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31

抑制剂 & 化合物

7

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
TQ0219	MK-8033	c-Met/HGFR	Tyrosine Kinase/Adaptors
	MK-8033 是一种新型ATP 竞争性c-Met/Ron 双重抑制剂，对野生型c-Met 的IC50=1 nM，对c-Met N1100Y 的IC50=2.0 nM。
T19723	AMTB hydrochloride AMTB	TRP/TRPV Channel	Membrane transporter/Ion channel
	AMTB hydrochloride (AMTB HCl) 是TRPM8通道的选择性阻滞剂。它抑制 icilin 诱导的 TRPM8 通道激活，pIC50为 6.23。它在膀胱过度活动和膀胱疼痛综合征中有研究的价值。它是电压门控钠通道的非选择性抑制剂 (NaV)。
T15017	CU-T12-9	TLR	Immunology/Inflammation
	CU-T12-9 是特异性 TLR1/2激动剂，可激活先天免疫系统和适应性免疫系统。它选择性激活 TLR1/2 异二聚体，可通过促进 TLR1 和 TLR2 二聚而激活 NF-κB 信号，引起下游 TNF-α、IL-10 和 iNOS 增加。
T6916	OICR-9429 OICR 9429	Histone Methyltransferase; JAK	Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells
	OICR-9429 是一个新颖的相互作用的小分子Wdr5-MLL 拮抗剂，IC50是 5 uM，在体外抑制急性髓性白血病细胞。
T0334	Rosiglitazone BRL49653,罗格列酮	Ferroptosis; TRP/TRPV Channel; PPAR; Autophagy	Apoptosis; Autophagy; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism
	Rosiglitazone (BRL49653) 是一种 PPARγ 激动剂、TRPC5 激活剂和 TRPM3 抑制剂，具有口服活性。Rosiglitazone 也是一种降糖剂，是噻唑烷二酮类胰岛素增敏剂。
T6646	Rosiglitazone hydrochloride 盐酸罗格列酮,BRL-49653 HCl,Rosiglitazone HCl	Ferroptosis; TRP/TRPV Channel; PPAR; Autophagy	Apoptosis; Autophagy; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism
	Rosiglitazone hydrochloride (BRL-49653 HCl) 是一种降血糖药物，通过与脂肪细胞中的 PPAR 受体结合来刺激胰岛素分泌。它对 PPARγ1、PPARγ2 和 PPARγ 的EC50值分别为 30 nM、100 nM 和 60 nM。它也是TRPC5的激活剂和TRPM3的抑制剂。
T15477	Hexaminolevulinate hydrochloride Hexyl 5-aminolevulinate hydrochloride,5-Aminolevulinic acid hexyl ester hydrochloride,P-1206,5-氨基酮戊酸己酯盐酸盐	Others	Others
	Hexaminolevulinate hydrochloride (P-1206) 是一种被批准的、可用于膀胱镜检测乳头状膀胱癌的荧光剂。
T23888	CID-5056270	ROCK	Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells
	CID-5056270具有抗癌活性，对肺癌肛门癌、膀胱癌、宫颈癌、外阴癌、阴茎癌、伯基特淋巴瘤乳腺癌和骨癌具有抑制作用，可用来研究高血压、老年痴呆症度、阿尔茨海默病和动脉硬化。
T24051	Exisulind Sulindac sulfone,CP248	Apoptosis; PKA	Apoptosis; Tyrosine Kinase/Adaptors
	Exisulind (CP248) 通过激活蛋白激酶 G (PKG) 诱导细胞凋亡。 Exisulind 在实体瘤和血液癌细胞系中表现出抗肿瘤活性，并且是结肠癌、前列腺癌、膀胱癌、乳腺癌和肺癌啮齿动物模型中肿瘤生长的抑制剂。
T15558	GSK319347A	IκB/IKK	NF-κB
	GSK319347A 是一种具有选择性和有效性的 TBK1 和 IKKε 的双重抑制剂，具有潜在的抗肿瘤活性，对 IKK2 活性有抑制作用，可用于研究膀胱癌和肺腺癌。
T36898	Sandacanol Sandranol,2-Ethyl-4-(2,2,3-trimethylcyclopent-3-en-yl)-but-2-en-1-ol	Apoptosis	Apoptosis
	Sandacanol（Sandranol）是一种选择性嗅觉受体（OR10H1）激动剂。Sandacanol可诱导膀胱癌细胞的细胞周期停止和部分凋亡，可降低细胞迁移率和增殖率。
T60039	KSQ-4279 USP1-IN-1	PARP; DUB	Cell Cycle/Checkpoint; Chromatin/Epigenetic; DNA Damage/DNA Repair; Ubiquitination
	KSQ-4279 (USP1-IN-1)是 USP1 和 PARP 的抑制剂。KSQ-4279 具有抗癌活性，可用于研究非小细胞肺癌、骨肉瘤、卵巢癌、乳腺癌、胶质母细胞瘤、膀胱癌、子宫癌和胰腺癌。
