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41

抑制剂 & 化合物

3

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Cat. No. Product Name Target Signaling Pathways
T12058 MK2-IN-3 hydrate

MK-2 Inhibitor III

ERK; MAPK; MNK MAPK
MK2-IN-3 hydrate (MK-2 Inhibitor III) 是一种口服有活性的、ATP 竞争性的MAPKAP-K2 (MK-2)选择性抑制剂(IC50:0.85 nM)。
T4442 MK2-IN-1 hydrochloride

MK2 Inhibitor,MK 25

MAPK MAPK
MK2-IN-1 hydrochloride (MK 25) 是一种高效的选择性 MAPKAPK2(MK2)激酶抑制剂,其 IC50值为0.11uM。
T9034 MK2-IN-3

MK2 Inhibitor III

MAPK MAPK
MK2-IN-3 (MK2 Inhibitor III) 是选择性的 MAPKAP-K2 (MK-2)抑制剂(IC50:8.5 nM),能够抑制 U937 细胞及体内 TNFα 的生成。
T22988 MK-4827 Racemate

Niraparib Racemate,2-(4-piperidin-3-ylphenyl)indazole-7-carboxamide

PARP Chromatin/Epigenetic; DNA Damage/DNA Repair
MK-4827 Racemate (Niraparib Racemate) 是一种选择性 PARP1 和 PARP2 抑制剂,IC50 分别为 3.8 nM 和 2.1 nM,对 PARP3、V-PARP 和 Tank1 的选择性超过 330 倍。
T15212 Emamectin Benzoate

MK-244,甲胺基阿维菌素苯甲酸盐

Apoptosis; Reactive Oxygen Species; GABA Receptor; Parasite Apoptosis; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience; NF-κB
Emamectin Benzoate (MK-244) 是口服有效的神经系统毒物,其通过结合昆虫中的 GABA 受体发挥作用。它是阿维菌素的半合成衍生物之一,具有广谱的杀虫和杀螨活性。它诱导ROS 介导的 DNA 损伤和细胞凋亡。
T31813 Fludalanine

MK641,D-Alanine-2-d, 3-fluoro-,3-Fluoro-D-(2-2H)alanine

Fludalanine (MK641), an analogue of D-alanine, irreversiably inactivates racemase and also inhibits synthase. When used in combination with cycloserine, it has been found to be more active against a variety of non-mycobacterium organisms than fludalanine
T36778 MK2-IN-1

MK2-IN-1 (MK2 Inhibitor)

MK2-IN-1 is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode.
T3722 MK-1064

Urokinase inhibitor 1,MK 1064

OX Receptor GPCR/G Protein; Neuroscience
MK-1064 (Urokinase inhibitor 1) 是一种选择性食欲素 2 (2-SORA)受体拮抗剂,可用于失眠患者的研究。
T2316 Omarigliptin

MK-3102,奥格列汀

Proteasome; DPP-4 Proteases/Proteasome; Ubiquitination
Omarigliptin (MK-3102) 是高效选择性 DPP4抑制剂,IC50=为1.6nM。
T3148 MK-571 sodium

L-660711 (sodium salt),L-660711 sodium salt,Verlukast sodium,L-660711,MK571,MK-571 sodium salt,Propanoic acid

Leukotriene Receptor; LTR GPCR/G Protein; Immunology/Inflammation
MK-571 sodium (L-660711 sodium salt) 是一种可口服的选择性白三烯 D4受体拮抗剂,在豚鼠和人肺膜的 Ki 分别为0.222.1 nM。
T12069 MK-8353

SCH900353

ERK MAPK
MK-8353 (SCH900353) 是口服有效的ERK1/2选择性抑制剂,IC50分别为 23.0 nM 和 8.8 nM。它显示出抗肿瘤活性。
T6032 Birabresib

OTX-015,OTX015 (MK 8628/Birabresib),MK-8628

Epigenetic Reader Domain Chromatin/Epigenetic
Birabresib (MK-8628) 是一种 BRD2/3/4抑制剂,IC50值为 92 到 112 nM 之间,具有潜在的抗肿瘤活性。
T0242L Sitagliptin phosphate monohydrate

