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47

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T22748	DQP 1105	NMDAR	Neuroscience
	DQP 1105 是一种高效非竞争性NMDA 受体拮抗剂。DQP-1105 抑制含有 GluN2C (IC50:7.0 Μm) 和 GluN2D (IC50:2.7 Μm) 的受体。 IC50值至少比重组 GluN2B-、GluN2A-、GluA1- 或 GluK2 受体低 50 倍。
T15401	GNE-371	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	GNE-371 是一种选择性人类转录起始因子 TFIID 亚基 1 和转录起始因子 TFIID 亚基 1-like 第二溴结构域的探针。
T14971	CIQ	NMDAR	Neuroscience
	CIQ 是亚基选择性NMDA 受体增强剂，可作用于NR2C 或NR2D 亚基。
T22192	BMS 195614 BMS614	Retinoid Receptor	Metabolism
	BMS 195614 (BMS614)是一种选择性的RARα拮抗剂。BMS 195614可以与RARα亚基结合。
T7870	TCN 201 TCN-201	NMDAR; iGluR	Membrane transporter/Ion channel; Neuroscience
	TCN 201 是选择性的、有效的，非竞争性的GluN1/GluN2A NMDA 受体拮抗剂，pIC50值为 6.8。与 GluN1/GluN2B NMDA 受体 (pIC50<4.3) 相比，它对 GluN1/GluN2A NMDA 受体具有选择性。
T21824	Sephin1 NSC 65390,IFB-088	Phosphatase	Metabolism
	Sephin1 (IFB-088) 是 GADD34 (PPP1R15A) 的选择性抑制剂，这是一种应激诱导的蛋白磷酸酶 1 复合物调节亚基，可将 eIF2α 去磷酸化。
T12758	Ro 25-6981	NMDAR	Neuroscience
	Ro 25-6981 是一种有效的选择性活性依赖性 NMDA 受体阻滞剂，含有 NR2B 亚基，对克隆受体亚基组合 NR1C/NR2B 和 NR1C/NR2A 的 IC50 分别为 0.009 和 52 μM。 Ro 25-6981 可用于帕金森病的研究。
T5375	Loreclezole	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Loreclezole 是一种选择性 GABAA 受体调节剂，可作为含有 β2 或 β3 亚基的受体的正变构调节剂，有抗癫痫作用。
T2067	NS11394 NS 11394	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	NS11394 是可口服GABAA 的阳性变构调节剂 (PAM)，Ki 值为 0.5 nM。它对GABAA 的选择性依次为 α5、α3、α2 和α1 受体，具有抗炎和抗焦虑活性。
T39217	PKA-IN-1	PKA	Tyrosine Kinase/Adaptors
	PKA-IN-1 是一种具有选择性和有效性的 cyclic AMP 依赖性蛋白激酶 (PKA) 催化亚基 (cAK) 抑制剂（IC50 ： 0.03 μM）。PKA-IN-1 可用于研究免疫系统疾病。
T9174	Icerguastat Sephin 1,lcerguastat,IFB-088	Phosphatase	Metabolism
	Icerguastat (IFB-088) 是一种缺乏 α2-肾上腺素能活性的 Guanabenz 衍生物，是一种磷酸酶调节亚单位 PPP1R15A (R15A)的选择性抑制剂。它能够抑制 eIF2α 去磷酸化，从而延长保护反应。它具有抗朊病毒作用。
TP2063	α-Conotoxin MII	AChR	Neuroscience
	α-Conotoxin MII 是可从僧袍芋螺中分离得到的一种天然产物，有效抑制 nAChR 受体的α3β2亚基，IC50值为 0.5 nM。它还可有效抑制 β3-containing 神经尼古丁受体。
T38272	Thiacloprid	AChR; Parasite	Microbiology/Virology; Neuroscience
	Thiacloprid 属于氯烟碱类杀虫剂，主要用于防治蔬菜和果园中的蚜虫。它会破坏 DNA 的稳定性，通过疏水或氢相互作用，结合到小沟槽中，改变 DNA 的结构和稳定性。
T73447	NP10679
	NP10679 是一种选择性、pH 依赖性的GluN2B 亚基特异的 N-methyl-D-aspartate (NMDA) 受体抑制剂，具有较高的口服生物利用度和良好的脑穿透性。NP10679 在 pH 6.9 和 7.6 下，抑制 GluN2B 的IC50分别为 23 和 142 nM。NP10679 是histamine H1的拮抗剂和hERG 通道抑制剂，IC50分别为 73 和 620 nM。NP10679 是一种可逆的人肝脏CYP 酶抑制剂。
T16795	Rpn11-IN-1 Capzimin intermediate	Others	Others
	Rpn11-IN-1 is an effective and selective inhibitor of proteasome subunit Rpn11 (IC50: 390 nM).
T23457	threo Ifenprodil hemitartrate	Others	Others
	σ receptor agonist and NR2B subunit-selective NMDA receptor antagonist
T12758L	Ro 25-6981 Maleate	Others	Others
	Ro 25-6981 Maleate is a potent and selective activity-dependent NMDA receptors blocker containing the NR2B subunit.(IC50 values are 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively).
