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77

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
TP2281	p53 tumor suppressor fragment	Others	Others
	p53 tumor suppressor fragment (232-240) is a peptide with the sequence H2N-Lys-Tyr-Met-Cys-Asn-Ser-Ser-Cys-Met-OH, MW= 1066.3. p53 is a tumor suppressor protein that in humans is encoded by the TP53 gene. p53 is crucial in multicellular organisms, where i
T8497	SX-682	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	SX-682 是口服有效的 CXCR1和 CXCR2变构抑制剂，可以阻断肿瘤髓系抑制细胞募集并增强 T 细胞活化和抗肿瘤免疫，具有治疗去势抵抗性前列腺癌的潜力。
T16269	Nanaomycin A	DNA Methyltransferase; Dehydrogenase; Parasite	Chromatin/Epigenetic; Metabolism; Microbiology/Virology
	Nanaomycin A 是一种醌类抗生素，可重新激活人类癌细胞中沉默的肿瘤抑制基因。 Nanaomycin A 是 DNMT3B 的特异性抑制剂 (IC50 = 500 nM)。
T6696	Tazarotene 他扎罗汀,Tazorac,AGN 190168,Zorac	Retinoid Receptor; Autophagy	Autophagy; Metabolism
	Tazarotene (Zorac) 是一种选择性视黄酸受体激动剂，用于研究寻常痤疮和斑块状银屑病。
T3184	Kevetrin hydrochloride Thioureidobutyronitrile HCl,thioureido butyronitrile hydrochloride,4-Isothioureidobutyronitrile hydrochloride	Mdm2; p53	Apoptosis
	Kevetrin hydrochloride (4-Isothioureidobutyronitrile hydrochloride) 是一种小分子，是肿瘤抑制蛋白 p53 的激活剂，具有潜在的抗肿瘤活性。
T8967	SW155246	DNA Methyltransferase	Chromatin/Epigenetic
	SW155246 是选择性 DNA 甲基转移酶 (DNMT1) 抑制剂，能够抑制 hDNMT1 (IC50:1.2 μM) 以及 mDNMT3A (IC50:38 μM)。它能够促使 A549细胞中肿瘤抑制基因 RASSF1的重新表达，可用于研究癌症和其他疾病。
T35362	NSC622608	Others	Others
	NSC622608 是 V 域 Ig 抑制 T 细胞活化 (VISTA) 的小分子配体，VISTA 是影响 T 细胞攻击肿瘤能力的免疫检查点。
T31932	GJ071 oxalate GJ 071,GJ-071,GJ071	Others	Others
	GJ071 oxalate 是一种无义抑制剂。无义抑制剂（NonSups）诱导“读出”，即在提前终止密码子处选择近同源tRNA，并将相应的氨基酸插入新生多肽中。
T20533	NNK Nicotine-derived nitrosamine ketone	Lipoxygenase	Metabolism
	NNK (Nicotine-derived nitrosamine ketone) 是尼古丁亚硝化衍生物。它可以激活 ERK1/2和 PKCα，并在 Ser70 激活 Bcl2磷酸化，以及在 Thr58和 Ser62激活 c-Myc。它可用于构建肺癌小鼠模型，以及诱导人肺癌细胞的增殖和存活。
T10352	APTO-253 LOR-253,LT-253	Apoptosis; c-Myc; KLF	Apoptosis; Cell Cycle/Checkpoint; MAPK
	APTO-253 (LOR-253) 抑制 c-Myc 表达，稳定 G-四链体 DNA，并诱导急性髓细胞白血病细胞的细胞周期停滞和凋亡。它通过诱导 KLF4 肿瘤抑制因子介导抗癌活性，具有抗关节炎活性。
TP1345	Kisspeptin-10, human (TFA)(374675-21-5,FREE)	GPR; Kisspeptin	Endocrinology/Hormones; GPCR/G Protein
	Kisspeptin-10, human (TFA)(374675-21-5,FREE) 是一种有效的血管收缩剂和血管生成抑制剂。 Kisspeptin-10，人类 TFA 通过其受体 GPR54 充当肿瘤转移抑制因子。 Kisspeptin-10-GPR54系统在胚胎肾发育中发挥重要作用。 Kisspeptin-10/GPR54 信号通过 NFATc4 介导的 BMP2 表达诱导成骨细胞分化
T11631	iFSP1	Ferroptosis	Apoptosis
	iFSP1 是一种强效、选择性和谷胱甘肽独立的铁死亡抑制蛋白 1 (FSP1) (AIFM2) 抑制剂，具有EC50 为 103 nM。它能够使多种人类癌细胞系对铁死亡诱导剂敏感，例如 (1S,3R)-RSL3。它在过表达 FSP1 的 GPX4 敲除细胞中选择性地诱导铁死亡。
T83658	SQLE-IN-1	Antifungal	Microbiology/Virology
	SQLE-IN-1 是一种角鲨烯环氧化酶 (SQLE) 抑制剂，具有抗肿瘤活性，可抑制肝癌细胞系 Huh7 的增殖和迁移能力，抑制细胞胆固醇的生成，增加抑癌基因PTEN的表达，抑制PI3K和AKT的蛋白表达。
T9636	Dalpiciclib SHR-6390	CDK	Cell Cycle/Checkpoint
