天冬氨酸 (RGD) 的多肽,也是一种竞争性且可逆的抑制肽,可抑制整联蛋白-纤连蛋白结合,可用于整联蛋白在骨形成和吸收中作用的研究。
T7566L1 GRGDSPK acetate

GRGDSPK acetate(111119-28-9 Free base)

Beta Amyloid Neuroscience
GRGDSPK acetate 显示出对整合素-纤连蛋白结合的抑制活性,可用于研究整合素在骨形成和吸收中的作用。
T13360 XRK3F2

Autophagy Autophagy
XRK3F2 是 p62-ZZ 结构域的抑制剂,在体外减弱 MM 诱导的 Runx2 抑制,在体内肿瘤存在的情况下诱导新骨形成和重塑。
T1971 WAY-262611

Wnt/beta-catenin Cytoskeletal Signaling; Stem Cells
WAY262611是一种 Wnt/β- 联蛋白激动剂,也是一种Dkk1的抑制剂。它能够增加骨形成速率,在 TCF- 荧光素酶测定实验中的EC50=0.63 μM。
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。
T15259 Evatanepag

CP-533536 free acid,2-[3-[N-(4-叔丁基苄基)-N-(吡啶-3-基磺酰基)氨基甲基]苯氧基]乙酸

Prostaglandin Receptor GPCR/G Protein; Immunology/Inflammation
Evatanepag (CP-533536 free acid) 是一种 EP2 受体选择性前列腺素 E2 (PGE2) 激动剂,可诱导局部骨形成,EC50 为 0.3 nM。它在大鼠骨折愈合模型中以单剂量局部给药时表现出愈合骨折的能力。
T1210 Sodium etidronate

依替膦酸钠,Didronel

Phosphatase Metabolism
Sodium etidronate (Didronel) 是一种内源性 pyrophosphate 的合成治疗性 diphosphonate 类似物。作为称为 bisphosphonates 盐类药物家族的一员,etidronate disodium 与内源性 pyrophosphate 的不同之处在于其对酶水解的耐受性。该药剂吸附 hydroxyapatite 细胞并减少破骨细胞的数量,从而抑制异常骨吸收。 Etidronate 还可以直接刺激成骨细胞的骨形成。
T60554 Schnurri-3 inhibitor-1

Others Others
Schnurri-3 inhibitor-1 是有效的 schnurri-3 抑制剂,schnurri-3是成人骨形成的重要调节因子。在成骨细胞系 Shn3FFL 中,Schnurri-3 inhibitor-1 通过 EF1alpha 启动子抑制 Shn3 蛋白表达 (AC50= 2.09 μM)。Schnurri-3 inhibitor-1 可用于骨质疏松症相关的研究。
T26448 A 79175

A79175,A-79175

A 79175 is a 5-lipoxygenase inhibitor that increases bone formation.
T69837 YKL-05-093

YKL-05-093 is a alt inducible kinase (SIK) inhibitor. YKL-05-093 increases bone formation and bone mass.
T69974 Phenamil

Phenamil is an irreversible inhibitor of amiloride-sensitive Na channels; derivative of amiloride, synergizing bone formation with BMP2 and inhibits BMP2 induced cyst-like bone formation.
T31940 Glucosylgalactosylhydroxylysine

Hydroxylysine-glucose-galactose

Glucosylgalactosylhydroxylysine is a bone formation and bone resorption marker that is related to bone turnover processes during growth and development as well as metabolic bone diseases.
T70872 Smurf1 inhibitor 1

Smurf1 inhibitor 1 is a inhibitor that promotes bone formation.
T36065 N-Oleoyl-L-Serine

Bone mass and shape is continuously remodeled by the concerted and balanced action of osteoblasts (bone forming cells) and osteoclasts (bone-resorbing cells). The endocannabinoid system plays an essential role in the maintenance of normal bone mass via signaling through the CB2 receptor. N-Oleoyl-L-serine is an endogenous lipid that has been reported to stimulate bone formation and to inhibit bone resorption.
T69793 VEL-0230

VEL-0230, also known as NC-2300, is a potent cathespin K inhibitor. VEL-0230 has dual-acting properties that both stimulates bone formation and inhibits loss. VEL-0230 is being studied preclinically for the treatment of diseases involving bone mineral disorders such as bone loss related to multiple myeloma, osteoporosis, bone metastases, and rheumatoid arthritis. Velcura Therapeutics is currently being developed by Velcura Therapeutics. Given VEL- 0230's promotion of bone formation, inhibition o...
T69656 E197

E197 is a DOCK5 inhibitor. E197 can inhibit both mouse and human osteoclast activity. In particular, E197 prevented pathological bone loss in mice. Most interestingly, treatment with E197 did not affect osteoclast and osteoblast numbers and hence did not impair bone formation. E197 could represent a lead molecule to develop new antiosteoporotic drugs targeting the mechanism of osteoclast adhesion onto the bone.
T78278 Blosozumab

