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36

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T15441	GSK8573	Epigenetic Reader Domain	Chromatin/Epigenetic
	GSK8573 是 GSK2801 的非活性对照化合物。它与BRD9具有结合活性，Kd 值为 1.04 μM。
T10608	BRD5648 (R)-BRD0705	GSK-3	PI3K/Akt/mTOR signaling; Stem Cells
	BRD5648 ((R)-BRD0705) 是 BRD0705 的阴性对照，BRD0705 是旁系选择性和口服有效的 GSK3α 抑制剂，Kd 为 4.8 μM，IC50为 66 nM。与 GSK3β (IC50为 515 nM) 相比，BRD0705 对 GSK3α 的选择性更高 (8 倍)。BRD0705 可用于急性髓细胞性白血病。
T60023	CL-278474	Others	Others
	CL-278474 (化合物 I-79) 是有效的 β-N- 乙酰己糖氨基酶 OfHex1 抑制剂。
T23478	Trometamol hydrochloride TRIS hydrochloride,三(羟甲基)氨基甲烷盐酸盐	Others	Others
	Trometamol hydrochloride (TRIS hydrochloride) 是低毒性的生物惰性氨基醇，可以在体内、外缓冲二氧化碳和酸，能用于生理范围内控制 pH 值。
T0898	Chloroxylenol 酚洁新PX,5-dimethylphenol,4-Chloro-3,4-Chloro-3,5-dimethylphenol,氯二甲酚,PCMX	Influenza Virus; Antibacterial; Antibiotic	Microbiology/Virology
	Chloroxylenol (PCMX) 是广谱抗菌剂, 对控制细菌，藻类，真菌和病毒起作用。
T2035	WHI-P258	EGFR; JAK; JNK	Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; MAPK; Stem Cells; Tyrosine Kinase/Adaptors
	WHI-P258 是喹唑啉化合物，结合到JAK3的活性位点(Ki:72 µM)。甚至当WHI-P258到达 100 μM 时也不会抑制 JAK3 ，且对凝血酶诱导的血小板聚集无影响。
T13877	(S,S,S)-AHPC hydrochloride (S,S,S)-VH032-NH2 hydrochloride,(S,S,S)-AHPC盐酸盐	Ligand for E3 Ligase	PROTAC
	(S,S,S)-AHPC hydrochloride ((S,S,S)-VH032-NH2 hydrochloride) 是 von Hippel-Lindau (VHL) 氨基砌块。(S,S,S)-AHPC (Compound 27) 常作为 (S,R,S)-AHPC 的阴性对照。(S,R,S)-AHPC 是基于 VH032 的 VHL 配体，可用于募集 VHL 蛋白。
TP2203	Bax inhibitor peptide, negative control	Others	Others
	The compound is a negative control peptide for the Bax inhibitor peptides V5 and P5.
T31831	Fluvalinate Kartan,Fluvalinate II,Fluvalinate I,Mavrik,Klartan,Apistan
	Fluvalinate is a synthetic chemical compound and can be commonly used to control varroa mites in honey bee colonies.
T40822	TRPA1 Antagonist 3 TRPA1 Antagonist 3
	TRPA1 Antagonist 3 is a compound with photoswitchable properties that acts as an agonist on the TRPA1 channel, providing the ability for optical control.
T70662	UCSF924NC
	UCSF924NC is the recommended negative control compound for the high-affinity dopamine D4 receptor (DRD4) partial agonist UCSF924. UCSF924NC exhibits a 1/2500-fold reduced D4 affinity when compared with that of UCSF924.
T39239	TRC-766
	TRC-766, a negative control of RTC-5 (TRC-382), is a compound that exhibits protein phosphatase 2A (PP2A) binding properties while lacking phosphatase activation capabilities.
T29063	UNC-4219 TFA UNC4219,UNC-4219,UNC 4219
	UNC4219 is a negative control compound for UNC3866, a potent antagonist of the methyllysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains.
T36505	Sulpho NONOate
	Sulpho NONOate produces nitrous oxide but no NO at physiological pH. Therefore, this compound may be used as a negative control in experiments using other NO donors of the NONOate class.
T39750	CMP98
	CMP98, a proteolysis targeting chimera (PROTAC), exhibits a lack of VHL degradation efficacy. It can function as a negative control compound in comparison to CM11. CMP98 comprises two von Hippel-Lindau ligands operating within their active domains.
T38743	Scrambled TRAP Fragment