	Dalpiciclib (SHR-6390) 是一种高选择性、口服生物利用度和相当效力的 CDK4 和 CKD6 抑制剂，IC50 分别为 12.4 nM 和 9.9 nM。它通过抑制磷酸化 Rb 蛋白和诱导 G1 细胞周期阻滞在食管鳞状细胞癌中发挥有效的抗肿瘤活性。
T64529	MDL-800 MDL 800,MDL800	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	SIRT6, responsible for deacetylation of histone H3 Nε-acetyl-lysines 9 (H3K9ac) and 56 (H3K56ac), is a tumor suppressor which has frequently been found to have low expression in various cancers. MDL-800 is a selective SIRT6 activator. It increased the deacetylase activity of SIRT6 by up to 22-fold and led to a global decrease in H3K9ac and H3K56ac levels in human hepatocellular carcinoma (HCC) cells. Also, it inhibited the proliferation of HCC cells via SIRT6-driven cell-cycle arrest and was eff...
T3661	Citarinostat ACY241,HDAC-IN-2	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	Citarinostat (ACY241) 是一种强效、选择性和口服组蛋白脱乙酰酶 (HDAC) 抑制剂，具有抗肿瘤活性，对 HDAC1、HDAC2、HDAC3、HDAC6 和 HDAC8 的 IC50分别为 35、45、46、2.6 和 137 nM。
T60013	GA-017	Others	Others
	GA-017是一种有效的选择性 LATS1和 LATS2(大型肿瘤抑制激酶 1/2) 抑制剂，其 IC50值分别为 4.10 和 3.92 nM。GA-017 是细胞增殖的激活剂。GA-017 促进 YAP/TAZ 激活和核转位。GA-017 在 3D 培养条件下促进细胞生长。GA-017 增强小鼠肠道类器官的离体形成。
T60202	MMRi62 7-[(2,3-dichlorophenyl)-(pyridin-2-ylamino)methyl]quinolin-8-ol	Ferroptosis	Apoptosis
	MMRi62 (7-[(2,3-dichlorophenyl)-(pyridin-2-ylamino)methyl]quinolin-8-ol) 是一种铁死亡 (ferroptosis) 诱导剂，靶向 MDM2-MDM4 (抑癌基因 p53 负调控因子)。MMRi62 对胰腺导管腺癌 (PDAC) 细胞显示出 p53 独立的促凋亡 (apoptosis) 活性，并诱导其自噬 (autophagy)。MMRi62 诱导铁死亡，伴随着活性氧增加和铁蛋白重链 (FTH1) 溶酶体降解。MMRi62 还可导致突变型 p53 的蛋白酶体降解，并对具有 KRAS 和 TP53 高频突变特征的原位异种移植 PDAC 小鼠模型具有体内药效。
T21967	MEG hemisulfate Mercaptoethylguanidine hemisulfate	NOS	Immunology/Inflammation
	MEG hemisulfate (Mercaptoethylguanidine hemisulfate) 是一种有效和选择性的诱导型 NO 合酶 (iNOS) 的抑制剂，在组织匀浆中抑制 iNOS，ecNOS 和 bNOS 的 EC50 值分别为 11.5，110 和 60 μM。MEG hemisulfate 也有效的过氧亚硝酸盐清除剂，可抑制过氧亚硝酸盐诱导的氧化过程。MEG hemisulfate 在许多炎症实验模型中具有保护作用，包括缺血/再灌注损伤，牙周炎，失血性休克，炎性肠病以及内毒素和败血性休克。
T29871	Allantoin biotin
	Allantoin biotin is a protein aggregate suppressor.
T29872	Allantoin galacturonic acid Allantoin monogalactopyranuronate
	Allantoin galacturonic acid is a protein aggregate suppressor.
T29870	Allantoin ascorbate
	Allantoin ascorbate is a protein aggregate suppressor.
T12453	PHT-7.3	Others	Others
	PHT-7.3 is a selective connector enhancer of kinase suppressor of Ras 1 (Cnk1) pleckstrin homology (PH) domain inhibitor
T29874	Allantoin panthenol Alpantha
	Allantoin panthenol is a protein aggregate suppressor.
T29869	Allantoin acetyl methionine Allantoin N-acetyl-DL-methionine
	Allantoin acetyl methionine is a protein aggregation suppressor.
T29875	Allantoin calcium pantothenate
	Allantoin calcium pantothenate is a protein aggregate suppressor.
T29876	Allantoin polygalacturonic acid
	Allantoin polygalacturonic acid is a protein aggregate suppressor.
T29873	Allantoin glycyrrhetinic acid