Blosozumab (LY2541546)为针对人sclerostin (SOST)的单克隆抗体。它能促进骨生成,同时抑制骨吸收,可应用于骨质疏松症相关研究。
T74736 2MD

2MD是一种口服活性维生素D类似物,能刺激骨膜骨形成并减少小梁骨吸收,从而恢复小梁和皮质骨的质量与强度。在非人灵长类动物研究中,2MD还可以调节(IOP)相关基因,降低眼压。
T69755 Evatanepag sodium

Evatanepag, also known as CP-533536, is an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation. CP-533536 demonstrated the ability to heal fractures when administered locally as a single dose in rat models of fracture healing.
T36080 Rivenprost

ONO-4819

Prostaglandin E2 activates four distinct G protein-coupled receptors, EP1-4. Rivenprost is a potent and selective agonist for the EP4 receptor (Ki = 0.7, 56, 620, and >10,000 nM for EP4, EP3, EP2, and EP1, respectively). It has been used to promote EP4-mediated bone formation, prevent bone loss related to osteoporosis, drive osteoblast differentiation, and stabilize bone implants.[1][2][3][4][5] Rivenprost has also been used to support wound healing.[6]
T81350 pTH-Related Protein (1-37) (human, mouse, rat)

pTH-Related Protein (1-37) (human, mouse, rat) 为甲状旁腺相关蛋白 (pTHrP) 的肽段,涉及骨形成的生理调控过程。
T80529 VnP-16

Integrin Cytoskeletal Signaling
VnP-16 通过直接作用于β1整合素 (β1 integrin),激活FAK,促进成骨细胞分化和活性,加速骨形成。
T76657 Human PTH-(1-31)

Human PTH-(1-31) 是人PTH的第1至31个氨基酸片段。它能够促进cAMP的释放,并作为25-羟基维生素D-1α-羟化酶的弱激活剂。此外,Human PTH-(1-31) 能够促进骨生成,而不引起骨质吸收,表明其在骨质疏松症研究中的应用潜力。
T76660 pTH (1-37) (human)

pTH (1-37) (human) 为甲状旁腺激素(PTH)的一段,能诱导cAMP产生并提升碱性磷酸酶活性,进而增强尿毒症动物的生长速度、骨钙含量及骨矿物质密度(BMD),显示出对骨质疏松症研究的应用潜力。
T37413 Calcitonin (salmon) (trifluoroacetate salt)

Calcitonin is a peptide hormone that lowers blood calcium level and inhibits bone resorption. It belongs to the calcitonin family of peptides, which also includes amylin , calcitonin gene-related peptide , and adrenomedullin. The binding of salmon calcitonin to the human calcitonin receptor (CTR) is not modulated by receptor activity-modifying proteins (RAMPs), which influence affinity of human calcitonin to CTR. Salmon calcitonin binds to human CTR2 with IC50 values of 0.933, 0.224, 0.134, and ...
T35582 H-Arg-Gly-Asp-Cys-OH (trifluoroacetate salt)

H-Arg-Gly-Asp-Cys-OH is a tetrapeptide that contains the arginine-glycine-aspartate (RGD) motif, a sequence that acts as a recognition site for various adhesion proteins.1It inhibits the binding of fibrinogen to endothelial cells and ADP-stimulated platelets with IC50values of 320 and 35 μM, respectively.2Implantation of titanium rods coated with H-Arg-Gly-Asp-Cys-OH increases bone formation in rat femurs.3H-Arg-Gly-Asp-Cys-OH has been conjugated to polyethylenimine to improve gene transfection ...
T73690 Abaloparatide

Abaloparatide (BA 058) 是一种甲状旁腺激素受体 1 (PTHR1) 类似物。Abaloparatide 也是一种选择性 PTHR1激活剂。Abaloparatide 增强 Gs/cAMP 信号和β-arrestin 募集。Abaloparatide 可增强小鼠的骨形成和皮质结构。Abaloparatide 具有用于骨质疏松症研究的潜力。
T37441 KMN-80

The prostaglandin E receptor 4 (EP4) is one of four G protein-coupled receptors that mediate the actions of prostaglandin E2 . Binding of PGE2 to the EP4 receptor causes an increase in intracellular cyclic AMP, which plays important roles in bone formation and resorption, cancer, and atherosclerosis. KMN-80 is a substituted γ-lactam (pyrrolidinone) derivative of PGE1 that acts as a selective and potent agonist of EP4 with an IC50 value of 3 nM (IC50 = 1.4 μM for EP3 and > 10 μM for all other pro...
T75765 GRGDSPK TFA

