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Search Results for " nanomolar "

153

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T64320	ML251	Glucokinase; Parasite	Metabolism; Microbiology/Virology
	ML251 是一种有效的新型纳摩尔 T. brucei 和 T. cruzi 磷酸果糖激酶抑制剂，对 T. brucei PFK 和 T. cruzi PFK 的 IC50值为 0.37和 0.13 μM，可研究寄生虫。
T8507	MAC-545496	Antibacterial	Microbiology/Virology
	MAC-545496 是一种抗毒剂，可逆转耐甲氧西林的菌株中的 β-内酰胺耐药性。它是糖肽抗性相关蛋白 R 的纳摩尔抑制剂，对全长 GraR 蛋白具有很强的结合亲和力。
T6322	Copanlisib BAY 80-6946,可泮利塞,库潘尼西	Apoptosis; PI3K	Apoptosis; PI3K/Akt/mTOR signaling
	Copanlisib (BAY 80-6946) 是一种选择性的和 ATP 竞争性的泛 I 类PI3K 抑制剂，具有抗肿瘤活性，对PI3Kα，PI3Kδ，PI3Kβ和PI3Kγ的IC50分别为 0.5 nM、0.7 nM、3.7 nM 和 6.4 nM。
T14998	Copanlisib dihydrochloride 库潘尼西盐酸,BAY 80-6946 dihydrochloride	Apoptosis; PI3K; mTOR	Apoptosis; PI3K/Akt/mTOR signaling
	Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) 是一种选择性和 ATP 竞争性的泛 I 类 PI3K 抑制剂。它具有优越的抗肿瘤活性，对除 mTOR 以外的其他脂质和蛋白激酶的选择性也超过 2,000 倍。
T3582	BTZ043	Antibacterial; Antibiotic; DprE1	Microbiology/Virology; Others
	BTZ043 是一种 DprE1 的抑制剂，它对结核分枝杆菌 H37Rv 和耻垢分枝杆菌具有纳摩尔杀菌活性，MIC 值分别为 2.3 nM 和 9.2 nM。
T14501	BAY-2402234	Dehydrogenase; DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism
	BAY-2402234 是一种选择性二氢乳清酸脱氢酶的抑制剂，可研究骨髓恶性肿瘤。
T6931	PD0166285 PD-166285	Apoptosis; Wee1; Chk	Apoptosis; Cell Cycle/Checkpoint
	PD0166285是 P-gp 的底物，是一种有效的 Wee1 和 Chk1 抑制剂弱抑制。
T12328	OSMI-4	Others	Others
	OSMI-4是一种低纳摩尔的O-GlcNAc 转移酶（OGT）抑制剂（在细胞中的EC50为3μM）,可用来研究不同人类细胞系中的OGT 抑制作用。
T8701	GRP-60367	Others	Others
	GRP-60367 是一种小分子狂犬病病毒进入抑制剂，对某些 RABV 株具有纳摩尔作用效果。
T9295	BLU-263	c-Kit	Tyrosine Kinase/Adaptors
	BLU-263 是一种在研的、有效的、选择性的 KIT 口服小分子抑制剂，对 D816V 突变体 KIT 具有亚纳摩尔效力。
T26600	Alpidem Ananxyl,阿尔吡登	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Alpidem (Ananxyl) 可以选择性结合含有α1β2γ2 亚单位的GABAA 受体，具有抗焦虑作用。
T24040	ERDRP-0519 ERDRP0519,ERDRP 0519	Antiviral	Immunology/Inflammation
	ERDRP-0519 is an orally bioavailable small-molecule inhibitor of the Measles virus (MeV) polymerase. It effectively prevents measles disease in squirrel monkeys (Saimiri sciureus) and exhibits potent inhibition of morbilliviruses in the nanomolar range.
T2300	AZD1208	Apoptosis; Pim; Autophagy	Apoptosis; Autophagy; Chromatin/Epigenetic; JAK/STAT signaling
	AZD1208 是一种具有口服活性的高度选择性PIM 抑制剂。
T37376	PHY34	Autophagy	Autophagy
	PHY34是一种晚期自噬抑制剂，具有纳摩尔水平的抑制作用。在体内，PHY34具有抗高级别浆液性卵巢癌（HGSOC）活性。
T39039	FSCPX	Adenosine Receptor	GPCR/G Protein; Neuroscience