T15713	Larotaxel XRP9881	P-gp	Membrane transporter/Ion channel; Neuroscience
	Larotaxel (XRP9881) 是一种紫杉烷类似物，具有抗癌活性，通过促进微管蛋白装配和稳定微管发挥其细胞毒性作用，并通过细胞凋亡诱导细胞死亡。Larotaxel (XRP9881) 是一种可穿过血脑屏障的化合物，对 Docetaxel 的亲和力比 P-糖蛋白 1 高，可用于研究乳腺癌和膀胱癌。
T0976	Propoxur 残杀威,Aprocarb,Propoxure,Baygon	AChR; Antifungal	Microbiology/Virology; Neuroscience
	Propoxur (Propoxure) 是一种氨基甲酸酯类杀虫剂，用于控制蟑螂、苍蝇、蚊子以及草坪和草坪昆虫。
T25892	N-Trifluoroacetyladriamycin NSC-283464,NSC 283464,AD 41,AD-41,NSC283464
	N-Trifluoroacetyladriamycin is a metabolite of Valrubicin (N-trifluoroacetyladriamycin-14-valerate, trade name Valstar). Valrubicin is a chemotherapy drug utilized to treat bladder cancer. Valrubicin is the anthracycline doxorubicin analog and is administ
T70512	Isobetanin
	Isobetanin is a betacyanin that has been shown to enhance vitexin-2-O-xyloside mediated inhibition of proliferation of T24 bladder cancer cells.
T38970	Hematoporphyrin monomethyl ether
	Hematoporphyrin monomethyl ether (HMME), a second-generation porphyrin-related photosensitizer, is a highly selective and low-toxicity compound known for its singular form and high yield of singlet oxygen. It finds extensive application in diagnosing and treating various tumors, including lung cancer, bladder cancer, nevus flammeus, and brain glioma.
T74466	ASR-488
	ASR-488 可激活 mRNA 结合蛋白 CPEB1，诱导细胞凋亡 (apoptosis) 并抑制膀胱癌的生长。
T73826	PZ703b hydrochloride
	PZ703b hydrochloride 是一种Bcl-xlPROTAC 降解剂，可以诱导细胞凋亡 (apoptosis)，抑制癌细胞增殖。PZ703b hydrochloride 可用于膀胱癌的研究。
T16354	NSC745885	Others	Others
	NSC745885 is an effective down-regulator of EZH2 via proteasome-mediated degradation. NSC745885 is also an effective anti-tumor agent that displays selective toxicity against multiple cancer cell lines but not normal cells. NSC745885 offers possibilities
T77913	PZ703b TFA	PROTACs	PROTAC
	PZ703b TFA为一种Bcl-xl PROTAC降解剂，具备诱导细胞凋亡(apoptosis)及抑制癌细胞增殖功能，主要应用于膀胱癌研究领域。
T74521	Anticancer agent 52
	Anticancer agent 52 是一种有效的抗癌剂。Anticancer agent 52 显示出体外细胞毒性。Anticancer agent 52 诱导细胞凋亡 (apoptosis)。Anticancer agent 52 显示出抗肿瘤作用。Anticancer agent 52 具有研究膀胱癌的潜力。
T81574	PAA4
	PAA4为含中心甲基化物碳的多核Au(I)簇，具有抗增殖活性。PAA4能时间依赖性地提升pH2AX表达，并在原位膀胱癌小鼠模型中展现抗肿瘤效果。
T12068	MK-8033 hydrochloride	Others	Others
	MK-8033 hydrochloride 是一种有效的、具有口服活性的 ATP 竞争性 c-Met/Ron 双重抑制剂，对c-Met 的为1 nM ，对Ron 的IC50为7nM。MK-8033 hydrochloride 对活化的激酶构象 (activated kinase conformation)具有很高的亲和力，可用于乳腺癌，膀胱癌、非小细胞肺癌 (NSCLC)等癌症的研究。
T36882	CAY10773