GRGDSPK TFA (EMD 56574 TFA) 是一种含有精氨酸-甘氨酸-天冬氨酸 (RGD) 序列的多肽。作为竞争性且可逆的抑制剂,它能够抑制整联蛋白与纤连蛋白的结合,用于探究整联蛋白在骨形成及吸收过程中的功能。
T68480 4SC-207

4SC-207 is a novel microtubule inhibitor , which shows strong anti-proliferative activity in a large panel of tumor cell lines with an average GI50 of 11 nM. In particular, 4SC-207 is active in multi-drug resistant cell lines, such as HCT-15 and ACHN, suggesting that it is a poor substrate for drug efflux pumps. 4SC-207 inhibits microtubule growth in vitro and in vivo and promotes, in a dose dependent manner, a mitotic delay/arrest, followed by apoptosis or aberrant divisions due to chromosome a...
T83849 OP-145 TFA

acetyl-IGKEFKRIVERIKRFLRELVRPLR-amide,P60.4-Ac

OP-145是一种合成抗菌肽及抗菌肽LL-37的衍生物。它对E. coli、P. aeruginosa、C. albicans和A. niger具有活性(MICs分别为2、3、6和18 µM)。含有OP-145的聚乳酸-共-聚乙二醇酸(PLGA)微球能够在骨折部位接种细菌后通过外科股骨骨折所诱导的小鼠骨感染模型中防止生物膜的形成。

化合物

Balicatib
Cat.No: T1850
Synonym: AAE581,巴利卡替
Target: Cysteine Protease
CYM 50769
Cat.No: T22702
Synonym:
Target: Neuropeptide W
Muramyl dipeptide
Cat.No: T16159
Synonym: MDP
Target: NOD
GRGDSPK
Cat.No: T7566
Synonym: EMD 56574
Target: Others
GRGDSPK acetate
Cat.No: T7566L1
Synonym: GRGDSPK acetate(111119-28-9 Free base)
Target: Beta Amyloid
XRK3F2
Cat.No: T13360
Synonym:
Target: Autophagy
WAY-262611
Cat.No: T1971
Synonym:
Target: Wnt/beta-catenin
Thonzonium Bromide
Cat.No: T2188
Synonym: 嘧苯十六铵,通佐溴胺
Target: Proton pump, Antibacterial, Autophagy
Evatanepag
Cat.No: T15259
Synonym: CP-533536 free acid,2-[3-[N-(4-叔丁基苄基)-N-(吡啶-3-基磺酰基)氨基甲基]苯氧基]乙酸
Target: Prostaglandin Receptor
Sodium etidronate
Cat.No: T1210
Synonym: 依替膦酸钠,Didronel
Target: Phosphatase
Schnurri-3 inhibitor-1
Cat.No: T60554
Synonym:
Target: Others
A 79175
Cat.No: T26448
Synonym: A79175,A-79175
Target:
YKL-05-093
Cat.No: T69837
Synonym:
Target:
Phenamil
Cat.No: T69974
Synonym:
Target:
Glucosylgalactosylhydroxylysine
Cat.No: T31940
Synonym: Hydroxylysine-glucose-galactose
Target:
Smurf1 inhibitor 1
Cat.No: T70872
Synonym:
Target:
N-Oleoyl-L-Serine
Cat.No: T36065
Synonym:
Target:
VEL-0230
Cat.No: T69793
Synonym:
Target:
E197
Cat.No: T69656
Synonym:
Target:
Blosozumab
Cat.No: T78278
Synonym:
Target:
2MD
Cat.No: T74736
Synonym:
Target:
Evatanepag sodium
Cat.No: T69755
Synonym:
Target:
Rivenprost
Cat.No: T36080
Synonym: ONO-4819
Target:
pTH-Related Protein (1-37) (human, mouse, rat)
Cat.No: T81350
Synonym:
Target:
VnP-16
Cat.No: T80529
Synonym:
Target: Integrin
Human PTH-(1-31)
Cat.No: T76657
Synonym:
Target:
pTH (1-37) (human)
Cat.No: T76660
Synonym:
Target:
Calcitonin (salmon) (trifluoroacetate salt)
Cat.No: T37413
Synonym:
Target:
H-Arg-Gly-Asp-Cys-OH (trifluoroacetate salt)
Cat.No: T35582
Synonym:
Target:
Abaloparatide
Cat.No: T73690
Synonym:
Target:
KMN-80
Cat.No: T37441
Synonym:
Target:
GRGDSPK TFA
Cat.No: T75765
Synonym:
Target:
4SC-207
Cat.No: T68480
Synonym:
Target:
OP-145 TFA
Cat.No: T83849
Synonym: acetyl-IGKEFKRIVERIKRFLRELVRPLR-amide,P60.4-Ac
Target:
Cat. No. Product Name Target Signaling Pathways
TN7036 N-(3-Methoxybenzyl)-(9Z,12Z,15Z)-octadecatrienamide