	FSCPX is a potent and selective irreversible antagonist of the A1 adenosine receptor (A1AR), exhibiting low nanomolar binding potency. Additionally, FSCPX can effectively decrease the interstitial adenosine level in the guinea pig atrium, thereby modifying the effect of NBTI, a nucleoside transport inhibitor.
TQ0019	RR6	Others	Others
	RR6 是竞争性的、可逆的、具有口服活性的vanin 选择性抑制剂，对重组vanin-1的IC50值为540 nM。它还有效抑制人血清泛酶(IC50:40 nM)，牛血清泛酶(IC50:41 nM)和大鼠血清泛酶(IC50:87 nM)。
T8827	EMAC10101d	Carbonic Anhydrase	Metabolism
	EMAC10101d 是 hCA II 选择性抑制剂(Ki:8.1 nM)。
T7336	ICA-121431 2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl	Sodium Channel	Membrane transporter/Ion channel
	ICA-121431 (2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl) 是强效的、广谱的电压门控钠通道阻滞剂，对人 Nav1.1 和 Nav1.3 亚型具有等效选择性，IC50分别为 13 nM 和 23 nM。它对Nav1.2 的抑制作用较弱，IC50为240 nM，对 Nav1.4、Nav1.6、抗TTX 的人 Nav1.5、Nav1.8 通道表现出大于 1000 倍的选择性，IC50>10 μM。
T10533	BI-2852	Ras	GPCR/G Protein; MAPK
	BI-2852 是具有纳摩尔亲和力的开关 I/II 口袋（SI/II-口袋）的 KRAS 抑制剂，可抑制 KRAS 突变细胞的下游信号传导和抗增殖作用。
T3506	Nazartinib 那扎替尼,EGF816,NVS-816	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Nazartinib (EGF816) 是一种共价、不可逆、突变选择性 EGFR 抑制剂，对激活 mt (L858R, ex19del) 和 T790M mt 具有纳摩尔抑制效力，在体外其选择性比野生型 (wt) EGFR 高 60 倍。
T64355	TDI-10229	cAMP	GPCR/G Protein
	TDI-10229 是一种口服有效的可溶性腺苷酸环化酶 (sAC, ADCY10) 抑制剂 (IC50 值为 195 nM)。TDI-10229 在生化和细胞分析中都显示出对 sAC 的纳摩尔级抑制，并表现出足以保证其用作体内工具化合物的小鼠药代动力学特性。
T16392	ONC206	Dopamine Receptor	GPCR/G Protein; Neuroscience
	ONC206 是一种 ONC201 的类似物，是一种多巴胺 D2- 样受体 (DRD2/3/4) 的选择性拮抗剂，其拮抗作用在纳摩尔级别。它具有广谱抗肿瘤活性。
T6828	ZL0420	Epigenetic Reader Domain	Chromatin/Epigenetic
	ZL0420 是有效且选择性的 BET 溴结构域 4 (BRD4) 抑制剂，对 BRD4 的溴结构域 (BD) 具有纳摩尔结合亲和力。ZL0420 对 BRD4 BD1和 BRD4 BD2 的IC50分别为 27 nM 和 32 nM。
T3701	MCC950 CP-456773	NOD	Immunology/Inflammation; NF-κB
	MCC950 (CP-456773) 是NLRP3的选择性抑制剂，能够作用于BMDMs(IC50:7.5 nM) 和 HMDMs(IC50:8.1 nM)。
T16703	Quarfloxin CX-3543	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Quarfloxin (CX-3543) 是一种氟喹诺酮衍生物，具有抗肿瘤活性，可靶向抑制RNA pol I 的活性，在神经母细胞瘤细胞中的 IC50 值在纳摩尔范围内。它破坏核糖体 DNA 模板中核仁蛋白和 G-四链体 DNA 结构之间的相互作用。
T28773	SI-2 SI2,EPH 116,EPH116,EPH-116	Others	Others
	SI-2是类固醇受体辅激活因子-3（SRC-3或 AIB1）的抑制剂（SMI）。SI-2可选择性降低细胞中 SRC-3的转录活性和蛋白浓度，并选择性诱导低纳摩尔范围（3-20 nM）内的乳腺癌症细胞死亡，但不影响正常细胞存活率。
T9864	Debio-0123 WEE1-IN-5	Wee1	Cell Cycle/Checkpoint
	Debio-0123 (WEE1-IN-5) 是一种口服有效且高度特异性的WEE1抑制剂，IC50值在低纳摩尔范围内。Debio-0123 抑制磷酸化 CDC2。Debio-0123 可增强卡铂在体内的抗肿瘤活性，而这两种药物单独使用都没有活性。
T8873	Bractoppin	Others; DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Others
