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32

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T9149	2BAct 2B-Act,2B Act	PERK	Apoptosis
	2BAct 是一种具有口服活性的高选择性真核起始因子eIF2B 活化剂，EC50为 33 nM。它可防止由慢性综合应激反应引起的神经系统缺陷。
T25829	Mopidamol RA233,RA 233,RA-233,Rapenton,OLX 102	PDE	Metabolism
	Mopidamol (RA 233) 是一种磷酸二酯酶抑制剂，是 dipyridamole 衍生物，具有抗癌活性，可预防实验性糖尿病的视网膜血管缺陷。
T35074	VRT-325 CFcor 325,VRT-534,CFcor325,VRT 325,VRT325,CF-106951,CFcor-325	Others	Others
	VRT-325 可以通过促进两个 NBD 的二聚化或促进 TMD 的折叠来修复折叠缺陷。VRT-325 可加速CF细胞单层的愈合速度。
T14847	B I09	Others; IRE1	Cell Cycle/Checkpoint; Others
	B I09是一种 IRE-1 RNase 抑制剂，IC50为1230 nM，对人 WaC3细胞中 XBP1 mRNA 的剪接和 LPS 刺激的 B 细胞中 xbp -1的表达有抑制作用。B I09可用于 CLL 细胞模拟XBP-1缺陷的研究。
T0183	Pramiracetam CI-879,普拉西坦	Others	Others
	Pramiracetam (CI-879) 来源于piracetam，能改善脑外伤引起的认知障碍。它是更有效的促智药物。
T29114	VRT-532 CFpot-532,CFpot-532)	CFTR	Membrane transporter/Ion channel
	VRT-532 (CFpot-532)是CFTR 的有效调节剂，常用于CFTR 缺陷引起的囊性纤维化(CF)研究。降解囊性纤维化中积累的硫酸化糖胺聚糖(gag)所必需的Arylsulfatase B (ARSB)，小分子调节剂VRT-532对CFTR 的修饰能增加ARSB 并减少4-硫酸软骨素的积累。
T32125	Hyperphyllin HP
	Hyperphyllin specifically mimics the branch defects of AMP1, including plastid reduction and expansion and proliferation of the branch meristem.
T4497L	Amifampridine phosphate BRN0110232,3,6-DAP,SC10,BRN 0110232,BRN-0110232,NSC 521760
	Amifampridine is mainly used to treat many rare muscle diseases. In the United States, aminopyridine is being studied for the treatment of Lambert-Eaton myasmus syndrome (LEMS). Amifampridine is also used to treat many congenital myasthenia syndromes, par
T27562	Hydroxyellipticine-1a
	Hydroxyellipticine-1a, a selective r(CGG)exp probe, improves pre-mRNA splicing defects, inhibits formation of nuclear inclusions and RANT in a FXTAS cellular mode.l
T69440	Sephin1 Hydrochloride
	Sephin1 hydrochloride is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A), which prolongs the benefit of eIF2α phosphorylation, thereby protecting cells from proteostatic defects.
T22860	Imeglimin	Others	Others
	Imeglimin is the first in a new tetrahydrotriazine-containing class of oral antidiabetic agents. It has been shown to act on the liver, muscle, and pancreatic β-cells to uniquely target the key defects of type 2 diabetes.
T40908	KLD-12
	KLD-12, a 12-residue self-assembling peptide, displays properties that promote chondrogenic differentiation of bone marrow stromal cells (BMSCs). Moreover, KLD-12 hydrogel can effectively fill full-thickness osteochondral defects in their original location, leading to improved cartilage repair.
T73107	RAD51-IN-4
	RAD51-IN-4 是一种有效的RAD51抑制剂。RAD51是一种真核生物基因。RAD51-IN-4 具有研究线粒体缺陷病症的潜力。
T76649	Osteostatin (human)
	Osteostatin (human)，一种甲状旁腺激素相关蛋白(PTHrP) 107-139片段，可在骨缺损动物模型中促进骨修复并在炎症性关节炎中防止骨侵蚀。
T82056	IP2
	IP2作为免疫调节剂，能增强癌细胞内PTP衍生的抗原呈递，但对癌细胞本身不具有细胞毒性。在小鼠实验中，IP2能诱导肿瘤生长缺陷。
T37666	Trihydroxycholestanoic Acid Trihydroxycoprostanic Acid
	Trihydroxycholestanoic acid is an intermediate in the biosynthesis of cholic acid .1 Elevated plasma levels of trihydroxycholestanoic acid have been found in patients with Zellweger syndrome, a neurological disorder characterized by mutations in PEX genes which result in defects in peroxisome formation.2,3 \|1. Keane, M.H., Overmars, H., Wikander, T.M., et al. Bile acid treatment alters hepatic disease and bile acid transport in peroxisome-deficient PEX2 Zellweger mice. Hepatology 45(4), 982-997 ...
T32706	Levomefolate calcium pentahydrate
	Levomefolate calcium pentahydrate is the calcium salt of 5-methyltetrahydrofolic acid, a biologically active form of folic acid that functions, in conjunction with Vitamin B12. Levomefolate is included in formulations of certain oral contraceptives to ens
T38189	2-hydroxy Lignoceric Acid
	2-hydroxy Lignoceric acid is an α-hydroxy very long chain fatty acid that is normally present in the mammalian nervous system. In the brain, 2-hydroxy lignoceric acid is derived from lignoceric acid and further converted to ceramides and cerebrosides during the process of nerve sheath myelination. 2-hydroxy Lignoceric acid is produced by the α-oxidation of lignoceric acid in the peroxisome and defects in this pathway are associated with disorders such as Zellweger syndrome.