	Allantoin glycyrrhetinic acid is a protein aggregate suppressor.
T34026	Phevamine A PHVA	Others	Others
	Phevamine A (PHVA) 是植物免疫反应的抑制剂。
T27329	(R)-FL118 FL-118,FL 118
	FL118 inhibits human survivinion expression and activates tumor suppressor p53 as a MOA in p53 wild-type cancer cells.
T34472	S1QEL S-1QEL,S1 QEL,S 1QEL,S1QEL1.1,S1-QEL
	S1QEL is a suppressor of mitochondrial respiratory complex I site IQ electron leak which suppresses superoxide and/or H2O2 production without altering oxidative phosphorylation.
TP2133	[Ala92]-p16 (84-103)
	Peptide derived from the tumor suppressor protein p16; inhibits cyclin-dependent kinase-4 (cdk4)/cyclin D1 (IC50 ~ 1.5 μM) and binds to cdk6.
T28355	Pentamidine dimesylate
	Pentamidine dimesylate is an inhibitor of calcium-dependent complex formation with p53 [(Ca)S100B-p53) in malignant melanoma (MM). Pentamidine dimesylate restores p53 tumor suppressor activity in vivo.
T28790	SKF1
	SKF1 is a suppressor of the ability of FK506. SKF1 inhibits cell growth in the presence of high levels of NaCl, induces cell death in low salt conditions, interacts directly with yeast mitochodria.
T26639	Ap44mSe
	Ap44mSe is a potent and selective antitumor agent. Ap44mSe effectively depletes cellular Fe, resulting in transferrin receptor-1 up-regulation, ferritin down-regulation, and increased expression of the potent metastasis suppressor, N-myc downstream regula
T81892	M351-110
	M351-110为T细胞活化V域免疫球蛋白抑制因子(TCR V域)激动剂，应用于癌症研究领域。
T41065	Atrial natriuretic factor (1-28) (human, porcine) Atrial natriuretic factor (1-28) (human, porcine),Atrial natriuretic peptide (1-28)
	Atrial natriuretic factor (1-28) from both human and porcine sources is a powerful suppressor of pro-opiomelanocortin (POMC) mRNA, while it only has a modest inhibition effect on βEP-LI release.
T31933	GJ072 GJ-072,GJ 072
	GJ-072 is a Nonsense suppressor. Nonsense suppressors (NonSups) induce “readthrough”, i.e., the selection of near cognate tRNAs at premature termination codons and insertion of the corresponding amino acid into nascent polypeptide.
T24466	Milademetan free base DS3032B,DS-3032,DS3032,DS 3032,DS 3032B,DS-3032B
	Milademetan (DS-3032b or DS-3032) is a potent and selective MDM2 inhibitor with potential antineoplastic activity. Milademetan (p.o.) binds to and prevents the binding of MDM2 protein to the transcriptional activation domain of the tumor suppressor protei
T11327	FR 167653 FR 167653 sulfate	p38 MAPK	MAPK
	FR 167653 (FR 167653 sulfate) is effective in treating inflammation, relieving trauma and ischemia-reperfusion injury in vivo. FR 167653 , an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity.
T11327L	FR 167653 free base	Others	Others