(9Z,12Z,15Z)-N-[(3-Methoxyphenyl)methyl]-9,12,15-octadecatrienamide,间-甲氧基苄基-亚麻酰胺,Macamide Impurity 14

Wnt/beta-catenin Cytoskeletal Signaling; Stem Cells
N-(3-Methoxybenzyl)-(9Z,12Z,15Z)-octadecatrienamide (Macamide Impurity 14) 是一种从玛卡中分离得到的玛卡酰胺。它能够激活典型的Wnt/β‐catenin 信号通路,诱导间充质干细胞成骨分化和随后的骨形成,可用于研究骨质疏松症。
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。
T3S2312 Poncirin

枸橘苷,Isosakuranetin-7-neohesperidoside

Apoptosis; Others Apoptosis; Others
Poncirin (Isosakuranetin-7-neohesperidoside) 是从三叶草中分离出来的一种天然产物,具有抗炎活性。 它防止脂肪生成,增强间充质干细胞中的成骨细胞分化,增加骨矿物质密度,改善小梁微结构,可能反映 GIO 小鼠的骨形成增加和骨吸收减少。
T3662 Eleutheroside E

NF-κB NF-κB
Eleutheroside E 是刺五加的重要成分,具有抗炎,保护缺血心脏的功能。
T3S1729 Dihydrolycorine

Others Others
Dihydrolycorine 是分离自Lycoris radiate 草药中,是一种真核细胞中蛋白质合成的抑制剂。
T7190 Actein

Apoptosis; Akt; JNK; Autophagy Apoptosis; Autophagy; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling
Actein 是从升麻的根茎中分离的一种三萜糖苷,通过促进ROS/JNK 活化和钝化人膀胱癌中的AKT 途径来抑制细胞增殖,诱导自噬和凋亡。
T6677 Sophocarpine

ERK; p38 MAPK; NF-κB; TLR; COX; HER; JNK; STAT Angiogenesis; Immunology/Inflammation; JAK/STAT signaling; MAPK; Neuroscience; NF-κB; Stem Cells; Tyrosine Kinase/Adaptors
Sophocarpine 是一种从传统草药苦参中提取的重要生物碱。苦参具有抗病毒、抗肿瘤和抗炎等多种药理作用。它通过多种机制显著抑制癌细胞的生长,具有抗肿瘤活性。
TMA0132 Dihydrophaseic acid

Others Others
Dihydrophaseic acid 3'-O-b-D-glucopyranoside (D3G) can increase the proliferation and differentiation of osteoblast cells and enhance bone formation, suggests that D3G may be a good candidate for the treatment of osteoporosis.
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.
TN3552 Byzantionoside B

Others Others
Byzantionoside B shows stimulatory activity on human osteoblast cells, it may have the potential to stimulate bone formation and regeneration.
TN1536 Curculigoside B

Others Others
Curculigoside B shows antioxidative and antiosteoporotic activities, it can decrease area of bone resorption pit, osteoclastic formation and TRAP activity.

天然产物

N-(3-Methoxybenzyl)-(9Z,12Z,15Z)-octadecatrienamide
Cat.No: TN7036
Synonym: (9Z,12Z,15Z)-N-[(3-Methoxyphenyl)methyl]-9,12,15-octadecatrienamide,间-甲氧基苄基-亚麻酰胺,Macamide Impurity 14
Target: Wnt/beta-catenin
3,7,4'-Trihydroxyflavone
Cat.No: TN2143
Synonym: Resokaempferol,5-Deoxykampferol
Target: DNA
Poncirin
Cat.No: T3S2312
Synonym: 枸橘苷,Isosakuranetin-7-neohesperidoside
Target: Apoptosis, Others
Eleutheroside E
Cat.No: T3662
Synonym:
Target: NF-κB
Dihydrolycorine
Cat.No: T3S1729
Synonym:
Target: Others
Actein
Cat.No: T7190
Synonym:
Target: Apoptosis, Akt, JNK, Autophagy
Sophocarpine
Cat.No: T6677
Synonym:
Target: ERK, p38 MAPK, NF-κB, TLR, COX, HER, JNK, STAT
Dihydrophaseic acid
Cat.No: TMA0132
Synonym:
Target: Others
2,3-Bis(3-indolylmethyl)indole
Cat.No: T38799
Synonym:
Target:
Byzantionoside B
Cat.No: TN3552
Synonym:
Target: Others
Curculigoside B
Cat.No: TN1536
Synonym:
Target: Others
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