T28685	SB236057 SB-236057,SB 236057
	SB236057 is a potent and selective inverse agonist for the 5-HT receptor, acting especially at 5-HT autoreceptors on nerve terminals. It produces a rapid increase in 5-HT levels in the brain. SB236057 also acts as a potent teratogen, producing severe musc
T25496	Hexaglutamate folate Pteglu6
	Hexaglutamate folate is a naturally occurring form of folic acid. The bioavailability of dietary folate may be limited by the need for the glutamate moieties to be deconjugated before absorption. Folate deficiency in humans results in anemia, neural tube
T73702	Mecasermin
	Mecasermin（Human IGF-I; FK 780），一种重组人胰岛素样生长因子I（IGF-I），主要用于研究因生长激素（GH）受体缺陷或GH抑制抗体导致的GH不敏感性而引起的生长障碍。
T35729	Nemadipine-A
	Nemadipine A is an L-type calcium channel blocker that induces morphological and growth defects in wild-type C. elegans and those with hypoexpression of egl-19, which encodes the only L-type calcium channel α1-subunit in the C. elegans genome. It also inhibits L-type calcium channels in chick ciliary neurons. Nemadipine A increases TRAIL-induced cytotoxicity and synergistically enhances caspase-8 and caspase-3 activation in a concentration-dependent manner in H1299 lung adenocarcinoma cells. It ...
T35594	Cuspin-1
	The Survival of Motor Neurons (SMN) protein participates in RNA splicing. Decreases in SMN, typically a consequence of defects in the smn1 gene, result in the death of motor neurons and lead to the neurodegenerative disease, spinal muscular atrophy (SMA). Cuspin-1 is a small molecule upregulator of SMN that has been shown in vitro to increase levels of SMN in SMA patient fibroblasts by 50% at 18 μM. Its mechanism of action is thought to involve increased phosphorylation of ERK to initiate Ras-Ra...
T78241	Asfotase alfa ENB-0040
	Asfotase alfa (ENB-0040) 是一款针对骨骼的基因重组糖蛋白。该药物提升了Akp2−/−基因敲除小鼠的存活率、骨矿化及骨骼生长，并且缓解了脚部、胸部、下肢及颌骨矿化缺损。它主要用于对围产期、婴幼儿及青少年型低磷酸酶血症(HPP)进行研究。
T36801	Binucleine 2
	Binucleine 2 is an isoform-specific and ATP-competitive inhibitor of Drosophila Aurora B kinase (Ki = 0.36 μM), a kinase involved in cell division. It is specific for Drosophila Aurora B kinase, inhibiting it in a dose-dependent manner, with minimal inhibition of human or X. laevis Aurora B kinases at concentrations up to 100 μM. Binucleine 2 induces mitotic and cytokinesis defects in Drosophila Kc167 cells. It prevents Drosophila S2 cells from assembling a contractile ring during cell division ...
T37193	4-Methylumbelliferyl-2-acetamido-2-deoxy-β-D-Glucopyranoside
	4-Methylumbelliferyl-2-acetamido-2-deoxy-β-D-glucopyranoside is a fluorogenic substrate for β-hexosaminidases. Upon enzymatic cleavage by β-hexosaminidases, 4-methylumbelliferone (4-μU) is released and its fluorescence can be used to quantify β-hexosaminidase activity. 4-MU fluorescence is pH-dependent with excitation maxima of 320 and 360 nm at low (1.97-6.72) and high pH (7.12-10.3), respectively, and an emission maximum ranging from 445 to 455 nm, increasing as pH decreases. 4-Methylumbellife...
T81592	Osteostatin PTHrP (107–111)
	Osteostatin为甲状旁腺激素相关蛋白(PTHrP) 107-111片段，该化合物在动物模型中促进骨缺损修复，预防炎症性关节炎引起的骨侵蚀，并抑制骨胶原诱导的关节炎及破骨细胞的吸收作用。Osteostatin主要应用于免疫炎症的研究领域。
T78024	Selcopintide acetate Cpne7-DP acetate
	Selcopintide acetate (Cpne7-DP) 是一种合成肽，其结构基于hCPNE7蛋白的10个氨基酸残基344-353片段。该化合物通过上调成牙本质细胞标记基因DSPP和巢蛋白，高度复现了CPNE7在体外的作用。Selcopintide acetate能够促进牙本质再生，对不同程度的牙本质缺损有治疗效果，再生的硬组织具有真牙本质的特性。
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...
T38187	6-Aminophenanthridine
	6-Aminophenanthridine is an antiprion agent. It inhibits prion formation in yeast- and mammalian-based screening assays when used alone and, to a greater extent, when used in combination with the α2-adrenergic receptor agonist guanabenz . 6-Aminophenanthridine (300 μM) inhibits protein folding activity of the ribosome (PFAR) by directly competing with protein substrates for the active site and decreases the yield of refolded protein without affecting the refolding rate. It prevents progressive w...
T21881	Fluconazole hydrate
	Fluconazole 水合物是抗真菌化合物，用于治疗和预防浅表和全身性的真菌感染。
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...