	Scrambled TRAP Fragment is a variant of the TRAP Fragment compound, characterized by its random amino acid sequence. It is typically employed as a negative control due to its similarity in composition to the active fragment.
T36240	AP219
	AP39 is a compound used to increase the levels of hydrogen sulfide (H2S) within mitochondria. It consists of a mitochondria-targeting motif (triphenylphosphonium) coupled to an H2S-donating moiety (dithiolethione) by an aliphatic linker. AP219 is a control compound for AP39, containing the triphenylphosphonium scaffold but lacking the H2S-releasing portion.
T36305	FMF-04-159-R
	Potent inhibitor of CDK16 and CDK14 (IC50 values are 6 and 140 nM, respectively in kinase activity assay; IC50 = 563 nM for CDK14 in BRET assay). Also binds CDK2 (IC50 = 493 nM). Inhibition reversible upon compound wash-out. Control for FMF-04-159-2 (Cat. No. 7158).
T69012	Cinnarizine clofibrate
	Cinnarizine clofibrate is a calcium channel protein inhibitor as well as an antihistamine channel blocker. The compound is a drug derivative of piperazine. Cinnarizine is used for the control of vomiting due to motion sickness. It acts by interfering with the signal transmission between vestibular apparatus of the inner ear and the vomiting centre of the hypothalamus
T36254	dTAGV-1 hydrochloride
	Hydrochloride salt of dTAGV-1. Suitable for use in vivo. Following ip administration of 10 mg/kg in mice: T = 4.43 h; Cmax = 2123 ng mL-1; AUCinf = 18517 hrng mL-1 and CL = 9.05 mL min-1 kg-1 Negative control* dTAGV-1-NEG also available. Important: It is recommended that DMSO stock solutions of this compound are made and used on the same day and are not subjected to freeze/thaw.
T41157	MS 154N
	MS 154N 是 MS 154的阴性对照。该化合物对 WT 和 l858r 突变体 EGFR 具有高结合亲和力(kd 值分别为3 nM 和4.3 nM)，但不显著诱导 EGFR 突变体降解。
T82923	Bamadutide SAR425899
	Bamadutide (SAR425899)是一种高效的GLP-1/GIP受体激动剂，主要通过增强β细胞功能和降低葡萄糖吸收速率，从而改善餐后血糖控制。该化合物适用于2型糖尿病的研究。
T72557	Transketolase-IN-2
	Transketolase-IN-2（化合物4w）是一种强效的Transketolase抑制剂，对Digitaria sanguinalis和Amaranthus retroflexus展现出显著的抑制效果（200 mg/L浓度下抑制率超过90%，100 mg/L浓度下抑制率约为80%）。该化合物适用于研究杂草防治。
T60620	UCSF686
	UCSF686 是一种 UCSF678 类似物，不具有 5-HT5A 效力，同时保留了脱靶亲和力（5-HT1A、5-HT2B 和 5-HT7）。当使用 UCSF678 探测培养物和体内的 5-HT5A 依赖性活性时，建议将 UCSF686 作为对照化合物 [1]。
T74558	SK-575-NEG
	SK-575-NEG（化合物28）是SK-575的甲基化对应物，通过对SK-575中的哌啶-2,6-二酮氨基进行甲基化合成而得，用作对照化合物。SK-575-NEG强效结合PARP1，IC50值仅为2.64 nM。在1 μM浓度下，SK-575-NEG对MDA-MB-436和Capan-1细胞中PARP1的降解完全无效。
T62531	TRK-IN-12
	TRK-IN-12 (Compound 9e) 是一种大环衍生的有效TRK抑制剂，具有显著的TRKG595R抑制活性 (IC50= 13.1 nM)。在Ba/F3-LMNA-NTRK1细胞系中具有出色的抗增殖效果 (IC50= 0.080 μM)，并且在Ba/F3-LMNA-NTRK1-G595R细胞系中展示了超过对照活性分子LOXO-101的抑制能力 (IC50= 0.646 μM)。
T76263	Beinaglutide
	Beinaglutide 是一种重组人 GLP-1(rhGLP-1) 多肽，与人 GLP-1(7-36) 具有几乎 100% 的同源性。Beinaglutide 在血糖控制、抑制食物摄入和胃排空和促进体重减轻方面表现出依赖于剂量的作用。Beinaglutide 具有研究超重/肥胖和非酒精性脂肪性肝炎 (NASH) 的潜力。
T38336	W140 (trifluoroacetate salt) W140 (trifluoroacetate salt)
	Sphingosine-1-phosphate (S1P) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis. It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8. W140 is an inactive enantiomer of W146, a selective S1P1 antagonist (Ki = 77 nM), that binds to the S1P1 receptor with a Ki of 4.6 μM (2a = W146; 2b = W...
T81932	LIN28-IN-1
