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Search Results for " p53-dependent "

39

抑制剂 & 化合物

7

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T36964	BML-259 CAY10554	CDK	Cell Cycle/Checkpoint
	BML-259 是 CDK5 和 CDK2 的抑制剂，IC50 分别为 64 和 98 nM。 BML-259 可用于癌症和神经退行性疾病治疗的研究。
T2707	Pifithrin-α hydrobromide Pifithrin hydrobromide,Pifithrin-α (PFTα) HBr,Pifithrin-α,PFTα,PFTα hydrobromide	Ferroptosis; Aryl Hydrocarbon Receptor; p53	Apoptosis; Immunology/Inflammation
	Pifithrin-α hydrobromide (Pifithrin-α hydrobromide) 是一种 p53 抑制剂，可抑制 p53 反应基因的 p53 依赖性反式激活。它也是芳烃受体的激动剂。
T27093	CT-1 CT 1	p53	Apoptosis
	CT-1 是一种 DNA 小沟配体，可导致 p53 依赖性乳腺癌细胞凋亡。
T28663	Sarmustine NSC-364432,SarCNU,Sarcosinamide,NSC 364432,NSC364432
	Sarmustine (SarCNU) 是一种具有抗癌活性的烷化剂，通过 p53 依赖性和 p53 非依赖性途径抑制前列腺癌细胞的生长。Sarmustine 在体外介导 P140K 甲基鸟嘌呤-DNA-甲基转移酶转导的人 CD34(+)细胞的选择。
T9122	XL177A	DUB	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Ubiquitination
	XL177A 是一种选择性不可逆的 USP7 抑制剂，IC50为 0.34 nM。它通过 p53 依赖性机制引发癌杀伤细胞作用。
T1887	Inauhzin INZ	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	Inauhzin (INZ) 是一种新型小分子，通过抑制 SIRT1 活性有效地重新激活 p53，促进人 Y 细胞的 p53 依赖性凋亡，在 A549 细胞中的IC50为3 uM。
T27029	cjoc42 cjoc 42,cjoc-42
	Cjoc42 是gankyrin 的抑制剂，以剂量依赖性方式抑制 gankyrin 活性。它可防止 p53 蛋白水平的降低。它恢复 p53 依赖性转录和对 DNA 损伤的敏感性。
T14303	Alrizomadlin APG-115,AA-115	Mdm2	Apoptosis
	Alrizomadlin (APG-115) 是一种具有口服活性的 MDM2 抑制剂，IC50 为 3.8 nM，Ki 分别为 1 nM[1]。 Alrizomadlin 阻断 MDM2 和 p53 的相互作用，并以 p53 依赖性方式诱导细胞周期停滞和细胞凋亡。
TQ0133	Amifostine thiol dihydrochloride WR 1065,硫代乙基氨基乙基胺盐酸盐	p53	Apoptosis
	Amifostine thiol dihydrochloride (WR 1065) 可通过 JNK 依赖性信号通路激活 p53。它还可以保护正常组织免受某些抗癌药物的毒性作用。
T21527	HBX 41108 HBX-41108,7-氯-9-氧代-9H-茚并[1,2-B]吡嗪-2,3-二甲腈	DUB; p53	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Ubiquitination
	HBX 41108 (HBX-41108) 是一种泛素特异性蛋白酶 7 的非竞争性抑制剂，IC50为 424 nM。它诱导 p53 依赖的凋亡，抑制 USP7 介导的 p53 去泛素化以稳定 p53 并抑制癌细胞生长。
T3637	Pifithrin-β hydrobromide Cyclic PFT-α,PFT-β,Cyclic Pifithrin-α hydrobromide,Pifithrin-β,PFT β (hydrobromide)	Ferroptosis; p53	Apoptosis
	Pifithrin-β hydrobromide (Cyclic PFT-α) 是一种 p53 的抑制剂，可逆地阻断 p53 依赖性转录激活和细胞凋亡。IC50值为23 μM。
T41068	P53R3	p53	Apoptosis
	P53R3是一种有效的 p53再激活剂。P53R3可恢复 p53热点突变体的序列特异性 DNA 结合，包括p53 R175H、p53 R248W 和p53 R273H。P53R3特异性诱导p53依赖性抗增殖作用，其特异性比PRIMA-1高得多的。P53R3增强野生型p53和p53 M237I 向靶基因启动子的募集。P53R3强烈增强死亡受体死亡受体5（DR5）的mRNA、总蛋白和细胞表面的水平。P53R3用于癌症研究。
T3465	Vesnarinone 维司力农,OPC-8212,Arkin,Piteranometozine	HIV Protease; PDE	Metabolism; Microbiology/Virology; Proteases/Proteasome
	Vesnarinone (Arkin) 是一种喹啉酮衍生物，可抑制磷酸二酯酶III 活性，增加钙通量和减小钾通量。
T26585	AK301 AK-301,AK 301	Apoptosis; Microtubule Associated	Apoptosis; Cytoskeletal Signaling
	AK301 是一种强效的管蛋白聚合选择性抑制剂，也是癌细胞对凋亡配体的有效增敏剂（EC50 < 200 nM）。AK301 可阻止有丝分裂的结肠癌细胞在停用化合物并解除阻止后很容易发生 p53 依赖性凋亡。
T21617	MG-115 Z-LL-Nva-CHO	Proteasome	Proteases/Proteasome; Ubiquitination
	MG-115 (Z-LL-Nva-CHO) 是一种有效且可逆的蛋白酶体抑制剂，对20S 和26S 蛋白酶体的 Ki 值分别为 21 nM 和 35 nM。MG-115 特异性抑制蛋白酶体的胰凝乳蛋白酶样活性，诱导 p53 依赖性细胞凋亡。
T4019	Cambinol SIRT1/2 Inhibitor IV,NSC 112546	Apoptosis; Phospholipase; Sirtuin	Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Metabolism