	Bractoppin 是一种BRCA1 (t)BRCT domain 识别磷酸肽的选择性抑制剂，IC50为 74 nM。它优先抑制 BRCA1 -tBRCT 依赖的 DNA 损伤。它减少 BRCA1 对 DNA 断裂片段的招募，进而抑制损伤诱导的 G2 期阻滞和重组酶 RAD51 的组装。
T21537L	TMC647055 Choline Hydroxide Salt TMC647055 Choline Hydroxide Salt (1204416-97-6 free base)	HCV Protease	Microbiology/Virology; Proteases/Proteasome
	TMC647055 Choline Hydroxide Salt 是一种新型有效的 HCV NS5B 聚合酶非核苷抑制剂，可用于治疗 HCV 感染。它具有纳摩尔级细胞效力（EC(50) 为 82 nM），相关细胞毒性较小（CC(50)>20 μM），在大鼠和狗中具有良好的药代动力学特征。 TMC647055 显示出有体外生化、动力学和病毒学特征的前景。
T71589	AS15
	AS15 is a novel covalent nanomolar inhibitor of protein disulfide isomerase (PDI).
T26075	Rhizopodin
	Rhizopodin is a potent natural macrolide antibiotic that effectively affects the actin cytoskeleton at nanomolar concentrations.
T25169	Bodilisant
	Bodilisant is a hH3R ligand with affinity in the nanomolar concentration range that made from a piperidine-based lead structure for the human histamine H3 receptor (hH3R) with the BODIPY fluorophore.
T15618	JNJ-46281222	GluR	Neuroscience
	JNJ-46281222 is an metabotropic glutamate (mGlu) 2-selective, highly potent PAM (positive allosteric modulator). It has nanomolar affinity (Kd = 1.7 nM) and a high modulatory potency (pEC50 = 7.71).
T38839	MCX 28
	MCX 28, a triple PI3K/mTOR/PIM inhibitor, displays low nanomolar activity.
T35480	dBRD9-A dBRD9-A
	Potent BRD9 degrader. Selectively binds BRD9 and elicits near complete degradation of BRD9 at nanomolar concentrations. Inhibits growth of synovial sarcoma cells in vitro and tumor progression in a synovial sarcoma xenograft mouse model.
T69293	Lasonolide A
	Lasonolide A is a potential anticancer molecule isolated from the marine sponge Forcepia sp., with nanomolar growth inhibitory activity and a unique cytotoxicity profile against the National Cancer Institute 60-cell-line screen
T60946	SLK/STK10-IN-1
	SLK/STK10-IN-1 是具有纳摩尔效力的 SLK 和 STK10选择性抑制剂。
T69869	Cyanabactin
	Cyanabactin is a novel ABA receptor agonist. It preferentially activates Pyrabactin Resistance 1 (PYR1) with low nanomolar potency.
T82723	ChTX-Lq2
	ChTX-Lq2为Ca2+激活的K+流出抑制剂，Kd值为43 nM。
T40087	DSM502
	DSM502, a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor, demonstrates potent nanomolar activity against Plasmodium DHODH and Plasmodium parasites, while not inhibiting mammalian DHODHs.
T71353	CCT239065
	CCT239065 is a novel, selective, and efficacious nanomolar pyridopyrazinone V600EBRAF and LCK inhibitor.
T13007	ST1936 oxalate	5-HT Receptor	GPCR/G Protein; Neuroscience