	FR 167653 free base is an orally active p38 MAPK inhibitor and is effective in treating inflammation, relieving trauma, and ischemia-reperfusion injury in vivo. It also is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MA
T26895	BRD0476 BRD-0476,ML 187,ML187,ML-187,BRD 0476
	BRD0476 is a suppressor of pancreatic β-cell apoptosis. BRD0476 inhibits interferon-gamma (IFN-γ)-induced Janus kinase 2 (JAK2) and signal transducer and activation of transcription 1 (STAT1) signaling to promote β-cell survival. BRD0476 inhibits JAK-STAT
T77852	INX-SM-56
	INX-SM-56是一种用于合成抗VISTA抗体活性分子偶联物的cytotoxin。VISTA代指含V区域免疫球蛋白的T细胞活化抑制因子。
T69880	YW2065
	YW2065 has excellent anti-colorectal cancer effects in vitro and in vivo. YW2065 achieves its inhibitory activity for Wnt signaling by stabilizing Axin-1, a scaffolding protein that regulates proteasome degradation of β-catenin. Simultaneously, YW2065 also led to the activation of the tumor suppressor AMPK, providing an additional anticancer mechanism. In addition, YW2065 showed favorable pharmacokinetic properties without obvious toxicity.
T14282	Amuvatinib hydrochloride HPK 56 hydrochloride,MP470 hydrochloride	Others	Others
	Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret and is also a DNA repair suppressor through suppression of DNA repai
TP1127	Nemifitide diTFA INN 00835 diTFA	5-HT Receptor	GPCR/G Protein; Neuroscience
	Nemifitide diTFA (INN 00835 diTFA) 是一种合成的五肽，是一种可透过血脑屏障的黑色素细胞抑制因子 (MIF) 的肽类似物，具有有效的抗抑郁活性。
T37797	Coumarin-Quinone Conjugate
	Coumarin-quinone conjugate is a fluorescent substrate for NADH:ubiquinone oxidoreductases.1It is comprised of a coumarin fluorophore conjugated to a ubiquinone analog that can be reduced by NADH:ubiquinone oxidoreductases. It has been used to measure the kinetic parameters of apoptosis-inducing factor mitochondria-associated 2/ferroptosis suppressor protein 1 (AIFM2/FSP1). 1.Doll, S., Freitas, F.P., Shah, R., et al.FSP1 is a glutathione-independent ferroptosis suppressorNature575(7784)693-698(20...
T11240	Ethacrynic acid D5	Others	Others
	Ethacrynic acid, a diuretic, functions as an inhibitor of L-type voltage-dependent and store-operated calcium channels, facilitating the relaxation of airway smooth muscle (ASM) cells. It exhibits anti-inflammatory effects, notably reducing retinoid-induced ear edema in mice, and inhibits glutathione S-transferases (GSTs), making it a potent suppressor of the NF-kB signaling pathway. Additionally, ethacrynic acid modulates leukotriene formation. A variant, Ethacrynic acid D5, is distinguished by...
T72343	KRAS G12C inhibitor 40
	KRAS G12C inhibitor 40 是一种有效的KRAS G12C 抑制剂。Ras 蛋白家族是一种重要的细胞内信号分子，在生长发育中起重要作用。KRAS G12C inhibitor 40 具有研究 KRAS G12C 介导的癌症的潜力。
T82260	Grisnilimab WT1
	Grisnilimab (WT1)为IgG2a亚型的单克隆抗体（抗CD7），与Wilms' tumor发病相关的肿瘤抑制因子。该抗体能够调控多个靶基因的转录活性，并可能涉及RNA的转录后修饰过程。