T30428	Besonprodil Besonprodil (USAN),UNII-5K3N2D15WW,253450-09-8,CHEMBL219631,CI-1041
	Besonprodil is a drug that acts as an NMDA antagonist and is selective for the NR2B subunit.
TQ0233L	Traxoprodil Mesylate
	Traxoprodil Mesylate is a potent noncompetitive N-methyl-D-aspartate (NMDA) receptors antagonist and has selective for the NR2B subunit.
T70620	VU0466551
	VU0466551 is a selective activator of homomeric G protein gated, inwardly rectifying, potassium subunit 1 (GIRK1) channels.
T24717	Ro 25-6981 HCl Ro 25 6981 HCl
	Ro 25-6981 HCl is an effective and selective NMDA glutamate receptors containing the NR2B subunit antagonist.
T24609	Thymidine 3',5'-disphosphate Thymidine 3',5'-biphosphate,pdTp
	pdTp is a highly selective, small-molecule miRNA regulatory complex RISC subunit SND1 inhibitor.
T17193	UBP 302	Others	Others
	UBP 302 is an effective and selective GLUK5-subunit-containing kainate receptor antagonist (apparent Kd=402 nM) and displays very little affinity on GluK2 kainate receptors.
T68697	TC-1698 dihydrochloride
	TC-1698 dihydrochloride is a selective nicotinic α7 receptor agonist that also displays weak partial agonist/antagonist activity at β-subunit-containing receptors. This product is a neuroprotectant.
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.
T37421	Ac-PAL-AMC
	Ac-PAL-AMC is a fluorogenic substrate for the β1i/LMP2 subunit of the 20S immunoproteasome. Upon cleavage, 7-amino-4-methylcoumarin (AMC) is released and its fluorescence can be used to quantify the activity of the β1i/LMP2 subunit of the 20S immunoproteasome. Ac-PAL-AMC is selective for the immunoproteasome over the constitutive proteasome. AMC displays excitation/emission maxima of 351/430 nm, respectively.
T39694	GluN2B receptor modulator-1 GluN2B receptor modulator-1
	GluN2B receptor modulator-1 is a potent and selective allosteric modulator of the GluN2B receptor. It demonstrates negative modulation, inhibiting receptor activity, and exhibits high selectivity towards the GluN2B subunit, with an impressive IC50 value of 31 nM.
T68973	EVT-101 free base
	EVT-101, also known as ENS-101, is an experimental medication which originated from Roche and is under development by Evotec AG for the treatment of major depressive disorder. It acts as a selective NMDA receptor subunit 2B (NR2B) antagonist.
TP2061	α-Conotoxin AuIB
	Selective antagonist of α3β4 nicotinic acetylcholine receptors. Displays > 100-fold selectivity over other receptor subunit combinations including α2β2, α2β4, α3β2, α4β2, α4β4 and α1β1γδ.
T16292	NFPS	Thrombin	Proteases/Proteasome
	NFPS exerts neuroprotection via glyR alpha1 subunit in the rat model of transient focal cerebral ischaemia and reperfusion. NFPS is a selective and non-competitive glycine transporter-1 (GlyT1) inhibitor (IC50s: 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively).
