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37

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T9072	Tuxobertinib BDTX-189	EGFR; HER; BTK; RIP kinase	Angiogenesis; Apoptosis; JAK/STAT signaling; NF-κB; Tyrosine Kinase/Adaptors
	Tuxobertinib (BDTX-189) 是一种高效可口服的选择性 EGFR 和 HER2变构突变抑制剂，具有抗癌活性。它对 EGFR、HER2、BLK 和 RIPK2 的 KD 值分别为 0.2、0.76、13 和 1.2 nM。
T0686	Orlistat Ro-18-0647,奥利司他,Tetrahydrolipstatin	Apoptosis; Others; Fatty Acid Synthase	Apoptosis; Metabolism; Others
	Orlistat (Tetrahydrolipstatin) 是一种不可逆的胰腺和胃脂肪酶抑制剂，也是一种脂肪酸合成酶抑制剂，可研究肥胖症，具有抗动脉粥样硬化作用。
T11823	LB-60-OF61	NAMPT	Metabolism
	LB-60-OF61 是一种 NAMPT 抑制剂，是一种对对 MYC 癌基因的依赖性癌细胞株显示出抗增殖活性。
T36010	p38 MAPK Inhibitor	p38 MAPK	MAPK
	p38 MAPK Inhibitor 是p38 MAPK 激酶的有效抑制剂（IC50＝ 35 nM）。p38 MAPK Inhibitor 抑制癌基因RAS 诱导的衰老。
T8825	Capmatinib 2HCl.H2O INCB28060 2HCl.H2O,INC-280 2HCl.H2O,NVP-INC280 2HCl.H2O	c-Met/HGFR	Tyrosine Kinase/Adaptors
	Capmatinib 2HCl.H2O (NVP-INC280 2HCl.H2O) 是一种具有潜在抗肿瘤活性的原癌基因 c-Met (HGFR) 的口服生物可利用抑制剂。
T8970	ML162	Ferroptosis; GPX; Glutathione Peroxidase	Apoptosis; Metabolism; oxidation-reduction
	ML162 是一种共价谷胱甘肽过氧化物酶 4 抑制剂。它选择性抑制表达突变 RAS 癌基因的细胞系。
T1962	ASP3026 ASP 3026	Apoptosis; ALK	Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors
	ASP3026 是一种选择性的，具有口服活性的间变性淋巴瘤激酶抑制剂，可诱导肿瘤细胞凋亡，可研究非小细胞肺癌。
T1963	Capmatinib NVP-INC280,INC-280,卡马替尼,INCB28060	Apoptosis; c-Met/HGFR	Apoptosis; Tyrosine Kinase/Adaptors
	Capmatinib (INCB28060) 是一种具有口服活性的，选择性的，ATP 竞争性的c-Met 激酶抑制剂，IC50值为0.13 nM。它有效抑制 c-Met 依赖性肿瘤细胞的增殖和迁移，可诱导细胞凋亡，有抗肿瘤活性。
T3061	Lorlatinib 劳拉替尼,PF-6463922,PF-06463922,Loratinib	Apoptosis; Tyrosine Kinases; ROS; ALK; ROS Kinase	Angiogenesis; Apoptosis; Immunology/Inflammation; Tyrosine Kinase/Adaptors
	Lorlatinib (PF-6463922) 是一种具有口服活性，选择性，脑渗透性和 ATP 竞争性的ROS1/ALK 抑制剂，具有抗癌活性。它对 ROS1、野生型 ALK 和 ALKL1196M 的Ki 值分别为 <0.025 nM、<0.07 nM 和 0.7 nM。
T3455	Merestinib LY2801653	Discoidin Domain Receptor (DDR); FLT; c-Met/HGFR; ROS; ROS Kinase	Angiogenesis; Immunology/Inflammation; Tyrosine Kinase/Adaptors
	Merestinib (LY2801653) 是一种有效的口服生物可利用的具有抗肿瘤活性的c-Met 抑制剂。
TP2311	C-MYC PEPTIDE EPITOPE TFA	Others	Others
	C-MYC PEPTIDE EPITOPE TFA 是 c-myc 原癌基因的产物，是一种螺旋-环-螺旋亮氨酸拉链磷蛋白，可调节细胞增殖、细胞分化和凋亡中的基因转录。该肽是人类 c-myc 表位。
T69877	SPOP-IN-6lc	Apoptosis	Apoptosis
	SPOP-IN-6lc 是一种有效的 SPOP 抑制剂，在癌症中有多种作用，在多种肿瘤中有抑癌作用，在肾癌中却发挥着癌基因功能。SPOP-IN-6lc 可用于研究细胞信号传送和细胞凋亡。
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。