	ST1936 oxalate 是一种 5-HT6 受体的选择性纳摩尔亲和激动剂，对人5-HT6、5-HT7和 5-HT2B 受体的 Ki 值分别为 13、168 和 245 nM。
T27201	DPC-082 DPC 082
	DPC-082 is a reverse transcriptase inhibitor. DPC-082 exhibits low-nanomolar potency toward wild-type virus, L100I and K103N single-mutation variants, and multiplies amino acid-substituted HIV type 1 mutants.
T78374	TfR-T12 TFA
	TfR-T12 TFA为能穿透血脑屏障的转铁蛋白受体(TfR)结合肽，展现出纳摩尔级的结合活性。
T29077	Urolinin nWWK-Tyr(3-NO2)-Abu
	Urolinin is a linear peptidic Urotensin-II Receptor Agonist with low nanomolar potency as well as improved metabolic stability. Urolinin is a hexameric UIIR agonist with an EC50 of 4.75 nM and a metabolic stability of 1319 min, 6.3-fold higher than wild-t
T36946	PW0464 PW0464
	PW0464, a nanomolar potent complete G protein biased ligand, is a noncatechol D1R agonist, with an EC50 of 5.8 nM (Gs-cAMP)[1]. PW0464 (compound 24) is found to elicit complete G protein bias, showing no activity for D1R-mediated β-arrestin recruitment[1].PW0464 (compound 24), the non-catechol agonist, forms bonds with S1985.42 and S2025.46 via its fluorine atom[2]. [1]. Pingyuan Wang, et al. Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Recept...
T35889	PB2
	PB2, a tris(2-carboxyethyl)phosphine (TCEP) analogue, enhances the survival of retinal ganglion cells (RGCs) following axotomy in vitro. Even at nanomolar and picomolar concentrations, PB2 demonstrates pronounced efficacy in promoting RGC survival. Notably, PB2 exhibits superior permeability compared to TCEP. Serving as a potent reducing agent, PB2 provides robust neuroprotection for RGCs[1].
T70096	AEG40730 HCl
	AEG40730 is a potent and selective IAP antagonist and a BIR-binding tetrapeptide. AEG40730 binds to cIAP1 and cIAP2, facilitates their autoubiquitination and proteosomal degradation, and causes a dramatic reduction in RIP1 ubiquitination. Treatment with nanomolar concentrations of AEG40730 resulted in the loss of both XIAP and c-IAP1 proteins, albeit with different kinetics.
T27388	FR-A 19 FR-A-19,FRA19
	FR-A 19, a Histamine H2 agonist, inhibits the release of IgE-mediated human basophil histamine in a nanomolar range. It has additional potent anti-allergic properties.
T61844	HIV-1 inhibitor-9
	HIV-1 inhibitor-9 exhibits potent inhibition activity at low nanomolar concentrations against both the wild-type (WT) HIV-1 strain and multiple strains that have developed resistance to non-nucleoside reverse transcriptase inhibitors (NNRTIs).