	Cambinol (SIRT1/2 Inhibitor IV) 是一种SIRT1和SIRT2的抑制剂，IC50值分别为 56 μM 和 59 μM。它是中性鞘磷脂酶的外泌体抑制剂。
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.
T69042	NSC-279287
	NSC-279287 is a novel Inhibitor of the p53-mdm2 Interaction, Activating p53-Dependent Transcription in mdm2-Overexpressing Cells.
T38616	Teprasiran QPI-1002
	Teprasiran (QPI-1002) is an RNA-based compound that transiently suppresses p53-dependent apoptosis, a process involved in the development of acute kidney injury (AKI).
T37538	Amifostine thiol
	Amifostine thiol (WR-1065), the active metabolite of cytoprotector Amifostine, serves as a cytoprotective agent possessing radioprotective properties. It activates p53 via a JNK-dependent signaling pathway[1][2][3].
T63297	ABL-L
	ABL-L 能够利用 p53 依赖的途径，诱导人喉癌细胞凋亡。
T73413	Cadein1
	Cadein1 是一种异喹啉衍生物，在p53功能缺失的癌细胞中，可导致 G2/M 延迟和caspase 依赖的凋亡。
T73000	SIRT2-IN-11
	SIRT2-IN-11 (AEM1) 是选择性的SIRT2抑制剂，IC50值为 18.5 μM。SIRT2-IN-11 以 p53 依赖的诱导细胞凋亡，激活CDKN1A，PUMA 和NOXA 的表达，并且促进 p53 的乙酰化。SIRT2-IN-11 可用于 p53 相关的癌症研究。
T78166	MEL24	Others	Others
	MEL24为Mdm2 E3连接酶抑制剂，通过p53依赖机制降低细胞存活率，增强对DNA损伤剂的敏感性，适用于体外抗肿瘤研究。
TP2299	tumor protein p53 binding protein fragment [Homo sapiens]/[Mus musculus]	Others	Others
	Tumor protein p53 binding protein (53BP1) has been identified in a yeast two-hybrid screen as a protein that interacts with the central DNA–binding domain of p532. Similar to breast cancer susceptibility gene 13, 4 (BRCA1; 53BP1 enhances p53-dependent tra
T41151	K34c
	K34c is a potent and selective α5β1 integrin inhibitor (IC50 = 3.1 nM). K34c inhibits cell survival and migration, inhibits p53-dependent senescence induced by Temozolomide or Ellipticine and promotes apoptosis in U87MG cells. K34c also prevents TGFβ-induced infiltrationin vivoand reduces cell adhesion on fibronectin.
T76288	GPR
	GPR为一种含有三氨基酸的肽类化合物，能够通过抑制caspase-3/p53依赖的细胞凋亡机制，保护培养的大鼠海马神经元不受Aβ诱发的神经元死亡影响，应用于阿尔茨海默病（AD）的研究中。
T69690	XL-188
	XL-188 is a highly potent and selective inhibitor of USP7. XL188 inhibited USP7 catalytic domain and full-length enzyme with IC50 values of 193 and 90 nM, respectively. XL188 Promotes USP7-Dependent Loss of HDM2 and Increase of p53 and p21. XL188 represents one of only a small set of mammalian DUB inhibitors with low nanomolar potency and a high degree of selectivity relative to other DUBs
T13862L	Recilisib sodium Brand name: Ex-RAD,ON 01210.Na,ON01210,ON-01210
	Recilisib, also known as ON 01210.Na, is a radioprotectant, which modifys cell cycle distribution patterns in cancer cells subjected to radiation therapy, and it has been identified as a potential candidate for radiation protection studies. It appears tha
T63074	Ivaltinostat formic
	Ivaltinostat (CG-200745) formic 是一种口服具有活力的泛 HDAC 抑制剂，具有异羟肟酸部分，能够在催化袋底部结合锌。Ivaltinostat formic 对组蛋白 H3 和微管蛋白的脱乙酰作用具有抑制效果。Ivaltinostat formic 能够促使 p53 的积累，诱导 p53 依赖性反式激活，并提高 MDM2 和 p21 (Waf1/Cip1) 蛋白的表达。Ivaltinostat formic 增加 Gemcitabine 耐药细胞对 Gemcitabine 和 5-Fluorouracil (5-FU) 的敏感性。Ivaltinostat formic 诱导凋亡，并具有抗肿瘤效果。
T70430	XK469
