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25

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T7581	voxelotor GBT 440	Others	Others
	Voxelotor (GBT 440) 是镰状血红蛋白 (HbS) 聚合抑制剂，有用于镰状细胞贫血病研究的潜力。
T21652	RN-1 dihydrochloride	Histone Demethylase; MAO	Chromatin/Epigenetic; Metabolism; Neuroscience
	RN-1 dihydrochloride 是血脑屏障通透性的、不可逆的赖氨酸特异性脱甲基酶 1 (LSD1) 选择性抑制剂，IC50为 70 nM，对 LSD1 的选择性高于 MAO-A 和 MAO-B，IC50分别为 0.51 μM 和 2.785 μM。
T35044	Velaresol BW 12C79,BW 12C,BW-12C79,BW12C79,BW-12C
	Velaresol (BW12C, BW12C79) is an oxygenated hemoglobin stabilizer that, in addition to stabilizing oxygenated hemoglobin, protects sickle cells from calcium-mediated dehydration.
T3528	Senicapoc 塞尼卡泊,ICA-17043	Potassium Channel	Membrane transporter/Ion channel
	Senicapoc (ICA-17043) 是有效的，选择性的Gardos 通道 (Ca2+激活的 K+通道;KCa3.1) 阻断剂，IC50为 11 nM。Senicapoc 阻断人红细胞的 Ca2+诱导的铷通量，IC50为 11 nM，抑制红细胞脱水的IC50为 30 nM。
T77399	Crizanlizumab ADAKVEO,SEG-101	Others	Others
	Crizanlizumab（Adakveo）是一种针对 P-选择素的人源化单克隆抗体，用于预防镰状细胞病的疼痛危象。
T2044	Varespladib LY315920,伐瑞拉地,伐瑞拉迪	Phospholipase	Metabolism
	Varespladib (LY315920) 是选择性group IIA, secretory phospholipase A2(sPLA2)抑制剂，其IC50=9 nM。它对大鼠，兔，豚鼠和人等各种物种血清的sPLA2活性具有明显的抑制作用，IC50分别为 8.1 nM，5.0 nM，3.2 nM 和 6.2 nM。
T21389	Enprofylline Enprofilina,3-propylxanthine,3-n-Propylxanthine,Enprofyllinum,恩丙茶碱	Others	Others
	Enprofylline (Enprofilina) 是具有选择性的 A2B 受体竞争性拮抗剂 (Ki:7 μM) ，也是磷酸二酯酶抑制剂。它可用于研究哮喘、慢性阻塞性肺疾病。
T61833	Tovinontrine IMR-687	PDE	Metabolism
	Tovinontrine (IMR-687) 是一种针对镰状细胞病治疗设计的强效且选择性的磷酸二酯酶-9 (PDE9) 抑制剂。其展现出高效能，对PDE9A1和PDE9A2的IC 50 值分别为8.19 nM和9.99 nM [1]。
T16478	PF-04447943 PF 04447943,Edelinontrine,PF04447943	PDE	Metabolism
	PF-04447943 (Edelinontrine) 是一种有效且具有选择性的的磷酸二酯酶 9A 抑制剂，IC50 为 12 nM，比作用于其他PDE家族成员选择性高 78 倍 (IC50>1000 nM)。PF-04447943 具有抗炎活性，通过抑制氧化应激、炎症和调节T细胞极化来减轻炎症反应，且可用于研究镰刀型贫血症。
T33730	N-Phenylacetylphenylalanine
	N-Phenylacetylphenylalanine is a biaromatic agent with properties that make them suitable candidates for the treatment of sickle cell disease.
T26095	Rivipansel GMI1070,GMI-1070,PF 06460031,GMI 1070,PF-06460031
	Rivipansel is a glycomimetic compound. It acts as a pan-selectin antagonist and reverses acute vascular occlusions in sickle cell mice.
T71292	Rivipansel sodium
	Rivipansel sodium is a glycomimetic drug candidate that acts as a pan-selectin antagonist and reverses acute vascular occlusions in sickle cell mice.
T39809	PRMT5-IN-14 PRMT5-IN-14
	PRMT5-IN-14 is a PRMT5 inhibitor to treat cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.
T39441	L-Arginine-15N4 hydrochloride L-Arginine-15N4 hydrochloride,(S)-(+)-Arginine-15N4 hydrochloride
	L-Arginine-15N4 ((S)-(+)-Arginine-15N4) hydrochloride, the 15N-labeled variant of L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride), serves as the nitrogen donor in the synthesis of nitric oxide. This potent vasodilator is crucial, especially during a sickle cell crisis where its levels are notably diminished.