	CAY10773 is a derivative of the ferroptosis inducer sorafenib .1It selectively inhibits proliferation of BEL-7402, MGC803, and T24 bladder cancer cells (IC50s = 5.77, 5.21 and 3.97 μM, respectively) over non-cancerous HCV-29 cells (IC50= 23.19 μM). CAY10773 induces apoptosis in T24 cells when used at concentrations ranging from 2 to 6 μM but induces ferroptosis at concentrations greater than or equal to 6 μM with 10 hour or longer incubation times. It increases the production of reactive oxygen ...
T70045	HUN47990
	HUN47990 is a bisphosphonate (BP) prodrug with antitumor activity. HUN47990 potently inhibits the in vitro growth of a variety of tumor cell lines, especially hematopoietic cell lines, at nanomolar concentrations. HUN47990 inhibited the prenylation of the RAP1A small GTPase signaling protein at concentrations as low as 1-10 nM. HUN47990 slowed the growth of human bladder cancer cells in an immunodeficient mouse model. HUN47990 is significantly more active than zoledronic acid, the most active FD...
T35616	Migrastatin
	Migrastatin is a bacterial metabolite that has been found inStreptomyceswith antimuscarinic and anticancer activities.1,2It binds to M1-5muscarinic acetylcholine receptors (Kis = >200, 200, 31, 43, and >200 μM, respectively) and inhibits calcium mobilization induced by carbamoylcholine in SK-N-SH cells (IC50= 28 μM), as well as in primary rat bladder smooth muscle cells.1Migrastatin inhibits the migration of EC17 esophageal cancer cells in a wound healing assay (IC50= 10 μg/ml) and 4T1 mouse mam...
T21693	PPM-18
	PPM-18 (NSC 73233) 是一种有效的抗炎剂，可抑制一氧化氮合酶的表达。PPM-18 是有效的 iNOS 表达抑制剂，可阻断 NF-κB 与启动子的结合。PPM-18 是维生素 K 的类似物，通过 ROS 和 AMPK 信号通路诱导膀胱癌细胞自噬和凋亡。
T63351	MS8511
	MS8511 是一种选择性的G9a/GLP 共价的不可逆抑制剂，可靶向底物结合位点的半胱氨酸残基，IC50值为 100 nM ( G9a) 和 140 nM (GLP)，Kd 值44 nM (G9a) 和 46 nM (GLP)。 MS8511 可降低细胞内 H3K9me2 水平并提高抗增殖活性。MS8511 可用于研究多种癌症 (包括脑癌、乳腺癌、卵巢癌、肺癌、膀胱癌、黑色素瘤、结肠直肠癌) 和其他疾病,如阿尔茨海默病 (AD)、镰状细胞病、Prader-Willi 综合征 (PWS).
T72780	HSP90/mTOR-IN-1
	HSP90/mTOR-IN-1 是一种有效的Hsp90和mTOR 抑制剂，IC50分别为 69 nM 和 29 nM。HSP90/mTOR-IN-1 通过过度激活PI3K/AKT/mTOR 通路抑制 SW780 细胞增殖。HSP90/mTOR-IN-1 通过对HSP90和mTOR 的选择性抑制来诱导细胞凋亡 (apoptosis) 和细胞自噬 (autophagy)。HSP90/mTOR-IN-1 在异种移植小鼠体内也表现出良好的抗肿瘤活性。HSP90/mTOR-IN-1 可用于膀胱癌的研究。
T36410	9(E),11(E),13(E)-Octadecatrienoic Acid
	9(E),11(E),13(E)-Octadecatrienoic acid (β-ESA) is a conjugated polyunsaturated fatty acid that is found in plant seed oils and in mixtures of conjugated linolenic acids synthesized by the alkaline isomerization of linolenic acid. It reduces growth of Caco-2 colon cancer cells in a dose-dependent and time-dependent manner. In vitro, β-ESA induces DNA fragmentation and upregulation of pro-apoptotic Bax mRNA. β-ESA decreases protein expression of the apoptosis suppression factor Bcl-2 and induces a...

