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36

抑制剂 & 化合物

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天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T67925	Nampt activator-1	NAMPT	Metabolism
	NAMPT activator-1 (compound 1) 是一种有效的、专用范围广泛的烟酰胺磷酸基转移酶 (NAMPT) 激活剂(EC50 为3.3-3.7 μM)。NAMPT activator-1能有效保护培养细胞免受 fk866介导的毒性，是神经保护的潜在化合物。
T12171	Nampt-IN-5	P450; NAMPT	Metabolism
	Nampt-IN-5 是烟酰胺磷酸核糖基转移酶抑制剂。它可抑制 A2780 和 COR-L23 细胞，IC50值分别为 0.7 nM 和 3.9 nM。它还抑制 CYP3A4 活性。
T4376	Nampt-IN-1 LSN3154567	c-Fms; NAMPT; CSF-1R	Metabolism; Tyrosine Kinase/Adaptors
	Nampt-IN-1 (LSN3154567) 是选择性的 NAMPT 抑制剂，能够抑制纯化的 NAMPT，IC50=3.1 nM。
T72617	Nampt activator-2	P450; NAMPT	Metabolism
	Nampt activator-2 是一种 NAMPT 激活剂（EC50 ： 0.023 μM）。 Nampt activator-2 对 CYP2C9、2D6、2C19 具有亲和力，亲和力数值分别为 0.060 μM、 0.41 μM 和 0.59 μM 。Nampt activator-2 可用来研究动脉粥样硬化，肥胖，II型糖尿病，胰岛素抵抗和I型糖尿病。
T13792	Nampt-IN-3	Others	Others
	Nampt-IN-3 simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and HDAC (IC50s of 31 nM and 55 nM, respectively).
T18477	NAMPT inhibitor-linker 1	Others	Others
	NAMPT inhibitor-linker 1, a drug-linker conjugate for ADC, integrates an NAMPT inhibitor (as a payload) with a linker. In the formulation of ADC-3, it pairs with an anti-c-Kit monoclonal antibody, demonstrating strong efficacy against c-Kit expressing cell lines, specifically GIST-T1 and NCI-H526, where it exhibits IC50 values of <3 pM and 9 pM, respectively.
T18478	NAMPT inhibitor-linker 2	Others	Others
	NAMPT inhibitor-linker 2, a drug-linker conjugate for antibody-drug conjugates (ADCs), comprises an NAMPT inhibitor payload and a linker. When combined with an anti-c-Kit monoclonal antibody to form ADC-4, it demonstrates potent efficacy against c-Kit expressing cell lines, including GIST-T1 and NCI-H526, with IC50 values of <7 pM and 40 pM, respectively.
T61597	Nampt-IN-7
	Nampt-IN-7, also known as compound GF8, is a powerful NAMPT inhibitor exhibiting an IC50 value of 7.31 μM. It possesses significant cytotoxic effects against the human HepG2 hepatocellular carcinoma cell line, with an IC50 value of 24.28 μM [1].
T74615	NAMPT degrader-1
	NAMPTdegrader-1 (Compound A3) 是一种酰胺磷酸核糖转移酶 (NAMPT) 降解剂，IC50为 0.023 μM。NAMPTdegrader-1 通过 autophagy-lysosomal 途径显著诱导 NAMPT 降解，表现出良好的细胞抗肿瘤能力。
T64057	Nampt-IN-8
	Nampt-IN-8 是一种 NAMPT 抑制剂 (IC50: 0.183 μM)，也是较好的 NQO1 底物。Nampt-IN-8 能够诱导活性氧 (ROS) 产生，并促使细胞凋亡 (apoptosis) 。
T62748	Nampt-IN-9
	Nampt-IN-9 (Compound 8) 是一种有效的 NAMPT 抑制剂，具有抗癌作用。Nampt-IN-9 能够用于研究胰腺导管腺癌。