MK-0431,MK-0431 phosphate monohydrate,西他列汀磷酸盐一水合物

Proteasome; DPP-4; Autophagy Autophagy; Proteases/Proteasome; Ubiquitination
Sitagliptin phosphate monohydrate (MK-0431 phosphate monohydrate) 是一种有效的 DPP-IV 抑制剂,在 Caco-2 细胞提取物中的 IC50 为 19 nM。
T1913 MK-3697

OX Receptor GPCR/G Protein; Neuroscience
MK3697是OX2受体的一种高效选择性拮抗剂,Ki 值为0.95nM。
T22986 MK 1903

GPR Endocrinology/Hormones; GPCR/G Protein
MK 1903 是一种有效的、具有选择性的羟基羧酸受体2 (HCA2) 的完全激动剂。HCA2也叫做G 蛋白偶联受体109A(GPR109A) 。MK 1903在使用表达人受体(ECso-12.9 nM)的 CHO 细胞进行的均匀时间分辨荧光(htf)测定中,它减少了福斯克林诱导的 cAMP 的产生。
T23358 Sitagliptin phosphate

磷酸西他列汀,Januvia,MK-0431 phosphate,Sitagliptin (phosphate)

DPP-4; Autophagy Autophagy; Proteases/Proteasome
Sitagliptin phosphate (MK-0431 phosphate) 是一种二肽基肽酶 4 (DPP4) 抑制剂,在 Caco-2 细胞中,IC50值为 19 nM。
T4106 MK-8617

MK8617

HIF/HIF Prolyl-Hydroxylase Chromatin/Epigenetic; Metabolism
MK-8617 是一种口服具有活力的低氧诱导因子脯氨酰羟化酶 1-3 (HIF PHD1-3) 泛抑制剂,对于PHD2的IC50=1 nM。
T12056 MK-0941 free base

Glucokinase Metabolism
MK-0941 free base 是一种口服具有活力的葡糖激酶抑制剂,在葡萄糖浓度为 2.5 和 10 mM 的条件下,对重组人 glucokinase 的EC50值分别为 240 和 65 nM。它具有较强的降血糖特性,是研究 2 型糖尿病的候选药物。
T1574 Etoricoxib

Arcoxia,MK-663,Tauxib,L-791456,Nucoxia,Desvenlafaxine,依托考昔

COX Immunology/Inflammation; Neuroscience
Etoricoxib (MK-663) 是一种合成的非甾体抗炎药 (NSAID),具有解热、镇痛和潜在的抗肿瘤特性。它是可口服的选择性 COX-2抑制剂,对人全血 COX-2 和 COX-1 的 IC50值分别为 1.1 和 116 μM。
T7130 Navarixin

MK-7123,SCH 527123

CXCR Autophagy; GPCR/G Protein; Immunology/Inflammation
Navarixin (MK-7123) 是一种可口服的 CXCR1和 CXCR2变构拮抗剂,对猕猴 CXCR1的 Kd 值为 41 nM,对大小鼠和猕猴 CXCR2的 Kd 值分别为 0.20、0.20 和 0.08 nM。
T60951 Molnupiravir

EIDD-2801,Lagevrio,MK-4482

SARS-CoV; Influenza Virus Microbiology/Virology
Molnupiravir (MK-4482) (EIDD-2801) 是核糖核苷类似物 EIDD-1931 的异丙酯前体药物,具有口服生物利用度。Molnupiravir 可用于 COVID-19 ,季节性和流行性流感的研究,对多种冠状病毒和流感病毒具有广谱的抗病毒活性,例如,SARS-CoV-2,MERS-CoV,SARS-CoV。
T4547 Grazoprevir

MK-5172

HCV Protease; SARS-CoV Microbiology/Virology; Proteases/Proteasome
Grazoprevir (MK-5172) 是一种丙型肝炎病毒 NS3/4a 蛋白酶的选择性抑制剂,具有跨基因型和耐药变体的广泛活性,对 gt1b、gt1a、gt2a、gt2b 和 gt3a 的Ki 分别为 0.01 nM、0.01 nM、0.08 nM、0.15 nM 和 0.90 nM。它也是 SARS-CoV-2 3CLpro 抑制剂。
T1185 Rofecoxib