化合物

Cat.No: T9149

Synonym: 2B-Act,2B Act

Target: PERK

Cat.No: T25829

Synonym: RA233,RA 233,RA-233,Rapenton,OLX 102

Target: PDE

Cat.No: T35074

Synonym: CFcor 325,VRT-534,CFcor325,VRT 325,VRT325,CF-106951,CFcor-325

Target: Others

Cat.No: T14847

Target: Others, IRE1

Cat.No: T0183

Synonym: CI-879,普拉西坦

Target: Others

Cat.No: T29114

Synonym: CFpot-532,CFpot-532)

Target: CFTR

Cat.No: T32125

Synonym: HP

Amifampridine phosphate

Cat.No: T4497L

Synonym: BRN0110232,3,6-DAP,SC10,BRN 0110232,BRN-0110232,NSC 521760

Hydroxyellipticine-1a

Cat.No: T27562

Sephin1 Hydrochloride

Cat.No: T69440

Cat.No: T22860

Target: Others

Cat.No: T40908

Cat.No: T73107

Osteostatin (human)

Cat.No: T76649

Cat.No: T82056

Trihydroxycholestanoic Acid

Cat.No: T37666

Synonym: Trihydroxycoprostanic Acid

Levomefolate calcium pentahydrate

Cat.No: T32706

2-hydroxy Lignoceric Acid

Cat.No: T38189

Cat.No: T28685

Synonym: SB-236057,SB 236057

Hexaglutamate folate

Cat.No: T25496

Synonym: Pteglu6

Cat.No: T73702

Cat.No: T35729

Cat.No: T35594

Cat.No: T78241

Synonym: ENB-0040

Cat.No: T36801

4-Methylumbelliferyl-2-acetamido-2-deoxy-β-D-Glucopyranoside

Cat.No: T37193

Cat.No: T81592

Synonym: PTHrP (107–111)

Selcopintide acetate

Cat.No: T78024

Synonym: Cpne7-DP acetate

Cat.No: T68480

6-Aminophenanthridine

Cat.No: T38187

Fluconazole hydrate

Cat.No: T21881

Cat.No: T37441

Cat. No.	Product Name	Target	Signaling Pathways
T0062	Folic acid Folate,Vitamin B9,Pteroylglutamic acid,Vitamin M,叶酸,Folacin	DNA/RNA Synthesis; Endogenous Metabolite	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism
	Folic acid (Vitamin B9) 是维生素B9，是合成DNA/RNA，新细胞产生和维持的必要成分。
T4877	L-Homocystine	Endogenous Metabolite	Metabolism
	L-Homocystine 是一种 L-homocysteine 的氧化物。其中 L-homocysteine 是抗血栓因子、血管舒张损害剂、促炎因子，也是研究心血管疾病发生机制的内质网应激反应的诱导剂。
T83582	(±)-Pantothenic acid (±)-Vitamin B5,(±)-Pantothenate
	(±)-Pantothenic acid ((±)-Pantothenate) 作为 B 组维生素的一员，对于哺乳动物细胞中辅酶 A (CoA) 的生物合成是不可或缺的。此外，该化合物能防护丙戊酸 (VPA) 在 CD-1 小鼠中引起的神经管缺陷 (NTD)。

天然产物

Cat.No: T0062

Synonym: Folate,Vitamin B9,Pteroylglutamic acid,Vitamin M,叶酸,Folacin

Target: DNA/RNA Synthesis, Endogenous Metabolite

Cat.No: T4877

Target: Endogenous Metabolite

(±)-Pantothenic acid

Cat.No: T83582

Synonym: (±)-Vitamin B5,(±)-Pantothenate

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