T75023	Nampt degrader-2
	Namptdegrader-2 是一种荧光PROTAC，可有效降解NAMPT，IC50为 41.9 nM。Namptdegrader-2 与NAMPT 和 VHL 结合形成三元复合物，随后通过泛素-蛋白酶体系统 (UPS) 诱导NAMPT 降解。Namptdegrader-2 导致 NAD+显着减少并发挥有效的抗肿瘤活性。
T79437	NAMPT degrader-3	NAMPT	Metabolism
	NAMPTdegrader-3 (compound C5)，是一种依赖VHL和蛋白酶体途径降解NAMPT的化合物。该化合物展现出对A2780细胞的细胞毒性作用，并能抑制其增殖。
T72623	Nampt activator-3
	NAMPTactivator-3 是一种 NAT 衍生物，是一种 NAMPT 激活剂，EC50为 2.6 μM，KD 为 132 nM。NAMPTactivator-3 有效保护培养细胞免受 FK866 介导的毒性。NAMPTactivator-3 在化疗引起的周围神经病变 (CIPN) 小鼠模型中表现出强大的神经保护功效，没有任何明显的毒性。
T74562	Nampt-IN-10 trihydrochloride
	Nampt-IN-10 trihydrochloride (compound 4) 为磷酸核糖转移酶 (NAMPT) 抑制剂。在A2780与CORL23细胞中展现出活性，IC50值依次为5和19 nM。Nampt-IN-10 trihydrochloride 同时作为抗体偶联活性分子 (ADC) 的非限制性有效载荷。
T64273	Nampt-IN-10 TFA
	Nampt-IN-10 TFA (compound 4) 是一种磷酸核糖转移酶 (NAMPT) 抑制剂。Nampt-IN-10 TFA 对 A2780 (IC50: 5 nM) 和 CORL23 (IC50: 19 nM) 具有细胞效能。Nampt-IN-10 TFA 能够用做 ADCs 的非抗有丝分裂有效载荷。
T4335	GNE-617 GNE617	NAMPT	Metabolism
	GNE-617 是一种新型的、特异性的Nampt 抑制剂，在A549细胞中IC50为18.9nM。
T6682	STF-118804 STF 118804,STF118804	Apoptosis; NAMPT	Apoptosis; Metabolism
	STF-118804是一种烟酰胺磷酸核糖基转移酶 Nampt 高选择性抑制剂，降低大多数 B-ALL 细胞系的活力，IC50 <10 nM。
T1998	CHS-828 CHS 828,GMX1778	Apoptosis; NAMPT	Apoptosis; Metabolism
	CHS-828 (GMX1778) 是一种竞争性的烟酰胺磷酸化转移酶抑制剂，IC50值 <25 nM。它通过降低细胞中的 NAD+水平发挥细胞毒性作用，具有抗癌活性。
T12854	SBI-797812	NAMPT	Metabolism
	SBI-797812 是在结构上类似于活性位点定向的 NAMPT 抑制剂的化合物，能够阻断这些抑制剂与 NAMPT 的结合。它将 NAMPT 反应平衡转向 NMN 形成，提高 NAMPT 对 ATP 的亲和力，稳定 His247 处的磷酸化 NAMPT，增加焦磷酸盐副产物的消耗，并通过 NAD+钝化反馈抑制。
T2644	(E)-Daporinad Daporinad,(E)-N-[4-(1-BENZOYL-PIPERIDIN-4-YL)-BUTYL]-3-PYRIDIN-3-YL-ACRYLAMIDE,APO866,FK866,达珀利奈	NAMPT; Transferase; Autophagy	Autophagy; Metabolism
	(E)-Daporinad (FK866) 是一种烟酰胺磷酸核糖基转移酶的小分子抑制剂，具有潜在的抗肿瘤和抗血管生成活性，IC50为 0.09 nM。
T4354	KPT9274 KPT-9274,KPT 9274,PAK4-IN-1	NAMPT; PAK	Cytoskeletal Signaling; Metabolism
	KPT9274 (PAK4-IN-1) 是一种非竞争性的 PAK4 和 NAMPT 双重抑制剂（IC50= ~120 nM）。它是一种口服生物可利用的小分子。
T11823	LB-60-OF61	NAMPT	Metabolism
	LB-60-OF61 是一种 NAMPT 抑制剂，是一种对对 MYC 癌基因的依赖性癌细胞株显示出抗增殖活性。
T26254	Teglarinad chloride GMX 1777 chloride,EB1627,GMX1777,GMX1777 chloride,GMX 1777,GMX-1777 chloride,EB-1627,EB-1627 chloride,EB1627 chloride	NAMPT	Metabolism
	Teglarinad chloride (GMX-1777 chloride) 是一种有效的 NAMPT 的抑制剂，是 GMX1778 的前体。Teglarinad chloride 具有抗肿瘤活性，通过干扰 DNA 修复和抑制血管生成来发挥作用。
T12330	OT-82	NAMPT	Metabolism
	OT-82 is a potent, selective and orally active NAMPT inhibitor.
T62938	GNE-617 hydrochloride
	GNE-617 hydrochloride 是一种 NAMPT 的特异性抑制剂，能够抑制 NAMPT 活性 (IC50: 5 nM)。