化合物

p53 tumor suppressor fragment

Cat.No: TP2281

Target: Others

Cat.No: T8497

Target: CXCR

Cat.No: T16269

Target: DNA Methyltransferase, Dehydrogenase, Parasite

Cat.No: T6696

Synonym: 他扎罗汀,Tazorac,AGN 190168,Zorac

Target: Retinoid Receptor, Autophagy

Kevetrin hydrochloride

Cat.No: T3184

Synonym: Thioureidobutyronitrile HCl,thioureido butyronitrile hydrochloride,4-Isothioureidobutyronitrile hydrochloride

Target: Mdm2, p53

Cat.No: T8967

Target: DNA Methyltransferase

Cat.No: T35362

Target: Others

Cat.No: T31932

Synonym: GJ 071,GJ-071,GJ071

Target: Others

Cat.No: T20533

Synonym: Nicotine-derived nitrosamine ketone

Target: Lipoxygenase

Cat.No: T10352

Synonym: LOR-253,LT-253

Target: Apoptosis, c-Myc, KLF

Kisspeptin-10, human (TFA)(374675-21-5,FREE)

Cat.No: TP1345

Target: GPR, Kisspeptin

Cat.No: T11631

Target: Ferroptosis

Cat.No: T83658

Target: Antifungal

Cat.No: T9636

Synonym: SHR-6390

Target: CDK

Cat.No: T64529

Synonym: MDL 800,MDL800

Target: Sirtuin

Cat.No: T3661

Synonym: ACY241,HDAC-IN-2

Target: HDAC

Cat.No: T60013

Target: Others

Cat.No: T60202

Synonym: 7-[(2,3-dichlorophenyl)-(pyridin-2-ylamino)methyl]quinolin-8-ol

Target: Ferroptosis

MEG hemisulfate

Cat.No: T21967

Synonym: Mercaptoethylguanidine hemisulfate

Target: NOS

Allantoin biotin

Cat.No: T29871

Allantoin galacturonic acid

Cat.No: T29872

Synonym: Allantoin monogalactopyranuronate

Allantoin ascorbate

Cat.No: T29870

Cat.No: T12453

Target: Others

Allantoin panthenol

Cat.No: T29874

Synonym: Alpantha

Allantoin acetyl methionine

Cat.No: T29869

Synonym: Allantoin N-acetyl-DL-methionine

Allantoin calcium pantothenate

Cat.No: T29875

Allantoin polygalacturonic acid

Cat.No: T29876

Allantoin glycyrrhetinic acid

Cat.No: T29873

Cat.No: T34026

Synonym: PHVA

Target: Others

Cat.No: T27329

Synonym: FL-118,FL 118

Cat.No: T34472

Synonym: S-1QEL,S1 QEL,S 1QEL,S1QEL1.1,S1-QEL

[Ala92]-p16 (84-103)

Cat.No: TP2133

Pentamidine dimesylate

Cat.No: T28355

Cat.No: T28790

Cat.No: T26639

Cat.No: T81892

Atrial natriuretic factor (1-28) (human, porcine)

Cat.No: T41065

Synonym: Atrial natriuretic factor (1-28) (human, porcine),Atrial natriuretic peptide (1-28)