T10436L	AZD4573 HCl (2057509-72-3 free base) AZD4573 hydrochloride,AZD4573,AZD4573 HCl,AZD-4573,AZD 4573
	AZD-4573 is a selective and short-acting inhibitor of the serine/threonine cyclin-dependent kinase 9, the catalytic subunit of the RNA polymerase II elongation factor positive transcription elongation factor b. It also has a potential antineoplastic activ
T24919	UBP714 UBP 714,UBP-714
	UBP714 is a derivative of the NMDA receptor negative allosteric modulator UBP608. It also enhanced NMDAR mediated field EPSPs in the CA1 region of the hippocampus. UBP714 is a novel template for the development of potent and subunit selective NMDAR potent
T29228	ZK93423 ZK-93423,ZK 93423
	ZK93423 is a potent agonist of benzodiazepine receptor (IC50 = 1 nM) with non-selective between α1-, α2-, α3- and α5-subunit containing GABAA receptors, Ki values are 4.1, 4.2, 6 and 4.5 nM for inhibition of [3H]Ro15-1788 binding to human recombinant α1β3
T16568	PR-924	Proteasome	Proteases/Proteasome; Ubiquitination
	PR-924 is a selective inhibitor of tripeptide epoxyketone immunoproteasome subunit LMP-7 (IC50: 22 nM). PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities. PR-924 covalently modifies proteasomal N-terminal threonine active sites.
T13734	ILS-920	Others	Others
	ILS-920 is a Rapamycin analog characterized by diminished immunosuppressive effects but remarkable neuroprotective properties. It exhibits selective binding affinity towards the immunophilin FKBP52 as well as the β1-subunit of L-type voltage-gated calcium channels (VGCC). ILS-920 displays a notable 200-fold preference for FKBP52 over FKBP12.
T63003	NMDA receptor potentiator-1
	NMDA receptor potentiator-1 (Compound 1368) 是一种亚基选择性的 NMDA receptor 增强剂。NMDA receptor potentiator-1 对 NR2C 和 NR2D 表达的 IC50 值分别为 4 μM 和 5 μM。
T27157	Dezapelisib INCB-040093,INCB 040093,INCB040093
	Dezapelisib is an orally bioavailable, selective inhibitor of the delta isoform of the 110 kDa catalytic subunit of class I phosphoinositide-3 kinases (PI3K). INCB040093 prevents both the production of the second messenger phosphatidylinositol-3,4,5-trisp
T39286	Br-PBTC
	Br-PBTC is a highly potent, 2/4 subtype-selective positive allosteric modulator of nicotinic acetylcholine receptors (nAChRs). It specifically targets α2β2, α2β4, α4β2, α4β4, (α4β2)2α4, and (α4β2)2β2 subtypes of nAChRs, with EC50 values ranging from 0.1 to 0.6 μM. Br-PBTC exerts its activity by binding to the c-tail region of an α subunit.
T79374	NMDA receptor antagonist 7	iGluR	Membrane transporter/Ion channel; Neuroscience
	NMDA receptor antagonist7 (Compound (S)-10a) 为针对 GluN2B 亚基具有选择性的 NMDA 受体拮抗剂，展现出 Ki 值为 93 nM 和 IC50 值为 72 nM。该化合物适用于神经退行性疾病的研究。
T39771	nAChR agonist CMPI hydrochloride