T3678	Entrectinib RXDX-101,恩曲替尼,NMS-E628	Trk receptor; ROS; ALK; Autophagy; ROS Kinase	Angiogenesis; Autophagy; Immunology/Inflammation; Tyrosine Kinase/Adaptors
	Entrectinib (RXDX-101) 是一种可口服的 Trk、ROS1和 ALK 抑制剂，具有抗肿瘤和中枢神经活性，抑制 TrkA、TrkB、TrkC、ROS1 和 ALK 的 IC50值分别为 1、3、5、12 和 7 nM。
T63790	Cbl-b-IN-3	E1/E2/E3 Enzyme	Ubiquitination
	Cbl-b-IN-3是一种有效的casitas b 系淋巴瘤原癌基因-b (Cbl-b)抑制剂（ic50 < 1 nM）。Cbl-b 是一种环型E3泛素蛋白连接酶，与T 淋巴细胞激活阈值的设定有关。Cbl-b 以不依赖于蛋白水解的方式负调控p85，通过其E3泛素连接酶活性，参与了p85向CD28和T 细胞抗原受体ζ的募集，抑制PI3K 抑制了Cblb-/- t 细胞活化的增强。
T39491	HS-131
	HS-131, a near-infrared dye-conjugated Hsp90 inhibitor, effectively identifies oncogene-driven breast cancers across various molecular subtypes.
T31864	FPFS-1169 HCl R-(-)-BPAP,FPFS 1169,FPFS-1169 hydrochloride,BPAP-cpd,R-FPFS-1169,FPFS1169
	FPFS-1169 (BPAP-CPD, R-(-)-BPAP, R- FpFS-1169) is a proto-oncogene protein C-Bcl-2 stimulant that is one of the "catecholaminergic and serotonergic enhancers" and may be used for the treatment of Parkinson's disease.
T38936	KRAS G13D peptide, 25 mer KRAS G13D peptide, 25 mer
	KRAS G13D peptide, a 25-mer sequence, is derived from the KRAS activating oncogene mutation and serves as an immune potentiator. This peptide possesses immunogenic properties and can be utilized for the development of a KRAS vaccine.
T21676	SCH 51344
	SCH 51344 抑制Ras 诱导的恶性转化。SCH 51344可防止癌基因转化的成纤维细胞的非锚定生长。
T70060	PF-06463922 acetate
	PF-06463922 acetate is a potent, selective brain-penetrable inhibitor of both anaplastic lymphoma kinase (ALK) and c-ros Oncogene 1 (ROS1) with strong activity against all known ALK and ROS1 mutants identified in patients with crizotinib-resistant disease. PF-06463922 is in clinical trials for the treatment of non–small cell lung cancer (NSCLC).
T22633	CCT251545 analogue, Compound 51	Others	Others
	CCT251545 analog is a potent and selective CDK8/19 inhibitor (IC50: 5.1 nM and 5.6 nM, respectively). Mediator complex-associated kinases CDK8 and CDK19 are involved in the regulation of multiple transcription pathways. CDK8 plays as an oncogene in gastri
T63359	c-Myc inhibitor 4
	c-Myc inhibitor 4 是有效的、口服具有活性的 c-Myc-reducing 化合物。C-Myc 是一种重要的原癌基因，与多种肿瘤的发生发展密切相关。
T81285	RGB-1
	RGB-1为多环芳烃类化合物，作为RNA G-四链体 (RNA G-quadruplexes) 的稳定剂，能够抑制RNA翻译，并在乳腺癌细胞中下调NRAS原癌基因的表达。
T71187	Foretinib phosphate
