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63

抑制剂 & 化合物

2

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Cat. No.	Product Name	Target	Signaling Pathways
T36758	CAIX Inhibitor S4 S4	Carbonic Anhydrase	Metabolism
	CAIX Inhibitor S4 (S4) 是一种有效的碳酸酐酶 IX/XII 抑制剂，Ki 分别为 7 nM 和 2 nM。 CA II 和 CA I 的 Ki 分别为 546 和 5600 nM。
T71516	RhlR Agonist S4
	RhlR agonist S4 is a quorum sensing modulator as an RhlR agonist.
T74891	Apratoxin S4
	Apratoxin S4（Apra S4）是一种Sec61抑制剂，能够有效阻止分泌蛋白的共翻译转运进入内质网(ER)。它对flaviviruses类病毒显示出抗病毒效果，IC50值在0.46 nM至170 nM不等。此外，Apratoxin S4通过抑制多条血管生成通路，能够抑制视网膜血管细胞活化，适用于病毒感染、血管生成相关疾病和癌症的研究。
T24072	Franganine Daechuine S4
	Franganine is a 14-membered-ring cyclopeptide analgesic alkaloid.
T2108	Andarine S-4,GTx-007	Androgen Receptor	Endocrinology/Hormones
	Andarine (GTx-007) 是一种选择性的、具有口服活性的、非甾体受体雄激素受体(AR)调节剂 (SARM) 和部分激动剂，Ki=4 nM。它是一种具有较强活性的、具有组织选择性的 SARM。
T9146	ms48107 Benzenemethanol, 2-[4-amino-6-[[(4-phenoxyphenyl)methyl]amino]-1,3,5-triazin-2-yl]-3-fluoro-	Others	Others
	MS48107 是 G 蛋白偶联受体 68 (GPR68) 的选择性正变构调节剂，对GPR68的选择性高于密切相关的神经递质转运蛋白，质子 GPCR 和 hERG 离子通道。它可以穿越过小鼠的血脑屏障。
T12112	MS402	Epigenetic Reader Domain	Chromatin/Epigenetic
	MS402 是一种新型 BD1 选择性 BET BrD 抑制剂，阻断 Th17 细胞分化并改善小鼠结肠炎，对BRD4(BD1)、BRD4(BD2)、BRD3(BD1)、BRD3(BD2)、BRD2(BD1)和BRD2(BD2)的Ki 分别为 77 、718、110、200、83 和 240 nM。
T16153	MS4078	ALK; Ligand for E3 Ligase; PROTACs	Angiogenesis; PROTAC; Tyrosine Kinase/Adaptors
	MS4078 是一种基于 Cereblon 配体的间变性淋巴瘤激酶 PROTAC ，结合 ALK 的 Kd 为 19 nM。
T1854	MS436	Epigenetic Reader Domain	Chromatin/Epigenetic
	MS436 是溴结构域抑制剂，作用于 BRD4 BrD1的Ki 为 30 到 50 nM 之间，比作用于 BrD2 选择性高 10 倍。
T3274	S49076	FGFR; c-Met/HGFR; TAM Receptor	Angiogenesis; Tyrosine Kinase/Adaptors
	S49076 是一种新型 MET、AXL/MER 和 FGFR1/2/3 高效抑制剂，IC50<20 nM。
T24677	PS47 PS 47,PS-47	PDK	PI3K/Akt/mTOR signaling
	PS-47(PS 47) 是一种 PS48 的非活性 E-异构体。其中 PS48 是一种 PDK1 的激活剂。PS47 (PS 47) 可用作 PS48 的阴性对照。
T6967	RHPS4 RHPS 4 methosulfate,NSC714187	Apoptosis; Telomerase	Apoptosis; DNA Damage/DNA Repair
	RHPS4 (RHPS 4 methosulfate) 是 DNA 损伤诱导剂，是一种有效的亚微摩尔端粒酶抑制剂，IC50为0.33 μM。
T16154	MS417 GTPL7512	Epigenetic Reader Domain; HIV Protease	Chromatin/Epigenetic; Microbiology/Virology; Proteases/Proteasome
	MS417 (GTPL7512) 是一种 BET 特异性 BRD4 抑制剂，与 BRD4-BD1 和 BRD4-BD2 结合，Kd 值分别为 36.1和25.4 nM，IC50值分别为 30和46 nM。它对 CBP BRD 的选择性较低，IC50值为 32.7 μM。
T21714	BMS453 BMS 453,BMS-189453	Retinoid Receptor	Metabolism
	BMS453 (BMS-189453) 是一种合成类维生素 A，是一种 RARβ激动剂，也是一种 RARα/RARγ拮抗剂。它主要通过诱导活性 TGFβ 来抑制乳腺细胞生长。
T14689	BMS493 BMS-493	Phospholipase; Retinoid Receptor	Metabolism
	BMS493 是泛维甲酸受体（RAR）的逆激动剂，可抑制维甲酸诱导的分化，增强核共抑制因子与 RARs 的相互作用，减弱 RA 信号传导，增强了 TPP 诱导的毒性，抑制磷脂酶 A2 活性的增加。
T37655	DS44960156	DHFR	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism
	DS44960156 是一种新型选择性亚甲基四氢叶酸脱氢酶 2 (MTHFD2) 的抑制剂，抑制 MTHFD2 和 MTHFD1，可用于研究癌症。
T40293	GPS491	Antiviral; HIV Protease	Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	GPS491 具有抗病毒活性，通过改变 RNA 加工来抑制 HIV-1、腺病毒和冠状病毒复制。