	nAChR agonist CMPI hydrochloride is a potent and selective positive allosteric modulator (PAM) of nAChR containing a α4:α4 subunit interface. nAChR agonist CMPI hydrochloride enhances the response of (α4) 3 (β2) 2 nAChR to ACh (10 μM) with an EC 50 of 0.26 μM. nAChR agonist CMPI hydrochloride has potential for the research of nicotine dependence and many neuropsychiatric conditions associated with decreased brain cholinergic activity.
T35525	PI3-Kinase α Inhibitor 2 PI3-Kinase α Inhibitor 2
	Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of the 3' hydroxyl position of PIs to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits, whereas PI3Kγ is a class 1B PI3K composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit. PI3Kα inhibitor 2 is a selective inhibitor of PI3Kα with IC50 values of 2, 16, 660, and 220 nM for the α, β, γ, and 2Cβ isoforms, respectively. It...
T77154	Etrolizumab
	Etrolizumab (rhuMAb Beta7) 是一种肠道选择性抗-β7整合素单克隆抗体。Etrolizuma b 是针对α4β7和 αEβ7 整合素的 β7 亚基的特异性靶向活性分子。Etrolizumab 可用于炎症性肠病 (IBD) 的研究。
T36678	Rp-8-CPT-cAMPS sodium
	Rp-8-CPT-cAMP is a structural combination of the lipophilic and non-hydrolyzable cAMP analogs, 8-CPT-cyclic AMP and Rp-cyclic AMPS .[1] It functions as a site-selective inhibitor of protein kinase A (PKA) type I and II, with preference towards site A of type I and site B of type II.2 By occupying cAMP binding sites at the regulatory subunit of PKA, Rp-8-CPT-cAMP prevents the kinase holoenzyme from dissociative activation.[2],[3]
T73824	Thymidine 3',5'-diphosphate tetrasodium
	Thymidine 3',5'-diphosphate (Deoxythymidine 3′,5′-diphosphate) tetrasodium，为一种选择性抑制剂，主要针对葡萄球菌核酸酶及含1的都铎结构域(SND1，MicroRNA调控复合体RISC亚基)和[3,5-2H2]酪氨酸核酸酶([3,5-2H2] tyrosyl nuclease)。此化合物还展示了抗肿瘤活性，并可在生化反应中作为催化剂使用。
T37419	Zetomipzomib
	KZR-616, a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. KZR-616 has the potential for the research of multiple autoimmune diseases[1][2]. KZR-616 also inhibits MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=688 nM). KZR-616 maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells. KZR-616 (250 nM) shows a comparable cytokine inhib...
T35432	α-Conotoxin ImI (trifluoroacetate salt)
	α-Conotoxin ImI is a conotoxin that has been found inC. imperialisand has receptor antagonist and anticancer activities.1It is a peptide antagonist of homomeric α7 nicotinic acetylcholine receptors (nAChRs; IC50= 220 nM). α-Conotoxin ImI is selective for α7 nAChRs over α2β2, α3β2, α4β2, α2β4, α3β4, α4β4, and α1β1γδ subunit-containing nAChRs at 5 μM but does inhibit homomeric α9 nAChRs (IC50= 1,800 nM). Administration of paclitaxel in micelles containing α-conotoxin ImI decreases tumor growth in ...
T73986	ONX-0914 TFA
	ONX-0914 (PR-957) TFA 为针对免疫蛋白酶体中的LMP7（低分子量多肽-7）的选择性抑制剂，LMP7为类糜蛋白酶亚单位。该化合物通过抑制细胞因子产生，减缓实验性关节炎进展，并已证实为分枝杆菌蛋白酶体的非竞争性不可逆抑制剂（Ki=5.2 μM）。此外，ONX-0914 TFA 能通过HSF-1介导的p-TEFb活化，激活潜伏的HIV-1。

