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22

抑制剂 & 化合物

2

天然产物

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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)。
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。
T1137	Clorsulon 克洛索隆,L631529,MK401,氯舒隆	ATPase; Antibiotic; Parasite	Membrane transporter/Ion channel; Microbiology/Virology
	Clorsulon (L631529) 是一种具有口服活性的灭虫试剂，用于犊牛和羊的肝吸虫感染。它也是 3-磷酸甘酸酯和 ATP 的竞争性抑制剂，可抑制成熟肝片吸虫对葡萄糖的利用以及乙酸和丙酸的形成。
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
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。
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。
T3700	SCH900776 (S-isomer) MK-8776 S-isomer,SCH900776 S-isomer	Chk; CDK	Cell Cycle/Checkpoint
	SCH900776 S-isomer (MK-8776 S-isomer) 是SCH900776的S 型同分异构体。
T16096	Filorexant MK-6096	OX Receptor	GPCR/G Protein; Neuroscience
	Filorexant (MK-6096) 是一种口服有效且选择性可逆的 OX1 和 OX2 受体拮抗剂，Ki 值小于3nM。
T2517	SCH900776 MK 8776,MK-8776	Chk; CDK	Cell Cycle/Checkpoint
	SCH900776 (MK-8776) 是一种靶向细胞周期检查点激酶 1(Chk1) 的抑制剂，IC50值为 3 nM。它比对 CDK2 和 Chk2 的选择性分别高 50 和 500 倍，具有潜在的放射增敏和化学增敏活性。
T2650	MK-8245	Dehydrogenase; Stearoyl-CoA Desaturase (SCD)	Metabolism
	MK8245 是肝靶向的硬脂酰 -CoA 去饱和酶(SCD)抑制剂，对人 SCD1 和鼠 SCD1 的IC50值分别为 1 nM 和 3 nM，具有抗糖尿病和抗血脂异常的作用。
T6893	MK-886 MK886,L 663536	Apoptosis; Leukotriene Receptor; COX; PPAR; FLAP	Apoptosis; DNA Damage/DNA Repair; GPCR/G Protein; Immunology/Inflammation; Metabolism; Neuroscience
	MK-886 (L 663536)是一种细胞可渗透的，具有口服活性的 FLAP (IC50为 30 nM) 和白三烯生物合成 (完整白细胞和人全血中的IC50分别为 3 nM 和 1.1μM) 的抑制剂。它也是一种非竞争性PPARα拮抗剂，可以诱导细胞凋亡。
T12062	MK-4074	Others	Others
	MK-4074 is a liver-specific acetyl-CoA carboxylase ACC1 and ACC2 inhibitor(IC50 of 3 nM).
T35052	Vibegron MK4618,MK 4618,MK-4618
	Vibegron (MK-4618) is an effective and selective Beta 3 adrenergic receptor agonist, used to treat overactive bladder (OAB).
T33439	MK-7725 MK7725
	Mk-7725 is an effective selective bombesin receptor subtype 3 agonist for the treatment of obesity.
T2126	MK-5046	Bombesin Receptor	GPCR/G Protein
	MK5046是一种新型 BRS-3激动剂，同BRS-3结合 (鼠 Ki = 1.6 nM, 人 Ki = 25 nM)的亲和力高。
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。
T38844	MK-8245 Trifluoroacetate
	MK-8245 trifluoroacetate is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy. IC50 value: 1 nM (hSCD1) Target: SCD1 in vitro: MK-8245, a phenoxy piperidine isoxazole derivative, has been identified as a potent and liver-specific SCD inhibitor. It contains a tetrazole acetic acid moiety, which is the key molecule for OATPs recognition and liver-targeting. MK...
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).
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。
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。

化合物

MK2-IN-3 hydrate

Cat.No: T12058

Synonym: MK-2 Inhibitor III

Target: ERK, MAPK, MNK

Cat.No: T9034

Synonym: MK2 Inhibitor III

Target: MAPK

Cat.No: T1137

Synonym: 克洛索隆,L631529,MK401,氯舒隆

Target: ATPase, Antibiotic, Parasite

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

Cat.No: T31813

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

Cat.No: T4106

Synonym: MK8617

Target: HIF/HIF Prolyl-Hydroxylase

Cat.No: T6032

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

Target: Epigenetic Reader Domain

SCH900776 (S-isomer)

Cat.No: T3700

Synonym: MK-8776 S-isomer,SCH900776 S-isomer

Target: Chk, CDK

Cat.No: T16096

Synonym: MK-6096

Target: OX Receptor

Cat.No: T2517

Synonym: MK 8776,MK-8776

Target: Chk, CDK

Cat.No: T2650

Target: Dehydrogenase, Stearoyl-CoA Desaturase (SCD)

Cat.No: T6893

Synonym: MK886,L 663536

Target: Apoptosis, Leukotriene Receptor, COX, PPAR, FLAP

Cat.No: T12062

Target: Others

Cat.No: T35052

Synonym: MK4618,MK 4618,MK-4618

Cat.No: T33439

Synonym: MK7725

Cat.No: T2126

Target: Bombesin Receptor

Cat.No: T82414

Synonym: MK-4280

MK-8245 Trifluoroacetate

Cat.No: T38844

Cat.No: T37423

Finasteride acetate

Cat.No: T21668

Cat.No: T76800

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。
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

Cat.No: T13555

Synonym: Ascaroside C6

Target: Others

Cat.No: T37008

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