	XK489 is a synthetic quinoxaline phenoxypropionic acid derivative with proapoptotic and antiproliferative activities. R(+)XK469 selectively inhibits topoisomerase II-beta, blocks activation of MEK/MAPK signaling kinases, stimulates caspases, and upregulates p53-dependent proteins, including cyclins A and B1, thereby arresting cancer cells in the G2/M phase of the cell cycle. Both R(+) and S(-) isomers of this agent are cytotoxic, although the R-isomer is more potent.
T79665	RUNX-IN-2	Apoptosis	Apoptosis
	RUNX-IN-2 (Compound Conjugate 3) 具有高度特异性，能与RUNX结合序列共价结合并阻断RUNX蛋白与其靶位点的互动。该化合物能诱导p53依赖性细胞凋亡(apoptosis)，抑制细胞增殖，并在PANC-1异种移植小鼠模型中抑制肿瘤生长，显示出高效的烷基化活性。
T62970	CDK1-IN-1
	CDK1-IN-7 是一种 CDK1 的有效抑制剂，对 CDK1/CycB 的 IC50 值为 161.2 nM。CDK1-IN-7 通过凋亡内在途径以 p53 依赖的方式诱导细胞凋亡。CDK1-IN-7 能够选择性作用于肿瘤组织，并具有潜在的抗增殖作用。CDK1-IN-7 是一种潜在的靶向抗肿瘤药物。
T79664	RUNX-IN-1	Apoptosis	Apoptosis
	RUNX-IN-1 Compound Conjugate 1) 具有与RUNX结合序列共价结合的特性，能有效抑制RUNX蛋白与其靶位点的相互作用。该化合物能激活p53依赖的细胞凋亡(apoptosis)过程，并能够抑制细胞增殖。此外，RUNX-IN-1在PANC-1异种移植小鼠模型中显示出对肿瘤生长的抑制作用。
T35696	Olomoucine II
	Olomoucine II is an inhibitor of cyclin-dependent kinases (CDKs; IC50s = 7.6, 0.1, 19.8, 0.45, and 0.06 μM for Cdk1, -2, -4, -7, and -9, respectively).1It is selective for CDKs over 10 additional kinases (IC50s = >100 μM for all) but does inhibit ERK2 (IC50= 32 μM) and the ATP-binding cassette transporter B1 (ABCB1; IC50= 6.4 μM).1,2Olomoucine II inhibits proliferation of a variety of cancer cells, including those expressing wild-type p53 or mutant p53 (mean IC50s = 7.4 and 10.1 μM, respectively...
T36114	Coenzyme Q2
	Coenzyme Q10 is a component of the electron transport chain and participates in aerobic cellular respiration, generating energy in the form of ATP. In its reduced form, it acts as an antioxidant. Coenzyme Q2 is a precursor of coenzyme Q10 that has 2, rather than 10, isoprenoid units on the ubiquinone base. It can act as an electron acceptor for bacterial Complex I. In mammalian cells, exogenous coenzyme Q2 prevents the production of reactive oxygen species associated with Complex I activity. For...
T36108	YW3-56 (hydrochloride) (technical grade) YW3-56 (hydrochloride) (technical grade)
	YW3-56 is an inhibitor of protein arginine deiminase 2 (PAD2) and PAD4 (IC50s = 0.5-1 and 1-5 μM, respectively).1It inhibits the growth of U2OS osteosarcoma cells (IC50= ~2.5 μM) in a p53-dependent mannerviainduction of SESN2 and subsequent inhibition of mTORC1. YW3-56 (10 mg/kg) reduces tumor growth in an S-180 murine sarcoma tumor model. It also inhibits tumor growth in the 1883 MDA-MB-231 breast cancer bone metastasis mouse xenograft model.2 1.Wang, Y., Li, P., Wang, S., et al.Anticancer pept...
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...
T35874	CC260
	CC260 is a selective PI5P4Kα and PI5P4Kβ inhibitor with Kis of 40 nM and 30 nM, respectively. CC260 does not inhibit or weakly inhibits other protein kinases, such as Plk1 and RSK2. CC260 can be used for cell energy metabolism, diabetes and cancer research[1]. In cultured C2C12 myotubes, CC260 (20 μM) enhances Insulin-induced Akt phosphorylation at both Thr-308 and Ser-473 but suppresses S6K phosphorylation (Thr-389) by mTORC1[1]. CC260 (2.5 μM, 5 μM, 10 μM, 20 μM) significantly increases phosph...