化合物

Cat.No: TQ0219

Target: c-Met/HGFR

AMTB hydrochloride

Cat.No: T19723

Synonym: AMTB

Target: TRP/TRPV Channel

Cat.No: T15017

Target: TLR

Cat.No: T6916

Synonym: OICR 9429

Target: Histone Methyltransferase, JAK

Cat.No: T0334

Synonym: BRL49653,罗格列酮

Target: Ferroptosis, TRP/TRPV Channel, PPAR, Autophagy

Rosiglitazone hydrochloride

Cat.No: T6646

Synonym: 盐酸罗格列酮,BRL-49653 HCl,Rosiglitazone HCl

Target: Ferroptosis, TRP/TRPV Channel, PPAR, Autophagy

Hexaminolevulinate hydrochloride

Cat.No: T15477

Synonym: Hexyl 5-aminolevulinate hydrochloride,5-Aminolevulinic acid hexyl ester hydrochloride,P-1206,5-氨基酮戊酸己酯盐酸盐

Target: Others

Cat.No: T23888

Target: ROCK

Cat.No: T24051

Synonym: Sulindac sulfone,CP248

Target: Apoptosis, PKA

Cat.No: T15558

Target: IκB/IKK

Cat.No: T36898

Synonym: Sandranol,2-Ethyl-4-(2,2,3-trimethylcyclopent-3-en-yl)-but-2-en-1-ol

Target: Apoptosis

Cat.No: T60039

Synonym: USP1-IN-1

Target: PARP, DUB

Cat.No: T15713

Synonym: XRP9881

Target: P-gp

Cat.No: T0976

Synonym: 残杀威,Aprocarb,Propoxure,Baygon

Target: AChR, Antifungal

N-Trifluoroacetyladriamycin

Cat.No: T25892

Synonym: NSC-283464,NSC 283464,AD 41,AD-41,NSC283464

Cat.No: T70512

Hematoporphyrin monomethyl ether

Cat.No: T38970

Cat.No: T74466

PZ703b hydrochloride

Cat.No: T73826

Cat.No: T16354

Target: Others

Cat.No: T77913

Target: PROTACs

Anticancer agent 52

Cat.No: T74521

Cat.No: T81574

MK-8033 hydrochloride

Cat.No: T12068

Target: Others

Cat.No: T36882

Cat.No: T70045

Cat.No: T35616

Cat.No: T21693

Cat.No: T63351

HSP90/mTOR-IN-1

Cat.No: T72780

9(E),11(E),13(E)-Octadecatrienoic Acid

Cat.No: T36410

Cat. No.	Product Name	Target	Signaling Pathways
T3S0737	Flavokawain A 2'-羟基-4,4',6'-三甲氧基查耳酮,Flavokavain A	Apoptosis; p38 MAPK	Apoptosis; MAPK
	Flavokawain A (Flavokavain A) 是 kava 提取物中的查耳酮，是一种抗癌试剂，具有抗肿瘤活性。它通过 Bax 蛋白依赖和线粒体依赖的凋亡途径诱导细胞凋亡，有潜力用于膀胱癌的相关研究。
T4S0350	Licochalcone B 甘草查尔酮 B,甘草查尔酮B	Beta Amyloid; Others	Neuroscience; Others
	Licochalcone B 是从Glycyrrhiza inflate 根中提取的。它能够抑制淀粉样蛋白 β 自聚集作用 (IC50=2.16 μM) ，分解预先形成的 Aβ42原纤维，并通过螯合金属离子抑制金属诱导的 Aβ42聚集。