化合物

Cat.No: T22748

Target: NMDAR

Cat.No: T15401

Target: DNA/RNA Synthesis

Cat.No: T14971

Target: NMDAR

Cat.No: T22192

Synonym: BMS614

Target: Retinoid Receptor

Cat.No: T7870

Synonym: TCN-201

Target: NMDAR, iGluR

Cat.No: T21824

Synonym: NSC 65390,IFB-088

Target: Phosphatase

Cat.No: T12758

Target: NMDAR

Cat.No: T5375

Target: GABA Receptor

Cat.No: T2067

Synonym: NS 11394

Target: GABA Receptor

Cat.No: T39217

Target: PKA

Cat.No: T9174

Synonym: Sephin 1,lcerguastat,IFB-088

Target: Phosphatase

α-Conotoxin MII

Cat.No: TP2063

Target: AChR

Cat.No: T38272

Target: AChR, Parasite

Cat.No: T73447

Cat.No: T16795

Synonym: Capzimin intermediate

Target: Others

threo Ifenprodil hemitartrate

Cat.No: T23457

Target: Others

Ro 25-6981 Maleate

Cat.No: T12758L

Target: Others

Cat.No: T30428

Synonym: Besonprodil (USAN),UNII-5K3N2D15WW,253450-09-8,CHEMBL219631,CI-1041

Traxoprodil Mesylate

Cat.No: TQ0233L

Cat.No: T70620

Cat.No: T24717

Synonym: Ro 25 6981 HCl

Thymidine 3',5'-disphosphate

Cat.No: T24609

Synonym: Thymidine 3',5'-biphosphate,pdTp

Cat.No: T17193

Target: Others

TC-1698 dihydrochloride

Cat.No: T68697

Sephin1 Hydrochloride

Cat.No: T69440

Cat.No: T37421

GluN2B receptor modulator-1

Cat.No: T39694

Synonym: GluN2B receptor modulator-1

EVT-101 free base

Cat.No: T68973

α-Conotoxin AuIB

Cat.No: TP2061

Cat.No: T16292

Target: Thrombin

AZD4573 HCl (2057509-72-3 free base)

Cat.No: T10436L

Synonym: AZD4573 hydrochloride,AZD4573,AZD4573 HCl,AZD-4573,AZD 4573

Cat.No: T24919

Synonym: UBP 714,UBP-714

Cat.No: T29228

Synonym: ZK-93423,ZK 93423

Cat.No: T16568

Target: Proteasome

Cat.No: T13734

Target: Others

NMDA receptor potentiator-1

Cat.No: T63003

Cat.No: T27157

Synonym: INCB-040093,INCB 040093,INCB040093

Cat.No: T39286

NMDA receptor antagonist 7

Cat.No: T79374

Target: iGluR

nAChR agonist CMPI hydrochloride

Cat.No: T39771

PI3-Kinase α Inhibitor 2

Cat.No: T35525

Synonym: PI3-Kinase α Inhibitor 2

Cat.No: T77154

Rp-8-CPT-cAMPS sodium

Cat.No: T36678

Thymidine 3',5'-diphosphate tetrasodium

Cat.No: T73824

Cat.No: T37419

α-Conotoxin ImI (trifluoroacetate salt)

Cat.No: T35432

Cat.No: T73986

Cat. No.	Product Name	Target	Signaling Pathways
T15467	Helenalin	Others	Others
	Helenalin is a selective inhibitor of transcription factor NF-κB by direct targeting of p65. It is an anti-inflammatory sesquiterpene lactone compound with alkylating activity. Through its ability to target the cysteine sulfhydryl groups in the p65 subunit of NF-κB, helenalin effectively inhibits its DNA binding.
T75540	Ipomoeassin F
	Ipomoeassin F 是一种高效且具有选择性的内质网(ER)蛋白转位抑制剂，它通过作用于ER膜上的Sec61复合物（Sec61α）的成孔亚基来实现其功能。此化合物能特异性抑制SARS-CoV-2蛋白在ER膜上的转位，同时阻碍分泌蛋白和I型跨膜蛋白（TMP）的ER转运，但对III型TMP的转运不产生影响。

天然产物

Cat.No: T15467

Target: Others

Cat.No: T75540

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