化合物

Cat.No: T36964

Synonym: CAY10554

Target: CDK

Pifithrin-α hydrobromide

Cat.No: T2707

Synonym: Pifithrin hydrobromide,Pifithrin-α (PFTα) HBr,Pifithrin-α,PFTα,PFTα hydrobromide

Target: Ferroptosis, Aryl Hydrocarbon Receptor, p53

Cat.No: T27093

Synonym: CT 1

Target: p53

Cat.No: T28663

Synonym: NSC-364432,SarCNU,Sarcosinamide,NSC 364432,NSC364432

Cat.No: T9122

Target: DUB

Cat.No: T1887

Synonym: INZ

Target: Sirtuin

Cat.No: T27029

Synonym: cjoc 42,cjoc-42

Cat.No: T14303

Synonym: APG-115,AA-115

Target: Mdm2

Amifostine thiol dihydrochloride

Cat.No: TQ0133

Synonym: WR 1065,硫代乙基氨基乙基胺盐酸盐

Target: p53

Cat.No: T21527

Synonym: HBX-41108,7-氯-9-氧代-9H-茚并[1,2-B]吡嗪-2,3-二甲腈

Target: DUB, p53

Pifithrin-β hydrobromide

Cat.No: T3637

Synonym: Cyclic PFT-α,PFT-β,Cyclic Pifithrin-α hydrobromide,Pifithrin-β,PFT β (hydrobromide)

Target: Ferroptosis, p53

Cat.No: T41068

Target: p53

Cat.No: T3465

Synonym: 维司力农,OPC-8212,Arkin,Piteranometozine

Target: HIV Protease, PDE

Cat.No: T26585

Synonym: AK-301,AK 301

Target: Apoptosis, Microtubule Associated

Cat.No: T21617

Synonym: Z-LL-Nva-CHO

Target: Proteasome

Cat.No: T4019

Synonym: SIRT1/2 Inhibitor IV,NSC 112546

Target: Apoptosis, Phospholipase, Sirtuin

Pentamidine dimesylate

Cat.No: T28355

Cat.No: T69042

Cat.No: T38616

Synonym: QPI-1002

Amifostine thiol

Cat.No: T37538

Cat.No: T63297

Cat.No: T73413

Cat.No: T73000

Cat.No: T78166

Target: Others

tumor protein p53 binding protein fragment [Homo sapiens]/[Mus musculus]

Cat.No: TP2299

Target: Others

Cat.No: T41151

Cat.No: T76288

Cat.No: T69690

Recilisib sodium

Cat.No: T13862L

Synonym: Brand name: Ex-RAD,ON 01210.Na,ON01210,ON-01210

Ivaltinostat formic

Cat.No: T63074

Cat.No: T70430

Cat.No: T79665

Target: Apoptosis

Cat.No: T62970

Cat.No: T79664

Target: Apoptosis

Cat.No: T35696

Cat.No: T36114

YW3-56 (hydrochloride) (technical grade)