T5715	(E)-Flavokawain A (E)-1-(2-羟基-4,6-二甲氧基苯基)-3-(4-甲氧基苯基)-2-丙烯-1-酮,FLAVOKAVAIN A(P),卡瓦胡椒素A	Apoptosis; P450	Apoptosis; Metabolism
	(E)-Flavokawain A 是一种来自卡瓦提取物的新型查尔酮，通过参与 Bax 蛋白依赖性和线粒体依赖性凋亡途径诱导膀胱癌细胞凋亡，并抑制小鼠肿瘤生长，具有抗癌作用。
T7028	Licochalcone C LICOCHALCONEC,甘草查尔酮C	Phosphatase; Antioxidant; Glucosidase	Metabolism; oxidation-reduction
	Licochalcone C (LICOCHALCONEC) 能够抑制 α-葡萄糖苷酶，其对 α-葡萄糖苷酶的 IC50 <100 nM，对蛋白酪氨酸磷酸酶 1B 的 IC50=92.43 μM 。
TN4382	Kazinol A	AMPK; mTOR	Chromatin/Epigenetic; PI3K/Akt/mTOR signaling
	Kazinol A shows strong inhibition of arachidonic acid (AA)-induced platelet aggregation. It also exhibits potent inhibition with IC50 values ranging 0.6-164 M against XOD. Kazinol A may be a candidate for the development of effective anti-cancer drug on h
T4366	Quinovic acid	NF-κB; Caspase	Apoptosis; NF-κB; Proteases/Proteasome
	Quinovic acid shows some anti-tumour activities, quinovic acid glycosides have a potent inhibitory effect on the growth of human bladder cancer cell lines by inducing apoptosis through modulation of NF-ÎºB.
TN3404	Altholactone	BCL; p38 MAPK; ROS; Akt; Caspase; Antifection; p53	Apoptosis; Cytoskeletal Signaling; Immunology/Inflammation; MAPK; Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome
	Altholactone may be a potential antimicrobial agent, particularly in ciprofloxacin-refractory S. aureus and E. faecalis infections. It can inhibit the growth of various types of cancer cells through inducing apoptosis via oxidative stress, including bladd

天然产物

Cat.No: T3S0737

Synonym: 2'-羟基-4,4',6'-三甲氧基查耳酮,Flavokavain A

Target: Apoptosis, p38 MAPK

Cat.No: T4S0350

Synonym: 甘草查尔酮 B,甘草查尔酮B

Target: Beta Amyloid, Others

(E)-Flavokawain A

Cat.No: T5715

Synonym: (E)-1-(2-羟基-4,6-二甲氧基苯基)-3-(4-甲氧基苯基)-2-丙烯-1-酮,FLAVOKAVAIN A(P),卡瓦胡椒素A

Target: Apoptosis, P450

Cat.No: T7028

Synonym: LICOCHALCONEC,甘草查尔酮C

Target: Phosphatase, Antioxidant, Glucosidase

Cat.No: TN4382

Target: AMPK, mTOR

Cat.No: T4366

Target: NF-κB, Caspase

Cat.No: TN3404

Target: BCL, p38 MAPK, ROS, Akt, Caspase, Antifection, p53

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