T40155	FTX-6058 hydrochloride
	FTX-6058 hydrochloride is a potent and orally active inhibitor of Embryonic Ectoderm Development (EED), with the ability to induce HbF protein expression in both cell and murine models. This compound is particularly valuable in the research of select hemoglobinopathies, such as sickle cell disease and β-thalassemia.
T72663	(Rac)-Etavopivat (Rac)-FT-4202
	(Rac)-Etavopivat((Rac)-FT-4202) 是Etavopivat 异构体。Etavopivat 是一种具有口服活性的的红细胞丙酮酸激酶-R (PKR) 激活剂，可以用于镰状细胞病和其他血红蛋白疾病研究。
T40154	FTX-6058
	FTX-6058 is a potent orally active inhibitor targeting Embryonic Ectoderm Development (EED). It effectively induces HbF protein expression in both cell and murine models. This compound holds significant potential for researching select hemoglobinopathies such as sickle cell disease and β-thalassemia.
T70613	SLP120701 HCl
	SLP120701 is a potent and selective sphingosine kinase 2 inhibitor. Sphingosine-1-phosphate (S1P) is a ubiquitous, endogenous small molecule that is synthesized by two isoforms of sphingosine kinase (SphK1 and 2). Intervention of the S1P signaling pathway has attracted significant attention because alteration of S1P levels is linked to several disease states including cancer, fibrosis, and sickle cell disease.
T61975	Pociredir
	Pociredir (FTX-6058) 是一种有效的、选择性的、具有口服活性的胚胎外胚层发育蛋白 (EED) 小分子抑制剂（KD= 0.163 nM）。Pociredir (FTX-6058) 在研究炎症或血红蛋白病中具有研究价值，如镰状细胞病 (SCD)。
T70614	SLR080811 HCl
	SLR080811 is a SphK inhibitor. Sphingosine-1-phosphate (S1P) is a ubiquitous, endogenous small molecule that is synthesized by two isoforms of sphingosine kinase (SphK1 and 2). Intervention of the S1P signaling pathway has attracted significant attention because alteration of S1P levels is linked to several disease states including cancer, fibrosis, and sickle cell disease.
T62954	Ferroportin-IN-1
	Ferroportin-IN-1 是一种铁转运蛋白 ferroportin 抑制剂，能够用于研究像地中海贫血、镰状细胞病和血色素沉着症等由于缺乏铁调素或铁代谢紊乱引起疾病。
T73188	RK-0133114
	RK-0133114 是G9a 抑制剂，也是RK-701 的 R-对映体。RK-0133114 抑制 G9a 的IC50值为 3.7 μM。RK-0133114 可用于镰状细胞病 (SCD) 的研究。
T81500	PF-07059013
	PF-07059013是口服活性的镰状血红蛋白(HbS)非共价调制剂，具有纳摩尔级别的亲和力特异性结合Hb，展现出显著的红细胞(RBCs)分裂作用，适用于镰状细胞病(SCD)的研究。
T70900	VT-ME6
	VT-ME6 is a potent and selective sphingosine kinase 2 inhibitor. VT-ME6, contained a quaternary ammonium group as a warhead and established that a positively charged moiety is necessary for engaging key amino acid residues in the enzyme binding pocket.13,14 This compound is moderately potent (Ki = 8 lM) and displays three-fold selectivity for SphK2 over SphK1. Sphingosine-1-phosphate (S1P) is a ubiquitous, endogenous small molecule that is synthesized by two isoforms of sphingosine kinase (SphK...
T63351	MS8511
	MS8511 是一种选择性的G9a/GLP 共价的不可逆抑制剂，可靶向底物结合位点的半胱氨酸残基，IC50值为 100 nM ( G9a) 和 140 nM (GLP)，Kd 值44 nM (G9a) 和 46 nM (GLP)。 MS8511 可降低细胞内 H3K9me2 水平并提高抗增殖活性。MS8511 可用于研究多种癌症 (包括脑癌、乳腺癌、卵巢癌、肺癌、膀胱癌、黑色素瘤、结肠直肠癌) 和其他疾病,如阿尔茨海默病 (AD)、镰状细胞病、Prader-Willi 综合征 (PWS).