Cat.No: T36108

Synonym: YW3-56 (hydrochloride) (technical grade)

Cat.No: T35812

Synonym: CAY10591

Cat.No: T35874

Cat. No.	Product Name	Target	Signaling Pathways
T8678	Naphthazarin 萘茜,5,8-Dihydroxy-1,4-naphthoquinone,DHNQ	Apoptosis	Apoptosis
	Naphthazarin (5,8-Dihydroxy-1,4-naphthoquinone) 是来自毛紫草的一种天然产物，通过氧化应激、线粒体凋亡诱导因子的激活、微管的解聚、干扰溶酶体功能和 p53 依赖性 p21 激活，可触发细胞凋亡并具有抗肿瘤作用。
T5S0168	Atractylenolide II 2-Atractylenolide,Asterolide,苍术内酯II	Apoptosis; ERK; p38 MAPK; Akt; STAT	Apoptosis; Cytoskeletal Signaling; JAK/STAT signaling; MAPK; PI3K/Akt/mTOR signaling; Stem Cells
	Atractylenolide II (2-Atractylenolide) 是一种从白术干燥根茎分离的倍半萜类天然产物，具有抗增殖活性。
T5S0331	Isoliquiritin 异甘草苷,Neoisoliquritin	p53; Antifungal	Apoptosis; Microbiology/Virology
	Isoliquiritin (Neoisoliquritin) 是从甘草根中分离得到的，具有镇咳、抗抑郁作用和抗真菌活性。它还能抑制血管生成和导管形成。
T6S1780	Protosappanin B 原苏木素B,Q-100961,FT-0689654	Apoptosis	Apoptosis
	Protosappanin B (Q-100961) 是从苏木中提取的一种多酚类天然产物，具有抗肿瘤作用。它通过激活 MDM2 依赖性泛素化过程诱导 p53 蛋白降解。它显著提高细胞活力，抑制细胞凋亡并上调生长相关蛋白 43 的表达。
TN1620	Eriocalyxin B 毛萼乙素	Apoptosis; cAMP; NF-κB; STAT	Apoptosis; GPCR/G Protein; JAK/STAT signaling; NF-κB; Stem Cells
	Eriocalyxin B 是从中草药枇杷素中分离得到的一种二萜类天然产物，可诱导细胞凋亡，具有抗癌和抗炎作用。
T7027	EURYCOMANONE 东革阿里提取物,Pasakbumin A	Others	Others
	Eurycomanone (Pasakbumin A) 能够抑制雌激素生成过程中磷酸二酯酶和芳香酶的活性，促进精子生成。它对 HepG2 细胞具有细胞毒性，能够上调 p53 和 Bax 以及下调 Bcl-2 ，诱导细胞凋亡。它具有抗癌活性，在浓度范围内以剂量依赖性方式抑制 A549 肺癌细胞增殖从 5 到 20 微克/毫升。
T6S1369	Vitexin 牡荆素,Apigenin-8-C-glucoside	Antioxidant	oxidation-reduction
	Vitexin 是一种存在于多种药用植物（如榕树、螺旋藻）中的 c-糖基化的黄酮。它具有广泛的药理作用，包括抗氧化，抗癌，抗炎，抗痛觉过敏和神经保护作用。

天然产物

Cat.No: T8678

Synonym: 萘茜,5,8-Dihydroxy-1,4-naphthoquinone,DHNQ

Target: Apoptosis

Atractylenolide II

Cat.No: T5S0168

Synonym: 2-Atractylenolide,Asterolide,苍术内酯II

Target: Apoptosis, ERK, p38 MAPK, Akt, STAT

Cat.No: T5S0331

Synonym: 异甘草苷,Neoisoliquritin

Target: p53, Antifungal

Protosappanin B

Cat.No: T6S1780

Synonym: 原苏木素B,Q-100961,FT-0689654

Target: Apoptosis

Cat.No: TN1620

Synonym: 毛萼乙素

Target: Apoptosis, cAMP, NF-κB, STAT

Cat.No: T7027

Synonym: 东革阿里提取物,Pasakbumin A

Target: Others

Cat.No: T6S1369

Synonym: 牡荆素,Apigenin-8-C-glucoside

Target: Antioxidant

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