	Foretinib phosphate is an orally bioavailable small molecule with potential antineoplastic activity. MET/VEGFR2 inhibitor GSK1363089 binds to and selectively inhibits hepatocyte growth factor (HGF) receptor c-MET and vascular endothelial growth factor receptor 2 (VEGFR2), which may result in the inhibition of tumor angiogenesis, tumor cell proliferation and metastasis. The proto-oncogene c-MET has been found to be over-expressed in a variety of cancers.
T71177	LCRF-0004
	LCRF-0004 is a potent and selective RON receptor tyrosine kinase inhibitor. The RON receptor tyrosine kinase has been identified as an important mediator of KRAS oncogene addiction and is overexpressed in the majority of pancreatic cancers. Preclinical studies show that inhibition of RON function decreases pancreatic cancer cell migration, invasion, and survival and can sensitize pancreatic cancer cells to chemotherapy. RON receptor tyrosine kinase is a potential as a therapeutic target.
T78896	SHP2-IN-22
	SHP2-IN-22 作为变构抑制剂，靶向SHP2，具有 17.7 nM 的 IC50。该化合物能够有效抑制MIA PaCa-2胰腺癌细胞的增殖、迁移和侵袭行为。SHP2-IN-22 主要用于研究含Kirsten大鼠肉瘤病毒癌基因(KRAS)突变型的癌症。
T35822	CAY10722
	CAY10722 is an inhibitor of sirtuin 3 (SIRT3), a class III HDAC (71% inhibition at 200 μM). SIRT3 is involved in modulating metabolic homeostasis as a NAD+-dependent protein deacetylase in the mitochondria. SIRT3 functions as either an oncogene or tumor suppressor, depending on cancer cell type. High SIRT3 expression in patient-derived esophageal cancer tissues is associated with shorter survival and, in mice, downregulation leads to a lower tumor load. In contrast, low SIRT3 expression in patie...
T70748	Bisthianostat
	Bisthianostat, also known as CF367 or CF367;-C, is a novel Orally Efficacious Pan-HDAC Inhibitor. Bisthianostat selectively binds to and inhibits HDACs, which inhibits deacetylation of histone proteins and leads to the accumulation of highly acetylated histones. This may result in an induction of chromatin remodeling, the inhibition of tumor oncogene transcription, and the selective transcription of tumor suppressor genes. This prevents cell division, induces cell cycle arrest and apoptosis. Thi...
T72201	Pyridostatin hydrochloride RR82 hydrochloride
	Pyridostatin (RR82) hydrochloride 是一种高选择性的 G-quadruplexDNA 稳定剂 (Kd=490 nM)。Pyridostatin hydrochloride 通过诱导复制和转录依赖的 DNA 损伤促进人类癌细胞生长停滞。Pyridostatin hydrochloride 靶向原癌基因 Src。Pyridostatin hydrochloride 降低人乳腺癌细胞 SRC 蛋白水平和 SRC 依赖的细胞运动。