Cat.No: T31933

Synonym: GJ-072,GJ 072

Milademetan free base

Cat.No: T24466

Synonym: DS3032B,DS-3032,DS3032,DS 3032,DS 3032B,DS-3032B

Cat.No: T11327

Synonym: FR 167653 sulfate

Target: p38 MAPK

FR 167653 free base

Cat.No: T11327L

Target: Others

Cat.No: T26895

Synonym: BRD-0476,ML 187,ML187,ML-187,BRD 0476

Cat.No: T77852

Cat.No: T69880

Amuvatinib hydrochloride

Cat.No: T14282

Synonym: HPK 56 hydrochloride,MP470 hydrochloride

Target: Others

Nemifitide diTFA

Cat.No: TP1127

Synonym: INN 00835 diTFA

Target: 5-HT Receptor

Coumarin-Quinone Conjugate

Cat.No: T37797

Ethacrynic acid D5

Cat.No: T11240

Target: Others

KRAS G12C inhibitor 40

Cat.No: T72343

Cat.No: T82260

Synonym: WT1

Cat. No.	Product Name	Target	Signaling Pathways
TN1722	Hamamelitannin	Antifection	Microbiology/Virology
	Hamamelitannin 是分离自 Hamamelis virginiana 树皮的一种多酚，是群体感应抑制剂。它通过影响肽聚糖生物合成和 eDNA 释放增加金黄色葡萄球菌生物膜的抗生素敏感性。
T4902	Isotrifoliin Isoquercetin,Isoquercitroside,槲皮素-3-氧葡萄糖甙	Reactive Oxygen Species	Immunology/Inflammation; Metabolism; NF-κB
	Isotrifoliin (Isoquercitroside) 是一种抗氧化剂，也是一种嗜酸性炎症抑制剂。
T4717	25-Hydroxycholesterol 25-羟基胆固醇,25-羟基胆甾醇	Others; Endogenous Metabolite; HMG-CoA Reductase	Metabolism; Others
	25-Hydroxycholesterol 是胆固醇的代谢产物，由巨噬细胞响应 Toll 样受体激活而分泌。它有效抑制 B 细胞产生 IgA，EC50约为 65 nM。
T24744	Rubone
	Rubone is the tumor suppressor miRNA-34a modulator that acts by inhibiting the growth of hepatocellular carcinoma.
TN2697	2,3-Dihydrohinokiflavone	MMP; Parasite; Antifection	Microbiology/Virology; Proteases/Proteasome
	2,3-Dihydrohinokiflavone 是基质金属蛋白酶 (MMP) 基因表达的抑制剂，对利什曼原虫具有很强的活性，IC50 为 1.6 μM。
T72152	Eicosapentaenoic Acid sodium 二十碳五烯酸钠盐,Timnodonic acid sodium,EPA sodium
	Eicosapentaenoic Acid (EPA) sodium 为口服活性 ω-3 长链多不饱和脂肪酸 (ω-3 LC-PUFAs)。其通过DNA去甲基化，促进肿瘤抑制基因CCAAT/增强子结合蛋白δ (C/EBPδ)的重新表达，并通过H-RAS内含子1 CpG岛的去甲基化，激活U937白血病细胞中RAS/ERK/C/EBPβ途径。此外，该化合物能够促进血管平滑肌细胞松弛和血管舒张。

天然产物

Cat.No: TN1722

Target: Antifection

Cat.No: T4902

Synonym: Isoquercetin,Isoquercitroside,槲皮素-3-氧葡萄糖甙

Target: Reactive Oxygen Species

25-Hydroxycholesterol

Cat.No: T4717

Synonym: 25-羟基胆固醇,25-羟基胆甾醇

Target: Others, Endogenous Metabolite, HMG-CoA Reductase

Cat.No: T24744

2,3-Dihydrohinokiflavone

Cat.No: TN2697

Target: MMP, Parasite, Antifection

Eicosapentaenoic Acid sodium

Cat.No: T72152

Synonym: 二十碳五烯酸钠盐,Timnodonic acid sodium,EPA sodium

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