T40233	(Iso)-MS4322 (Iso)-YS43-22,MS4322 (isomer),YS43-22 (isomer)	Histone Methyltransferase; PROTACs	Chromatin/Epigenetic; PROTAC
	(Iso)-MS4322 ((Iso)-YS43-22) 是一种具有选择性和强效性的蛋白质精氨酸甲基转移酶 5 (PRMT5) 降解剂，具有潜在的抗癌活性，有效地降低 MCF-7 细胞中的 PRMT5 蛋白水平，可抑制多种癌细胞的生长。
T13090	TAS4464 hydrochloride	E1/E2/E3 Enzyme; NEDD8	Metabolism; Ubiquitination
	TAS4464 hydrochloride 是高效的、选择性的 NEDD8 活化酶 (NAE)抑制剂，其 IC50=0.955 nM。
T2340	AC1NS4RE	Tyrosinase	Proteases/Proteasome
	是一种化学合成中的砌块
T78170	Kras4B G12D-IN-1	Ras	GPCR/G Protein; MAPK
	Kras4B G12D-IN-1为Kras4B G12D的抑制剂，表现出抗癌活性。在降低Kras4B G12D表达的小鼠胚胎成纤维细胞(MEF)中减少Kras蛋白水平。
T13090L	TAS4464	E1/E2/E3 Enzyme	Ubiquitination
	TAS4464 is a highly potent and selective inhibitor of the NEDD8 activating enzyme (IC50: 0.955 nM).
T76302	[Lys4] Sarafotoxin S6c
	[Lys4] Sarafotoxin S6c 是一种 sarafotoxin 类似物，是一种有效的内皮素受体 (endothelin receptor) 的部分激动剂。[Lys4] Sarafotoxin S6c 可诱导猪冠状动脉收缩，其 EC50为 1.5 nM。
T24547	NS4591 NS 4591,NS-4591
	NS4591 is a modulator of SK-IK channels.
T15013	CS476 NSC302998	Others	Others
	CS476 is a potent drug of hypoglycaemic.
T32419	KRAS4b-PDEδ stabilizer C19
	KRAS4b-PDEδ stabilizer C19 is a stabilizer of the KRAS4b-PDEδ complex which decreases the proliferation of colorectal cancer cells, and increases apoptosis via decreased activation of oncogenic KRAS4b signaling.
T73433	MS47134
	MS47134是一种MRGPRX4激动剂，具有高效性和选择性，其EC50为149 nM。该化合物可应用于疼痛、瘙痒以及肥大细胞介导的超敏反应研究。
T69528	GTS467
	GTS467 is a EAAT2 Activator.
T28116	MS453 MS-453,MS 453
	MS453 is a potent and selective SETD8 inhibitor with an IC50 value of 804 nM.
T73453	MRS4719
	MRS4719 是一种有效的P2X4受体拮抗剂，对人 P2X4 受体的IC50为 0.503 μM。MRS4719 可减少脑梗死体积，减少脑萎缩，在缺血性脑中风模型中具有神经保护和神经康复作用。MRS4719 还能减少 ATP 诱导的人单核细胞源性巨噬细胞 [Ca2+]i 内流。MRS4719 可用于研究缺血性脑中风。
T71717	KRAS4b-IN-D14
	KRAS4b-IN-D14 is a specific inhibitor of oncogenic KRAS4b signaling which stabilizes the KRAS4b-PDEδ complex and remarkably decreases tumor size and triggered apoptosis of tumor cells.
T24676	PS423 PS210AM,PS 210 AM,PS 423,PS210-AM,PS-423
	PS423 is a substrate-selective protein kinase PDK1 inhibitor that acts by binding to the PIF-pocket allosteric docking site.
T40719	(Cys47)-HIV-1 tat Protein (47-57) (Cys47)-HIV-1 tat Protein (47-57)
	(Cys47)-HIV-1 tat Protein (47-57) possesses membrane translocation functionality and can serve as a surface derivatization agent for magnetic pharmaceuticals, thereby enhancing their uptake into specific target cells.
T35636	SHS4121705
	SHS4121705 is an orally bioavailable mitochondrial uncoupler.1It increases oxygen consumption rate in L6 rat myoblast cells with an EC50value of 4.3 μM. SHS4121705 (25 mg/kg per day in the diet) reduces hepatic steatosis, liver triglyceride levels, and plasma alanine aminotransferase (ALT) levels in Stelic animal model (STAM) mice, a model of non-alcoholic steatohepatitis (NASH). 1.Salamoun, J.M., Garcia, C.J., Hargett, S.R., et al.6-Amino[1,2,5]oxadiazolo[3,4-b]pyrazin-5-ol derivatives as effic...
T24503	MS438 MS-438,MS 438
	MS438 is an effective agonist of the TSH receptor.