MK 966,罗非昔布,罗非考昔,MK-0966

COX Immunology/Inflammation; Neuroscience
Rofecoxib (MK 966) 是可口服的 COX-2特异性抑制剂,具有抗炎、解热和镇痛特性以及潜在的抗肿瘤特性。在人骨肉瘤细胞和中国仓鼠卵巢细胞中,对人 COX-2 的 IC50值分别为 26 和 18 nM。
T28060 MK-8133

MK-8133 is an antagonist of orexin-2 selective receptor with favorable development properties.
T28052 MK-0703

L-791515,MK0703,L791515,MK 0703,L 791515

MK-0703 is a selective cyclooxygenase-2 inhibitor.
T75883 Agitoxin-2 TFA

Agitoxin-2 TFA 是K+通道的阻断剂,其对 mKV1.3 和 mKV1.1 的IC50值分别为 201 pM 和 144 pM。
T6590 MK-3207 Hydrochloride

MK-3207 HCl

CGRP Receptor GPCR/G Protein; Neuroscience
MK-3207 Hydrochloride (MK-3207 HCl) 是口服具有活力的CGRP receptor 拮抗剂,IC50=0.12 nM,Ki=0.024 nM。
T12057 MK-0941

Others Others
MK-0941 is an orally active and allosteric glucokinase activator, has potential in the treatment of type 2 diabetes.
T24479 MK-8282

MK 8282

MK-8282 is an effective G-Protein-Coupled Receptor 119 agonist for the treatment of Type 2 Diabetes.
T33423 MK-0916

MK 0916

MK-0916 is a 11β-hydroxysteroid dehydrogenase type 1 inhibitor indicated for the treatment of type 2 diabetes and metabolic syndrome as well as obesity-related diseases.
T21558 MK-3207

MK-3207是口服生物相容性的CGRP 受体拮抗剂,IC50和 Ki 分别为 0.12 nM 和 0.024 nM,对 AM1,AM2,CTR 和 AMY3 的抑制性较弱。MK-3207可用于偏头痛研究。
T68000 MK 0533

Mk-0533是一种选择性过氧化物酶体增殖激活受体γ调节剂,用于治疗2型糖尿病。
T70468 MK-8666

MK-8666 is a partial GPCR (G-protein-coupled receptor) agonist that is coordinated with the action of GPR40. GPR40, also known as free fatty acid (FFA) receptor 1 modulates fatty acid-induced insulin secretion in pancreatic beta cells and in intestinal enteroendocrine cells. Thus, MK-8666 has been investigated for treatment of type 2 diabetes mellitus and has been shown to robustly lower glucose without negative effects.
T33415 MK 0767

MK0767,MK-0767

MK 0767 is a dual peroxisome proliferator-activated receptor (PPAR) α/γ agonist that has been investigated as a potential treatment for type 2 diabetes and dyslipidemia.
T69953 MK-8666 Tris

MK-8666 Tris is a partial GPCR (G-protein-coupled receptor) agonist that is coordinated with the action of GPR40. GPR40, also known as free fatty acid (FFA) receptor 1 modulates fatty acid-induced insulin secretion in pancreatic beta cells and in intestinal enteroendocrine cells. Thus, MK-8666 Tris has been investigated for treatment of type 2 diabetes mellitus and has been shown to robustly lower glucose without negative effects.
T37423 Reveromycin D

Reveromycin D is a bacterial metabolite originally isolated from Streptomyces. It inhibits EGF-induced mitogenic activity in Balb/MK cells and has pH-dependent antifungal activity against C. albicans (MICs = 2 and >500 μg/ml at pH 3 and 7.4, respectively). Reveromycin D also inhibits proliferation of KB and K562 cells (IC50s = 1.6 and 1.3 μg/ml, respectively).
T82414 Favezelimab

MK-4280

Favezelimab(MK-4280)为人源化抗LAG-3单克隆抗体,能够抑制LAG-3与其配体MHC II类结合。该抗体联合PD-L1抑制剂Pembrolizumab在结直肠癌(CRC)治疗研究中展现出应用前景。
T76800 Dalotuzumab