T83846	HOXB7 (8-25) TFA Homeobox B7 (8-25)
	HOXB7 (8-25) 是 homeobox B7 (HOXB7) 的肽段，是细胞增殖的主要调控因子和肿瘤基因途径的激活剂。通过 HOXB7 (8-25) 肽脉冲的树突状细胞展示抗原，这些树突状细胞来源于分离的人类外周血单核细胞（PBMCs），刺激CD4+辅助T细胞的激活和IFN-γ的产生，从而引发特异性和多向性肿瘤反应性的抗肿瘤反应。
T62911	Dalmelitinib
	Dalmelitinib 是一种选择性的、口服具有活力的 c-Met 激酶抑制剂 (IC50: 2.9 nM)，能够结合 c-Met 的 ATP-binding 区域。 Dalmelitinib 能够诱导 MET 的磷酸化，部分或完全抑制 AKT 和 ERK 的磷酸化。Dalmelitinib 对癌细胞 (c-Met 癌基因扩增) 的增殖表现出有效的抑制作用，可以用于研究癌症（如非小细胞肺癌）。
T35558	KAAD-Cyclopamine
	Cyclopamine-KAAD is a potent inhibitor of hedgehog signaling with an IC50 value of 20 nM in a Shh-LIGHT2 assay. It blocks binding of BODIPY-cyclopamine to cells expressing Smoothened (Smo) in a dose-dependent manner. Cyclopamine-KAAD is cell-permeable and binds to SmoA1 to promote its exit from the endoplasmic reticulum. It inhibits the invasion and migration (45.9 and 43.3% inhibition, respectively) of Bel-7402 hepatocarcinoma cells and decreases the expression of nuclear glioma-associated onco...
T64072	Cbl-b-IN-2
	Cbl-b-IN-2 是一种口服具有活力的生物化合物，能够抑制泛素蛋白酶体通路中的 E3 酶Casitas b 系淋巴瘤原癌基因-b (Cbl-b)，可以用于调节免疫系统和易受免疫系统调节疾病的研究。Cbl-b-IN-2 也能够单独或与一种或多种免疫检查点抑制剂，抗肿瘤剂和放射剂联合应用于癌症的研究。
T35430	Afatinib impurity 11
	Afatinib impurity 11 is an impurity of Afatinib. Afatinib is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively[1]. [1]. Li D, et al. BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene. 2008 Aug 7;27(34):4702-11.
T79801	TCIP 1	Epigenetic Reader Domain	Chromatin/Epigenetic
	TCIP 1是一款转录/表观遗传CIPs（TCIP）小分子，结构上为能够分别与BCL6和BRD4结合的小分子共价连接而成。该分子通过募集内源性癌症驱动因子或下游转录因子至细胞死亡基因的启动子，促进胞死亡基因的表达。TCIP 1能形成功能性三元复合物，特异性地与BCL6和BRD4作用，从而取消BCL6对凋亡基因的抑制，增强促凋亡基因的转录活性，并触发细胞凋亡。此外，TCIP 1有效降低致癌基因MYC的表达，并抑制弥漫大B细胞淋巴瘤（DLBCL）的增长。
T37581	SCIO 469 hydrochloride
	Selective, ATP-competitive p38 inhibitor (IC50 = 9 nM for p38α in vitro). Displays approximately 10-fold selectivity for p38α over p38β and 2000-fold selectivity for p38α over 20 other kinases. Reduces p38α phosphorylation in multiple myeloma cells in vitro and in vivo; activity results in decreased tumor burden and angiogenesis in murine models of multiple myeloma. Also enhances bortezomib-induced cytotoxicity against multiple myeloma cells. Hideshima et al (2004) p38 MAPK inhibition enhances P...
T35536	Tpl2 Kinase Inhibitor (hydrochloride)
	Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5...