T22804	GPP 78 hydrochloride (1202580-59-3 free base) GPP 78 hydrochloride	Others	Others
	NAMPT inhibitor
T70833	A-1293201
	A-1293201 is a potent and selective NAMPT inhibitor.
T14882	CB30865 ZM 242421	Others	Others
	CB30865 is a potent inhibitor of Nampt, an enzyme present in the NAD biosynthetic pathway.
T60667	NAT
	NAT 是 NAMPT 激活剂的苗头化合物。NAMPT 是研究与 NAD 耗竭相关的许多疾病，例如如神经退行性疾病的有吸引力的靶点，由于其为 NAD 回收途径中的限速酶。
T36874	7-Bromoheptanoic Acid
	7-Bromoheptanoic acid is a building block.1,2It has been used in the synthesis of azide-based nicotinamide phosphoribosyltransferase (Nampt) inhibitors with anticancer activity and SAHA derivatives that inhibit histone deacetylases (HDACs). 1.Colombano, G., Travelli, C., Galli, U., et al.A novel potent nicotinamide phosphoribosyltransferase inhibitor synthesized via click chemistryJ. Med. Chem.53(2)616-623(2010) 2.Suzuki, T., Nagano, Y., Kouketsu, A., et al.Novel inhibitors of human histone deac...
T15412	GPP78 CAY10618	Autophagy	Autophagy
	GPP78 is a potent inhibitor of Nampt (IC50: 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion). GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells (IC50: 3.8 nM by inducing autophagy). GPP78 has anti-cancer and anti-inflammatory effect
T40855	LB-60-OF61 hydrochloride LB-60-OF61 hydrochloride
	LB-60-OF61 hydrochloride is a highly effective inhibitor of NAMPT, a key enzyme involved in the transfer of nicotinamide phosphoribosyl groups. This compound, known for its cytotoxic properties, specifically targets cell lines that overexpress MYC, thereby demonstrating selectivity in its action.
T37578	GPP 78 hydrochloride
	GPP 78 hydrochloride 是一种有效的烟酰胺磷酸核糖转移酶 (Nampt) 抑制剂，对 NAD 消耗的 IC50 为 3 nM。GPP 78 hydrochloride 通过诱导自噬对神经母细胞瘤细胞 SH-SY5Y 具有毒性，IC50 为 3.8 nM。GPP78 具有抗癌和抗炎作用。
T71361	CHS-828 nicotinate
	CHS-828 nicotinate is a CHS-828 salt with Nicotinic acid.. CHS-828 also known as GMX-1778, is a potent and selective NAMPT inhibitor. CHS-828 inhibits cellular synthesis of NAD. CHS 828 kill tumour cells by inhibiting the nuclear factor-kappaB translocation but unlikely through down-regulation of proteasome. CHS 828 has shown promising anticancer activity in experimental tumor models and primary cultures of cancer cells from patients. CHS 828 showed a synergistic effect with melphalan in 67%, ...
T15403	GNE-618	NAMPT	Metabolism
	GNE-618 is a potent and orally active inhibitor of nicotinamide phosphoribosyltransferase (IC50: 6 nM). GNE-618 depletes NAD levels and induces tumor cell death. It has anti-tumor activity.