Dalotuzumab (MK-0646) 是一种靶向IGF-1R 的重组人源化单克隆抗体 (IgG1 型)。Dalotuzumab 通过抑制IGF-1和IGF-2介导的肿瘤细胞增殖、IGF-1R 自体磷酸化和Akt 磷酸化而发挥作用。Dalotuzumab 还可诱导细胞凋亡和周期停滞。Dalotuzumab 与其他抗癌活性分子(如他汀类活性分子)共同使用,可增强 Dalotuzumab 的体外和体内抗肿瘤活性。
T81784 MK-2206 free base

Akt Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
MK-2206 free base是一种口服活性、高选择性的变构Akt抑制剂,IC50分别针对Akt1、Akt2、Akt3为8、12和65 nM 。多种乳腺癌细胞系、PIK3CA突变以及PTEN缺失细胞系对此化合物敏感,显示出抗癌活性。
T21668 Finasteride acetate

Finasteride (MK-906) acetate 是一种高效的5α-还原酶 (5α-reductase) 竞争性抑制剂,其对 II 型 5α-还原酶的IC50值仅为 4.2 nM,其对该型酶的亲和力是对 I 型酶亲和力的约100倍。因此,Finasteride acetate 主要在良性前列腺增生症 (BPH) 和雄激素性脱发研究领域中应用。
T61585 Sulindac sodium

Sulindac (sodium) (MK-231) 是一种非甾体抗炎剂,具有口服活性。Sulindac (sodium) 用于减轻疼痛,肿胀和关节僵硬的关节炎。Sulindac 还用于脊柱关节炎、痛风性关节炎的研究。Sulindac (sodium) 作为一种免疫调节剂,可通过阻断 NF-κB 信号通路下调 PD-L1,调节 pMMR CRC 对抗 PD-L1 免疫治疗的应答,抑制结直肠癌 CRC 的发生发展。 Sulindac 还可通过下调 SIRT1 抑制 TGF-β1-诱导的 EMT,抑制肺癌细胞的迁移和侵袭。

