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Search Results for " retinoblastoma "

12

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T15648	KDM5-C70	Histone Demethylase	Chromatin/Epigenetic
	KDM5-C70 是 KDM5-C49 的乙酯衍生物，是一种有效的细胞渗透性泛 KDM5 组蛋白去甲基化酶抑制剂。它在骨髓瘤细胞中具有抗增殖作用，可诱导全基因组 H3K4me3 水平升高。
T8350	TPCK	Proteasome	Proteases/Proteasome; Ubiquitination
	TPCK 是丝氨酸蛋白酶抑制剂，通过与 HPV-18 E7 蛋白的视网膜母细胞瘤蛋白 (RB) 结合核心发生反应，并能够消除其 RB 结合能力。将它添加到培养基内，可修饰活角质形成细胞中的 E7 蛋白。
T7698	BS194 (2S,3S)-3-[[3-(异丙基)-7-[(苯基甲基)氨基]吡唑并[1,5-A]嘧啶-5-基]氨基]-1,2,4-丁三醇	CDK	Cell Cycle/Checkpoint
	BS194 是一种有效的细胞周期蛋白依赖性蛋白激酶 (CDK) 抑制剂。
T21314	Amsilarotene TAC-101,TAC 101,TAC101	CDK	Cell Cycle/Checkpoint
	Amsilarotene (TAC101) 是口服有活性的合成类视黄醇，对视黄酸受体 α (RAR-α) 具有选择性亲和力，对 RAR-α 和 RAR-β 的 Ki=为 2.4 nM 和 400 nM。它可造成人胃癌、卵巢癌细胞及肝细胞癌的凋亡，可用于研究癌症。
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。
T26855	BMS-665053 BMS665053
	BMS-665053 is a corticotropin-releasing factor-1 (CRF1) receptor antagonist (IC50 = 1.0 nM). BMS-665053)11 is a potent inhibitor of CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells (IC50 = 4.9 nM). In addi
T70377	BAY 61-3606 HCl
	BAY 61-3606 HCl is a cell-permeable, reversible inhibitor of spleen tyrosine kinase. BAY 61-3606 HCl can inhibit degranulation and block cytokine release from mast cells. Oral administration of BAY 61-3606 to rats was shown to suppress antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema. It can also sensitize MCF-7 breast cancer cells to TNF-related apoptosis-inducing ligand (TRAIL)-mediated apoptosis by inhibiting Cdk9. This compound has been used i...
T26456	A 83586C A83586C,A-83586C
	A-83586C is a depsipeptide antibiotic from Streptomyces karnatakensis with potent against Gram-positive activity in vitro. A-83586C acts as a highly potent inhibitor of beta-catenin/TCF4 signaling within cancer cells, while simultaneously downregulating o
T72928	CDK4/6-IN-15
	CDK4/6-IN-15 是一种口服有效和选择性 CDK4/6抑制剂。CDK4/6-IN-15 能有效抑制癌细胞生长。CDK4/6-IN-15 将细胞周期阻滞在 G1 期，并抑制视网膜母细胞瘤肿瘤抑制蛋白 (Rb) 在 S780 位点的磷酸化和 E2 因子 (E2F) 调控的基因表达。
T62235	CDK-IN-9
	CDK-IN-9 (compound 24) 是一种 CDK 的有效抑制剂。CDK-IN-9 也是一种能够诱导 CDK12 和 DDB1 相互作用的分子胶，能够作用于 CDK2/E (IC50: 4 nM) 。CDK-IN-9 能够导致细胞周期蛋白 K (cyclin K) 的多泛素化及其随后的降解。CDK-IN-9 可以利用去磷酸化视网膜母细胞瘤蛋白和RNA 聚合酶 II，进而诱导细胞凋亡 (apoptosis)。
T69196	AG-012986
	AG-012986 is a multitargeted cyclin-dependent kinase (CDK) inhibitor active against CDK1, CDK2, CDK4/6, CDK5, and CDK9, with selectivity over a diverse panel of non-CDK kinases. AG-012986 showed antiproliferative activities in vitro with IC(50)s of <100 nmol/L in 14 of 18 tumor cell lines. In vivo, significant antitumor efficacy induced by AG-012986 was seen (tumor growth inhibition, >83.1%) in 10 of 11 human xenograft tumor models. AG-012986 also showed dose-dependent retinoblastoma Ser(795) hy...
T69197	AG-012986 HCl
	AG-012986 HCl is a multitargeted cyclin-dependent kinase (CDK) inhibitor active against CDK1, CDK2, CDK4/6, CDK5, and CDK9, with selectivity over a diverse panel of non-CDK kinases. AG-012986 HCl showed antiproliferative activities in vitro with IC(50)s of <100 nmol/L in 14 of 18 tumor cell lines. In vivo, significant antitumor efficacy induced by AG-012986 HCl was seen (tumor growth inhibition, >83.1%) in 10 of 11 human xenograft tumor models. AG-012986 HCl also showed dose-dependent retinoblas...