化合物

Nampt activator-1

Cat.No: T67925

Target: NAMPT

Cat.No: T12171

Target: P450, NAMPT

Cat.No: T4376

Synonym: LSN3154567

Target: c-Fms, NAMPT, CSF-1R

Nampt activator-2

Cat.No: T72617

Target: P450, NAMPT

Cat.No: T13792

Target: Others

NAMPT inhibitor-linker 1

Cat.No: T18477

Target: Others

NAMPT inhibitor-linker 2

Cat.No: T18478

Target: Others

Cat.No: T61597

NAMPT degrader-1

Cat.No: T74615

Cat.No: T64057

Cat.No: T62748

Nampt degrader-2

Cat.No: T75023

NAMPT degrader-3

Cat.No: T79437

Target: NAMPT

Nampt activator-3

Cat.No: T72623

Nampt-IN-10 trihydrochloride

Cat.No: T74562

Nampt-IN-10 TFA

Cat.No: T64273

Cat.No: T4335

Synonym: GNE617

Target: NAMPT

Cat.No: T6682

Synonym: STF 118804,STF118804

Target: Apoptosis, NAMPT

Cat.No: T1998

Synonym: CHS 828,GMX1778

Target: Apoptosis, NAMPT

Cat.No: T12854

Target: NAMPT

Cat.No: T2644

Synonym: Daporinad,(E)-N-[4-(1-BENZOYL-PIPERIDIN-4-YL)-BUTYL]-3-PYRIDIN-3-YL-ACRYLAMIDE,APO866,FK866,达珀利奈

Target: NAMPT, Transferase, Autophagy

Cat.No: T4354

Synonym: KPT-9274,KPT 9274,PAK4-IN-1

Target: NAMPT, PAK

Cat.No: T11823

Target: NAMPT

Teglarinad chloride

Cat.No: T26254

Synonym: GMX 1777 chloride,EB1627,GMX1777,GMX1777 chloride,GMX 1777,GMX-1777 chloride,EB-1627,EB-1627 chloride,EB1627 chloride

Target: NAMPT

Cat.No: T12330

Target: NAMPT

GNE-617 hydrochloride

Cat.No: T62938

GPP 78 hydrochloride (1202580-59-3 free base)

Cat.No: T22804

Synonym: GPP 78 hydrochloride

Target: Others

Cat.No: T70833

Cat.No: T14882

Synonym: ZM 242421

Target: Others

Cat.No: T60667

7-Bromoheptanoic Acid

Cat.No: T36874

Cat.No: T15412

Synonym: CAY10618

Target: Autophagy

LB-60-OF61 hydrochloride

Cat.No: T40855

Synonym: LB-60-OF61 hydrochloride

GPP 78 hydrochloride

Cat.No: T37578

CHS-828 nicotinate

Cat.No: T71361

Cat.No: T15403

Target: NAMPT

Cat. No.	Product Name	Target	Signaling Pathways
T4721	β-Nicotinamide mononucleotide β-NM,β烟酰胺单核苷酸,烟酰胺单核苷酸	Others; Endogenous Metabolite	Metabolism; Others
	β-Nicotinamide mononucleotide (β-NM) 是烟酰胺磷酸核糖转移酶 (NAMPT) 反应的产物。β-nicotinamide mononucleotide 的作用包括其在细胞生化功能、心脏保护、糖尿病、肥胖相关并发症和阿尔茨海默病中的作用。

天然产物

β-Nicotinamide mononucleotide

Cat.No: T4721

Synonym: β-NM,β烟酰胺单核苷酸,烟酰胺单核苷酸

Target: Others, Endogenous Metabolite

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