化合物

Cat.No: T7581

Synonym: GBT 440

Target: Others

RN-1 dihydrochloride

Cat.No: T21652

Target: Histone Demethylase, MAO

Cat.No: T35044

Synonym: BW 12C79,BW 12C,BW-12C79,BW12C79,BW-12C

Cat.No: T3528

Synonym: 塞尼卡泊,ICA-17043

Target: Potassium Channel

Cat.No: T77399

Synonym: ADAKVEO,SEG-101

Target: Others

Cat.No: T2044

Synonym: LY315920,伐瑞拉地,伐瑞拉迪

Target: Phospholipase

Cat.No: T21389

Synonym: Enprofilina,3-propylxanthine,3-n-Propylxanthine,Enprofyllinum,恩丙茶碱

Target: Others

Cat.No: T61833

Synonym: IMR-687

Target: PDE

Cat.No: T16478

Synonym: PF 04447943,Edelinontrine,PF04447943

Target: PDE

N-Phenylacetylphenylalanine

Cat.No: T33730

Cat.No: T26095

Synonym: GMI1070,GMI-1070,PF 06460031,GMI 1070,PF-06460031

Rivipansel sodium

Cat.No: T71292

Cat.No: T39809

Synonym: PRMT5-IN-14

L-Arginine-15N4 hydrochloride

Cat.No: T39441

Synonym: L-Arginine-15N4 hydrochloride,(S)-(+)-Arginine-15N4 hydrochloride

FTX-6058 hydrochloride

Cat.No: T40155

(Rac)-Etavopivat

Cat.No: T72663

Synonym: (Rac)-FT-4202

Cat.No: T40154

Cat.No: T70613

Cat.No: T61975

Cat.No: T70614

Ferroportin-IN-1

Cat.No: T62954

Cat.No: T73188

Cat.No: T81500

Cat.No: T70900

Cat.No: T63351

Cat. No.	Product Name	Target	Signaling Pathways
TN2719	2',4'-Dihydroxy-6'-methoxyacetophenone	Antibacterial	Microbiology/Virology
	2',4'-Dihydroxy-6'-methoxyacetophenone 是从豆科植物和菊科植物中提取的酚类苯乙酮，具有抗菌活性，可用于合成吡喃镰酮。
T8074	Esafosfan trisodium Fosfructose trisodium,D-果糖-1,6-二磷酸三钠盐,D-Fructose-1,6-diphosphate trisodium salt octahydrate,FDP trisodium,Diphosphofructose trisodium	Others; Endogenous Metabolite	Metabolism; Others
	Esafosfan trisodium (FDP trisodium) 是一种细胞保护性的天然糖磷酸盐，用于镰状细胞性贫血，心血管缺血和哮喘的研究。Fosfructose trisodium 通过刺激无氧糖酵解起作用，其在缺血条件下产生三磷酸腺苷。
T3228	Fosfructose D-fructose-1,6-diphosphate,Betulanonaprenol,4937-84-2,Diphosphofructose,二磷酸果糖,Fructose 1,6-diphosphate,D-fructofuranose 1,6-bisphosphate,Esafosfan	Others; Endogenous Metabolite	Metabolism; Others
	D-fructose-1,6-diphosphate 是一种细胞保护性的天然糖磷酸盐，Fosfructose 通过刺激无氧糖酵解起作用，其在缺血条件下产生三磷酸腺苷,有潜力用于心血管缺血，镰状细胞性贫血和哮喘的研究。

天然产物

2',4'-Dihydroxy-6'-methoxyacetophenone

Cat.No: TN2719

Target: Antibacterial

Esafosfan trisodium

Cat.No: T8074

Synonym: Fosfructose trisodium,D-果糖-1,6-二磷酸三钠盐,D-Fructose-1,6-diphosphate trisodium salt octahydrate,FDP trisodium,Diphosphofructose trisodium

Target: Others, Endogenous Metabolite

Cat.No: T3228

Synonym: D-fructose-1,6-diphosphate,Betulanonaprenol,4937-84-2,Diphosphofructose,二磷酸果糖,Fructose 1,6-diphosphate,D-fructofuranose 1,6-bisphosphate,Esafosfan

Target: Others, Endogenous Metabolite

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