化合物

Cat.No: T64320

Target: Glucokinase, Parasite

Cat.No: T8507

Target: Antibacterial

Cat.No: T6322

Synonym: BAY 80-6946,可泮利塞,库潘尼西

Target: Apoptosis, PI3K

Copanlisib dihydrochloride

Cat.No: T14998

Synonym: 库潘尼西盐酸,BAY 80-6946 dihydrochloride

Target: Apoptosis, PI3K, mTOR

Cat.No: T3582

Target: Antibacterial, Antibiotic, DprE1

Cat.No: T14501

Target: Dehydrogenase, DNA/RNA Synthesis

Cat.No: T6931

Synonym: PD-166285

Target: Apoptosis, Wee1, Chk

Cat.No: T12328

Target: Others

Cat.No: T8701

Target: Others

Cat.No: T9295

Target: c-Kit

Cat.No: T26600

Synonym: Ananxyl,阿尔吡登

Target: GABA Receptor

Cat.No: T24040

Synonym: ERDRP0519,ERDRP 0519

Target: Antiviral

Cat.No: T2300

Target: Apoptosis, Pim, Autophagy

Cat.No: T37376

Target: Autophagy

Cat.No: T39039

Target: Adenosine Receptor

Cat.No: TQ0019

Target: Others

Cat.No: T8827

Target: Carbonic Anhydrase

Cat.No: T7336

Synonym: 2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl

Target: Sodium Channel

Cat.No: T10533

Target: Ras

Cat.No: T3506

Synonym: 那扎替尼,EGF816,NVS-816

Target: EGFR

Cat.No: T64355

Target: cAMP

Cat.No: T16392

Target: Dopamine Receptor

Cat.No: T6828

Target: Epigenetic Reader Domain

Cat.No: T3701

Synonym: CP-456773

Target: NOD

Cat.No: T16703

Synonym: CX-3543

Target: DNA/RNA Synthesis

Cat.No: T28773

Synonym: SI2,EPH 116,EPH116,EPH-116

Target: Others

Cat.No: T9864

Synonym: WEE1-IN-5

Target: Wee1

Cat.No: T8873

Target: Others, DNA/RNA Synthesis

TMC647055 Choline Hydroxide Salt

Cat.No: T21537L

Synonym: TMC647055 Choline Hydroxide Salt (1204416-97-6 free base)

Target: HCV Protease

Cat.No: T71589

Cat.No: T26075

Cat.No: T25169

Cat.No: T15618

Target: GluR

Cat.No: T38839

Cat.No: T35480

Synonym: dBRD9-A

Cat.No: T69293

Cat.No: T60946

Cat.No: T69869

Cat.No: T82723

Cat.No: T40087

Cat.No: T71353

Cat.No: T13007

Target: 5-HT Receptor

Cat.No: T27201

Synonym: DPC 082

Cat.No: T78374

Cat.No: T29077

Synonym: nWWK-Tyr(3-NO2)-Abu

Cat.No: T36946

Synonym: PW0464

Cat.No: T35889

Cat.No: T70096

Cat.No: T27388

Synonym: FR-A-19,FRA19

HIV-1 inhibitor-9

Cat.No: T61844

Cat. No.	Product Name	Target	Signaling Pathways
T15027	Cyclopiazonic acid 环匹阿尼酸,环二氮酸	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Cyclopiazonic acid 是一种神经毒性次级代谢产物 (SM)，源于A. flavus，是一种纳摩尔内质网钙 ATP 酶抑制剂 (Ca2+ATPase; SERCA)，是植物细胞死亡的有效诱导剂。
T5061	Lumichrome 7,8-Dimethylalloxazine,光色素	Others	Others
	Lumichrome (7,8-Dimethylalloxazine) 是人类体内的内源性化合物，由核黄素光降解产生。它利用 p53 依赖机制抑制人肺癌细胞生长并诱导凋亡。
TN2496	1,4-Anthraquinone	Others	Others
	1,4-Anthraquinone 是一种抗癌药物，在体外与柔红霉素相同纳摩尔范围内阻断核苷转运、抑制大分子合成、诱导 DNA 片段化并降低 L1210 白血病细胞的生长和活力。它被提议为一种用于高效液相色谱 (HPLC) 测定药物制剂中 N-乙酰半胱氨酸 (NAC) 和卡托普利 (CAP) 的新型柱前试剂。
T37471	Makisterone A
	Makisterone A is an ecdysteroid that drives molting in insects. It binds the heterodimeric ecdysone receptor with nanomolar affinity.
T36068	Brevetoxin B
	Brevetoxin B is a polyketide neurotoxin produced by Karenia species and other dinoflagellates. It binds to site 5 on the alpha subunit of voltage-gated sodium channels (IC50 = 15 nM) on neurons at the neuromuscular junction, causing the channel to open irreversibly at potentials more negative than normal, discharging action potentials repetitively. Brevetoxin B is ichthyotoxic at nanomolar concentrations and is responsible for an illness described as neurotoxic shellfish poisoning.
T13123	Tentoxin	Endogenous Metabolite	Metabolism
	Tentoxin 是一种由植物致病真菌产生的环状肽，在敏感植物中，当其浓度在纳摩尔到微摩尔之间时，会使 F1马达失活，而更高的浓度会超过该酶的天然活性

天然产物

Cyclopiazonic acid

Cat.No: T15027

Synonym: 环匹阿尼酸,环二氮酸

Target: Calcium Channel

Cat.No: T5061

Synonym: 7,8-Dimethylalloxazine,光色素

Target: Others

1,4-Anthraquinone

Cat.No: TN2496

Target: Others

Cat.No: T37471

Cat.No: T36068

Cat.No: T13123

Target: Endogenous Metabolite

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