化合物

Cat.No: T15648

Target: Histone Demethylase

Cat.No: T8350

Target: Proteasome

Cat.No: T7698

Synonym: (2S,3S)-3-[[3-(异丙基)-7-[(苯基甲基)氨基]吡唑并[1,5-A]嘧啶-5-基]氨基]-1,2,4-丁三醇

Target: CDK

Cat.No: T21314

Synonym: TAC-101,TAC 101,TAC101

Target: CDK

Cat.No: T9636

Synonym: SHR-6390

Target: CDK

Cat.No: T26855

Synonym: BMS665053

BAY 61-3606 HCl

Cat.No: T70377

Cat.No: T26456

Synonym: A83586C,A-83586C

Cat.No: T72928

Cat.No: T62235

Cat.No: T69196

Cat.No: T69197

Cat. No.	Product Name	Target	Signaling Pathways
T6S1917	Schisandrol B Gomisin A,TJN-101,Besigomsin,五味子醇乙,Gamma-Schisandrin,戈米辛A,Schizandrol B,Wuweizi alcohol-B	P450; Reactive Oxygen Species; Autophagy	Autophagy; Immunology/Inflammation; Metabolism; NF-κB
	Schisandrol B (Besigomsin) 是华中五味子的主要活性成分，具有保肝、抗炎、抗糖尿病和抗氧化的作用。它抑制活性氧的产生，也抑制 P-糖蛋白和CYP3A 的活性。
T72100	D-erythro-Sphingosine hydrochloride Erythrosphingosine hydrochloride,trans-4-Sphingenine hydrochloride,erythro-C18-Sphingosine hydrochloride,Erythrosphingosine hydrochloride ; erythro-C18-Sphingosine hydrochloride ; trans-4-Sphingenine hydrochloride
	D-erythro-Sphingosine (Erythrosphingosine) hydrochloride 是一种特异性 TRPM3活化剂。D-erythro-Sphingosine 还诱导视网膜母细胞瘤蛋白 (retinoblastoma protein) 去磷酸化。
T4110	Perivine Perivin,派利文碱	Others	Others
	Perivine (Perivin) 以视网膜母细胞瘤相关蛋白 (RbAp48) 为靶点，能够解决 RbAp48-FOG-1 复合物的不稳定性。Perivine 可用于研究阿尔茨海默病。

天然产物

Cat.No: T6S1917

Synonym: Gomisin A,TJN-101,Besigomsin,五味子醇乙,Gamma-Schisandrin,戈米辛A,Schizandrol B,Wuweizi alcohol-B

Target: P450, Reactive Oxygen Species, Autophagy

D-erythro-Sphingosine hydrochloride

Cat.No: T72100

Synonym: Erythrosphingosine hydrochloride,trans-4-Sphingenine hydrochloride,erythro-C18-Sphingosine hydrochloride,Erythrosphingosine hydrochloride ; erythro-C18-Sphingosine hydrochloride ; trans-4-Sphingenine hydrochloride

Cat.No: T4110

Synonym: Perivin,派利文碱

Target: Others

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