化合物

Cat.No: T9072

Synonym: BDTX-189

Target: EGFR, HER, BTK, RIP kinase

Cat.No: T0686

Synonym: Ro-18-0647,奥利司他,Tetrahydrolipstatin

Target: Apoptosis, Others, Fatty Acid Synthase

Cat.No: T11823

Target: NAMPT

p38 MAPK Inhibitor

Cat.No: T36010

Target: p38 MAPK

Capmatinib 2HCl.H2O

Cat.No: T8825

Synonym: INCB28060 2HCl.H2O,INC-280 2HCl.H2O,NVP-INC280 2HCl.H2O

Target: c-Met/HGFR

Cat.No: T8970

Target: Ferroptosis, GPX, Glutathione Peroxidase

Cat.No: T1962

Synonym: ASP 3026

Target: Apoptosis, ALK

Cat.No: T1963

Synonym: NVP-INC280,INC-280,卡马替尼,INCB28060

Target: Apoptosis, c-Met/HGFR

Cat.No: T3061

Synonym: 劳拉替尼,PF-6463922,PF-06463922,Loratinib

Target: Apoptosis, Tyrosine Kinases, ROS, ALK, ROS Kinase

Cat.No: T3455

Synonym: LY2801653

Target: Discoidin Domain Receptor (DDR), FLT, c-Met/HGFR, ROS, ROS Kinase

C-MYC PEPTIDE EPITOPE TFA

Cat.No: TP2311

Target: Others

Cat.No: T69877

Target: Apoptosis

Cat.No: T3661

Synonym: ACY241,HDAC-IN-2

Target: HDAC

Cat.No: T3678

Synonym: RXDX-101,恩曲替尼,NMS-E628

Target: Trk receptor, ROS, ALK, Autophagy, ROS Kinase

Cat.No: T63790

Target: E1/E2/E3 Enzyme

Cat.No: T39491

Cat.No: T31864

Synonym: R-(-)-BPAP,FPFS 1169,FPFS-1169 hydrochloride,BPAP-cpd,R-FPFS-1169,FPFS1169

KRAS G13D peptide, 25 mer

Cat.No: T38936

Synonym: KRAS G13D peptide, 25 mer

Cat.No: T21676

PF-06463922 acetate

Cat.No: T70060

CCT251545 analogue, Compound 51

Cat.No: T22633

Target: Others

c-Myc inhibitor 4

Cat.No: T63359

Cat.No: T81285

Foretinib phosphate

Cat.No: T71187

Cat.No: T71177

Cat.No: T78896

Cat.No: T35822

Cat.No: T70748

Pyridostatin hydrochloride

Cat.No: T72201

Synonym: RR82 hydrochloride

HOXB7 (8-25) TFA

Cat.No: T83846

Synonym: Homeobox B7 (8-25)

Cat.No: T62911

KAAD-Cyclopamine

Cat.No: T35558

Cat.No: T64072

Afatinib impurity 11

Cat.No: T35430

Cat.No: T79801

Target: Epigenetic Reader Domain

SCIO 469 hydrochloride

Cat.No: T37581

Tpl2 Kinase Inhibitor (hydrochloride)

Cat.No: T35536

Cat. No.	Product Name	Target	Signaling Pathways
TQ0165	Arglabin 阿格拉宾,(+)-Arglabin	NOD-like Receptor (NLR); Transferase; NOD; Autophagy	Autophagy; Immunology/Inflammation; Metabolism; NF-κB
	Arglabin ((+)-Arglabin) 是从青蒿中分离出的一种天然产物，是一种 NLRP3 炎性体抑制剂，具有抗动脉粥样硬化和抗癌作用。
T5S1103	Isoliensinine 异莲心碱,Isoliensinin	Apoptosis; Antioxidant	Apoptosis; oxidation-reduction
	Isoliensinine (Isoliensinin) 是从水芙蓉种子胚中提取的一种双苄基异喹啉生物碱，能诱导三阴性乳腺癌细胞凋亡，具有抗氧化、抗炎、抗癌活性。
TN2063	Physalin B NSC-287088	Apoptosis; NF-κB; Akt; PI3K; Nrf2; NOD	Apoptosis; Cytoskeletal Signaling; Immunology/Inflammation; NF-κB; PI3K/Akt/mTOR signaling
	Physalin B 是茄科植物的主要活性化合物之一，具有广泛的生物活性，可用于治疗炎症湿疹和疱疹等疾病。Physalin B 通过激活 PI3K/Akt 通路抑制 NF-κB 和 NLRP3，从而改善脂多糖诱导的急性肺损伤造成的炎症反应。Physalin B 通过激活 Nrf2 通路抑制 PDGF-BB 诱导的 VSMC 增殖、迁移和表型转化。Physalin B 通过抑制 LAP2α-HDAC1 介导的胶质瘤相关癌基因 1 的去乙酰化和肝星状细胞活化来发挥抗肿瘤活性。

天然产物

Cat.No: TQ0165

Synonym: 阿格拉宾,(+)-Arglabin

Target: NOD-like Receptor (NLR), Transferase, NOD, Autophagy

Cat.No: T5S1103

Synonym: 异莲心碱,Isoliensinin

Target: Apoptosis, Antioxidant

Cat.No: TN2063

Synonym: NSC-287088

Target: Apoptosis, NF-κB, Akt, PI3K, Nrf2, NOD

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