化合物

MK2-IN-3 hydrate
Cat.No: T12058
Synonym: MK-2 Inhibitor III
Target: ERK, MAPK, MNK
MK2-IN-1 hydrochloride
Cat.No: T4442
Synonym: MK2 Inhibitor,MK 25
Target: MAPK
MK2-IN-3
Cat.No: T9034
Synonym: MK2 Inhibitor III
Target: MAPK
MK-4827 Racemate
Cat.No: T22988
Synonym: Niraparib Racemate,2-(4-piperidin-3-ylphenyl)indazole-7-carboxamide
Target: PARP
Emamectin Benzoate
Cat.No: T15212
Synonym: MK-244,甲胺基阿维菌素苯甲酸盐
Target: Apoptosis, Reactive Oxygen Species, GABA Receptor, Parasite
Fludalanine
Cat.No: T31813
Synonym: MK641,D-Alanine-2-d, 3-fluoro-,3-Fluoro-D-(2-2H)alanine
Target:
MK2-IN-1
Cat.No: T36778
Synonym: MK2-IN-1 (MK2 Inhibitor)
Target:
MK-1064
Cat.No: T3722
Synonym: Urokinase inhibitor 1,MK 1064
Target: OX Receptor
Omarigliptin
Cat.No: T2316
Synonym: MK-3102,奥格列汀
Target: Proteasome, DPP-4
MK-571 sodium
Cat.No: T3148
Synonym: L-660711 (sodium salt),L-660711 sodium salt,Verlukast sodium,L-660711,MK571,MK-571 sodium salt,Propanoic acid
Target: Leukotriene Receptor, LTR
MK-8353
Cat.No: T12069
Synonym: SCH900353
Target: ERK
Birabresib
Cat.No: T6032
Synonym: OTX-015,OTX015 (MK 8628/Birabresib),MK-8628
Target: Epigenetic Reader Domain
Sitagliptin phosphate monohydrate
Cat.No: T0242L
Synonym: MK-0431,MK-0431 phosphate monohydrate,西他列汀磷酸盐一水合物
Target: Proteasome, DPP-4, Autophagy
MK-3697
Cat.No: T1913
Synonym:
Target: OX Receptor
MK 1903
Cat.No: T22986
Synonym:
Target: GPR
Sitagliptin phosphate
Cat.No: T23358
Synonym: 磷酸西他列汀,Januvia,MK-0431 phosphate,Sitagliptin (phosphate)
Target: DPP-4, Autophagy
MK-8617
Cat.No: T4106
Synonym: MK8617
Target: HIF/HIF Prolyl-Hydroxylase
MK-0941 free base
Cat.No: T12056
Synonym:
Target: Glucokinase
Etoricoxib
Cat.No: T1574
Synonym: Arcoxia,MK-663,Tauxib,L-791456,Nucoxia,Desvenlafaxine,依托考昔
Target: COX
Navarixin
Cat.No: T7130
Synonym: MK-7123,SCH 527123
Target: CXCR
Molnupiravir
Cat.No: T60951
Synonym: EIDD-2801,Lagevrio,MK-4482
Target: SARS-CoV, Influenza Virus
Grazoprevir
Cat.No: T4547
Synonym: MK-5172
Target: HCV Protease, SARS-CoV
Rofecoxib
Cat.No: T1185
Synonym: MK 966,罗非昔布,罗非考昔,MK-0966
Target: COX
MK-8133
Cat.No: T28060
Synonym:
Target:
MK-0703
Cat.No: T28052
Synonym: L-791515,MK0703,L791515,MK 0703,L 791515
Target:
Agitoxin-2 TFA
Cat.No: T75883
Synonym:
Target:
MK-3207 Hydrochloride
Cat.No: T6590
Synonym: MK-3207 HCl
Target: CGRP Receptor
MK-0941
Cat.No: T12057
Synonym:
Target: Others
MK-8282
Cat.No: T24479
Synonym: MK 8282
Target:
MK-0916
Cat.No: T33423
Synonym: MK 0916
Target:
MK-3207
Cat.No: T21558
Synonym:
Target:
MK 0533
Cat.No: T68000
Synonym:
Target:
MK-8666
Cat.No: T70468
Synonym:
Target:
MK 0767
Cat.No: T33415
Synonym: MK0767,MK-0767
Target:
MK-8666 Tris
Cat.No: T69953
Synonym:
Target:
Reveromycin D
Cat.No: T37423
Synonym:
Target:
Favezelimab
Cat.No: T82414
Synonym: MK-4280
Target:
Dalotuzumab
Cat.No: T76800
Synonym:
Target:
MK-2206 free base
Cat.No: T81784
Synonym:
Target: Akt
Finasteride acetate
Cat.No: T21668
Synonym:
Target:
Sulindac sodium
Cat.No: T61585
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T13555 Ascr#2

Ascaroside C6

Others Others
Ascr#2 (asc-C6-MK)是秀丽隐杆线虫中的糖苷类化合物,促进 dauer 形成。Ascr#2 在低浓度下与 ascr#3 的混合物可作为雄性引诱剂,可用于检测种群密度。
T75629 Ganoderic acid Mk

Ganoderic acid Mk (GA-Mk)为来源于灵芝菌丝的三萜酸类化合物,能有效抑制细胞增殖,并通过线粒体途径诱导HeLa细胞的细胞凋亡(apoptosis),在宫颈癌研究中具有应用价值。
T37008 Reveromycin A

Reveromycin A is the major component of a complex of spiroketal antibiotics isolated from Streptomyces sp. It inhibits the mitogenic activity of epidermal growth factor in Balb/MK cells (IC50 = 0.7 μg/ml), displays antiproliferative activity against human KB and K562 tumor cell lines (IC50s = 1.9 and 1.6 μg/ml, respectively), and demonstrates antifungal activity against C. albicans (MIC = 2 μg/ml at pH 3). Reveromycin A also has been shown to inhibit bone resorption by inducing apoptosis in oste...

天然产物

Ascr#2
Cat.No: T13555
Synonym: Ascaroside C6
Target: Others
Ganoderic acid Mk
Cat.No: T75629
Synonym:
Target:
Reveromycin A
Cat.No: T37008
Synonym:
Target:
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