	LIN28-IN-1（compound 5）是针对RNA结合蛋白LIN28的抑制剂，可与LIN28的冷休克结构域（CSD）发生结合。该化合物能有效阻断LIN28与let-7miRNA的交互作用，具有显著的IC50值为5.4 μM，从而抑制LIN28在表观遗传学中的负向调控功能。此外，LIN28-IN-1在IC50为6.4 μM的条件下，显著抑制了过表达LIN28的JAR癌细胞的增殖。
T68538	CEP-14083
	CEP-14083 is a potent ALK inhibitor that has shown activity in an NPM/ALKÂ–carrying T-cell lymphoma in vitro study. Presumably, this compound binds to the hinge region of the kinase in an ATP-competitive manner. CEP-14083 displays a potent activity against ALK in enzymatic assays (IC50 = 11 nmol/L). Further, CEP-14083 is also able to inhibit the insulin receptor at a concentration within a nanomolar range. In a preclinical assay, CEP-14083 showed that, via NPM/ALK TK inhibition, it could control...
T73658	Orexin A (human, rat, mouse) (acetate)
	Orexin A (Hypocretin-1) (human, rat, mouse) acetate 是一种具有镇痛特性的下丘脑神经肽 (可透过血脑屏障)。Orexin A (human, rat, mouse) acetate 也是一种OX1R 激动剂，能以时间和剂量依赖性的方式诱导 SH-SY5Y 细胞BDNF 和TH 蛋白的表达。Orexin A (human, rat, mouse) acetate 可用于食欲调节、神经退行性疾病，以及调节伤害性信息传递的研究。
T70207	Pimodivir tosylate
	Pimodivir, also known as VX-787, JNJ-872, is a novel inhibitor of influenza virus replication that blocks the PB2 cap-snatching activity of the influenza viral polymerase complex. VX-787 binds the cap-binding domain of the PB2 subunit with a KD (dissociation constant) of 24 nM as determined by isothermal titration calorimetry (ITC). The cell-based EC50 (the concentration of compound that ensures 50% cell viability of an uninfected control) for VX-787 is 1.6 nM in a cytopathic effect (CPE) assay...
T36367	RK-682 (calcium salt)
	Protein tyrosine phosphatases (PTPs) remove phosphate from tyrosine residues of cellular proteins. Reversible phosphorylation catalyzed by the coordinated actions of protein tyrosine kinases and phosphatases is key to the regulation of the signaling events that control cell growth and proliferation, differentiation, and survival or apoptosis, as well as adhesion and motility. RK-682, a bioactive compound originally isolated from the fermentation of Streptomyces sp. 88-682, is an inhibitor of the...
T72213	Efonidipine hydrochloride NZ-105 hydrochloride
	Efonidipine(NZ-105)盐酸盐是T 型和L 型钙离子通道双重阻断剂。
T35840	4-Amino-6-chloro-1,3-benzenedisulfonamide
	4-Amino-6-chloro-1,3-benzenedisulfonamide is a carbonic anhydrase inhibitor.1 Formulations containing this compound are diuretics.2 4-Amino-6-chloro-1,3-benzenedisulfonamide is detected as a hydrolysis product of chlorothiazide in the urine.2 Diuretics, including chlorothiazide, have been abused as performance-enhancing drugs and masking agents in sports doping.3References1. Nishimori, I., Vullo, D., Minakuchi, T., et al. Carbonic anhydrase inhibitors: Cloning and sulfonamide inhibition studies ...
T35812	CAY10591 CAY10591
	Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). Human SIRT1 is the homolog of yeast silent information regulator 2 (Sir2) and has been shown to regulate the activity of the p53 tumor suppressor and inhibit apoptosis. Small molecule activators of SIRT1, such as resveratrol, extend lifespan in yeast and C. elegans in a manner that resembles caloric restriction. CAY10591 has been identified as an activator of the enzyme SIRT1. This com...