T24498	MRS4458 MRS 4458,MRS-4458
	MRS4458 is an effective inhibitor of the P2Y14 Receptor.
T13781	MS4077	ALK; PROTACs	Angiogenesis; PROTAC; Tyrosine Kinase/Adaptors
	MS4077 is an degrader of anaplastic lymphoma kinase (ALK) PROTAC(Kd of 37 nM for binding affinity to ALK).
T63242	MRS4738
	MRS4738 is a potent antagonist with high affinity for the P2Y14R receptor. It demonstrates in vivo anti-hyperallodynic and antiasthmatic activity [1].
T28458	PS432 PS-432,PS 432
	PS432 is an allosteric inhibitor of atypical PKCs. PS432 targets the PIF-pocket resulting in significantly reduce tumor growth without side effects in mouse xenograft model.
T76521	HCV NS4A Protein (18-40) (JT strain)
	HCVNS4A Protein (18-40) (JT strain) 为HCVNS4A 肽，由第18至40个NS4A蛋白残基构成，能够增强NS3蛋白酶的催化效率。
T82378	Folate-MS432	PROTACs	PROTAC
	Folate-MS432作为PROTAC，通过叶酸受体依赖途径特异性降解癌细胞中的MEKs。
T13782	MS432	MEK; PROTACs	MAPK; PROTAC
	MS432 is a highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2.
T73452	MRS4596
	MRS4596为高效P2X4受体 (P2X4 receptor) 选择性拮抗剂，对人P2X4受体的IC50达1.38 μM。在缺血性脑卒中模型中，MRS4596显示出神经保护及神经康复的效应，适用于缺血性脑卒中的研究。
T3512	S49076 HCl S-49076 Hydrochloride	FGFR; c-Met/HGFR; TAM Receptor	Angiogenesis; Tyrosine Kinase/Adaptors
	S49076 HCl (S-49076 Hydrochloride) 是 MET、AXL/MER 和 FGFR1/2/3 的有效抑制剂。S49076 HCl 在体外和体内有效阻断 MET、AXL 和 FGFR 的细胞磷酸化并抑制下游信号传导。在细胞模型中，S49076 HCl (S-49076 Hydrochloride) 抑制 MET 和 FGFR2 依赖性胃癌细胞的增殖，阻断 MET 驱动的肺癌细胞迁移，并抑制表达 FGFR1/2 和 AXL 的肝癌细胞的集落形成。在肿瘤异种移植模型中，建立了口服 S49076 HCl (S-49076 Hydrochloride) 后 MET 和 FGFR2 抑制的良好药代动力学/药效学关系，并与对肿瘤生长的影响密切相关。
T29890	AlPcS4 Aluminum phthalocyanine tetrasulfonate tetrasodium,Chloroaluminum tetrasulfophthalocyanine
	AlPcS4 , also known as aluminum phthalocyanine tetrasulfonate Chloroaluminum tetrasulfophthalocyanine; or AlS4Pc, AlPcS4(a), is a potent photosensitizer, and is potentially useful in cancer sonodynamic therapy and cancer photodynamic therapy. Aluminum pht
T39712	RGLS4326 RG4326,RGLS4326
	RGLS4326 (RG4326) is a short oligonucleotide inhibitor of microRNA-17 (miR-17), with a pioneering role in its class. This compound, with a research focus on autosomal dominant polycystic kidney disease (ADPKD), effectively suppresses the activity of miR-17 in HeLa cells, displaying an EC50 value of 28.3 nM.
T40349	DS45500853
	DS45500853, an estrogen-related receptor α (ERRα) agonist, acts as an inhibitor of the binding interaction between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM), exhibiting an IC50 of 0.80 μM. This compound holds potential for research pertaining to metabolic disorders, particularly type 2 diabetes mellitus (T2DM).
T72793	YEATS4 binder-1
	YEATS4 binder-1(4e) 是一种有效的选择性YEATS4结合剂，可以与 YEATS 结构域的 KAc 识别位点结合，其Ki 值为37 nM。
T24502	MS437 MS 437,MS-437
	MS437 is a potent TSH receptor agonist.
T10887	CRS400393	Antibacterial	Microbiology/Virology
	CRS400393 is an effective anti-mycobacterial drug , with MIC of 0.03, 2, and ≤ 0.12 µg/mL against M. abs., M. avium, M. intracellulare, and M. tuberculosis, respectively.

化合物

CAIX Inhibitor S4

Cat.No: T36758

Synonym: S4

Target: Carbonic Anhydrase

RhlR Agonist S4

Cat.No: T71516

Cat.No: T74891

Cat.No: T24072

Synonym: Daechuine S4

Cat.No: T2108

Synonym: S-4,GTx-007

Target: Androgen Receptor

Cat.No: T9146

Synonym: Benzenemethanol, 2-[4-amino-6-[[(4-phenoxyphenyl)methyl]amino]-1,3,5-triazin-2-yl]-3-fluoro-

Target: Others

Cat.No: T12112

Target: Epigenetic Reader Domain

Cat.No: T16153

Target: ALK, Ligand for E3 Ligase, PROTACs

Cat.No: T1854

Target: Epigenetic Reader Domain

Cat.No: T3274

Target: FGFR, c-Met/HGFR, TAM Receptor

Cat.No: T24677

Synonym: PS 47,PS-47

Target: PDK

Cat.No: T6967

Synonym: RHPS 4 methosulfate,NSC714187

Target: Apoptosis, Telomerase

Cat.No: T16154

Synonym: GTPL7512

Target: Epigenetic Reader Domain, HIV Protease

Cat.No: T21714

Synonym: BMS 453,BMS-189453

Target: Retinoid Receptor

Cat.No: T14689

Synonym: BMS-493

Target: Phospholipase, Retinoid Receptor

Cat.No: T37655

Target: DHFR

Cat.No: T40293

Target: Antiviral, HIV Protease

Cat.No: T40233

Synonym: (Iso)-YS43-22,MS4322 (isomer),YS43-22 (isomer)

Target: Histone Methyltransferase, PROTACs

TAS4464 hydrochloride

Cat.No: T13090

Target: E1/E2/E3 Enzyme, NEDD8

Cat.No: T2340

Target: Tyrosinase

Kras4B G12D-IN-1

Cat.No: T78170

Target: Ras

Cat.No: T13090L

Target: E1/E2/E3 Enzyme

[Lys4] Sarafotoxin S6c

Cat.No: T76302

Cat.No: T24547

Synonym: NS 4591,NS-4591

Cat.No: T15013

Synonym: NSC302998

Target: Others

KRAS4b-PDEδ stabilizer C19

Cat.No: T32419

Cat.No: T73433

Cat.No: T69528

Cat.No: T28116

Synonym: MS-453,MS 453

Cat.No: T73453

Cat.No: T71717

Cat.No: T24676

Synonym: PS210AM,PS 210 AM,PS 423,PS210-AM,PS-423

(Cys47)-HIV-1 tat Protein (47-57)

Cat.No: T40719

Synonym: (Cys47)-HIV-1 tat Protein (47-57)

Cat.No: T35636

Cat.No: T24503

Synonym: MS-438,MS 438

Cat.No: T24498

Synonym: MRS 4458,MRS-4458

Cat.No: T13781

Target: ALK, PROTACs

Cat.No: T63242

Cat.No: T28458

Synonym: PS-432,PS 432

HCV NS4A Protein (18-40) (JT strain)

Cat.No: T76521

Cat.No: T82378

Target: PROTACs

Cat.No: T13782

Target: MEK, PROTACs

Cat.No: T73452

Cat.No: T3512

Synonym: S-49076 Hydrochloride

Target: FGFR, c-Met/HGFR, TAM Receptor

Cat.No: T29890

Synonym: Aluminum phthalocyanine tetrasulfonate tetrasodium,Chloroaluminum tetrasulfophthalocyanine

Cat.No: T39712

Synonym: RG4326,RGLS4326

Cat.No: T40349

YEATS4 binder-1

Cat.No: T72793

Cat.No: T24502

Synonym: MS 437,MS-437

Cat.No: T10887

Target: Antibacterial

Cat. No.	Product Name	Target	Signaling Pathways
T81843	Maximin S4
	Maximin S4为Bombina maxima蟾蜍源抗菌肽，对支原体表现出抗菌效能。
T80309	Dermaseptin-S4
	Dermaseptin-S4为源自青蛙皮肤的抗菌肽，具有针对丝状真菌的抗菌活性。

天然产物

Cat.No: T81843

Cat.No: T80309

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