化合物

Cat.No: T15441

Target: Epigenetic Reader Domain

Cat.No: T10608

Synonym: (R)-BRD0705

Target: GSK-3

Cat.No: T60023

Target: Others

Trometamol hydrochloride

Cat.No: T23478

Synonym: TRIS hydrochloride,三(羟甲基)氨基甲烷盐酸盐

Target: Others

Cat.No: T0898

Synonym: 酚洁新PX,5-dimethylphenol,4-Chloro-3,4-Chloro-3,5-dimethylphenol,氯二甲酚,PCMX

Target: Influenza Virus, Antibacterial, Antibiotic

Cat.No: T2035

Target: EGFR, JAK, JNK

(S,S,S)-AHPC hydrochloride

Cat.No: T13877

Synonym: (S,S,S)-VH032-NH2 hydrochloride,(S,S,S)-AHPC盐酸盐

Target: Ligand for E3 Ligase

Bax inhibitor peptide, negative control

Cat.No: TP2203

Target: Others

Cat.No: T31831

Synonym: Kartan,Fluvalinate II,Fluvalinate I,Mavrik,Klartan,Apistan

TRPA1 Antagonist 3

Cat.No: T40822

Synonym: TRPA1 Antagonist 3

Cat.No: T70662

Cat.No: T39239

Cat.No: T29063

Synonym: UNC4219,UNC-4219,UNC 4219

Cat.No: T36505

Cat.No: T39750

Scrambled TRAP Fragment

Cat.No: T38743

Cat.No: T36240

Cat.No: T36305

Cinnarizine clofibrate

Cat.No: T69012

dTAGV-1 hydrochloride

Cat.No: T36254

Cat.No: T41157

Cat.No: T82923

Synonym: SAR425899

Transketolase-IN-2

Cat.No: T72557

Cat.No: T60620

Cat.No: T74558

Cat.No: T62531

Cat.No: T76263

W140 (trifluoroacetate salt)

Cat.No: T38336

Synonym: W140 (trifluoroacetate salt)

Cat.No: T81932

Cat.No: T68538

Orexin A (human, rat, mouse) (acetate)

Cat.No: T73658

Pimodivir tosylate

Cat.No: T70207

RK-682 (calcium salt)

Cat.No: T36367

Efonidipine hydrochloride

Cat.No: T72213

Synonym: NZ-105 hydrochloride

4-Amino-6-chloro-1,3-benzenedisulfonamide

Cat.No: T35840

Cat.No: T35812

Synonym: CAY10591

Cat. No.	Product Name	Target	Signaling Pathways
TN3626	Cerbinal	Antifection	Microbiology/Virology
	Cerbinal 是一种天然化合物，来源于非洲非洲菊的草本植物。它具有杀虫活性，是一种潜在的新型害虫防治剂。
T82487	Ejaponine A
	Ejaponine A（化合物1）为源于日本卫矛的杀虫倍半萜酯。该化合物展现出强效针对粘虫的活性（LD50为89.2 μg/g），在相关杀粘虫机制研究中得到应用。

天然产物

Cat.No: TN3626

Target: Antifection

Cat.No: T82487

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