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Search Results for " cyclin-d1 "

44

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T22424	1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy)phenyl)urea	Apoptosis; STAT	Apoptosis; JAK/STAT signaling; Stem Cells
	SC-1 是一种 Sorafenib 的衍生物，可抑制 STAT3磷酸化，通过依赖 SHP-1 的 STAT3失活诱导细胞凋亡，具有抗癌作用。
T5994	KPT-6566 2-[[4-[[[4-(叔丁基)苯基]磺酰基]亚氨基]-1-氧代-1,4-二氢-2-萘基]硫基]乙酸	Others	Others
	KPT-6566 是共价结合的脯氨酰异构酶PIN1选择性抑制剂，能够与 PIN1 的催化位点共价结合，抑制并降解PIN1，具有抗癌活性。它对PIN1 PPIase 结构域的IC50=640 nM，Ki=625.2 nM。
T2378	RGB-286638 free base	GSK-3; MEK; JAK; CDK	Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; JAK/STAT signaling; MAPK; PI3K/Akt/mTOR signaling; Stem Cells
	RGB-286638 free base 是一种新型 CDK 抑制剂，抑制cyclin T1-CDK9、cyclin B1-CDK1、cyclin E-CDK2、cyclin D1-CDK4、cyclin E-CDK3和p35-CDK5活性，IC50分别为 1、2、3、4、5 和 5 nM。它也抑制 GSK-3β、TAK1、Jak2 和 MEK1，IC50值分别为 3、5、50和 54 nM。
T15335	FN-1501	FLT; CDK	Angiogenesis; Cell Cycle/Checkpoint; Tyrosine Kinase/Adaptors
	FN-1501 是一种有效的 FLT3 和 CDK 抑制剂，具有抗肿瘤的活性，对 CDK2/cyclin A、CDK4/cyclin D1、CDK6/cyclin D1 和 FLT3 的 IC50值分别为 2.47、0.85、1.96 和 0.28 nM。
T2059	Purvalanol A NG-60	Apoptosis; CDK; Autophagy	Apoptosis; Autophagy; Cell Cycle/Checkpoint
	Purvalanol A (NG-60) 是一种CDK 抑制剂，对 cdc2-cyclin B、cdc2-cyclin B、cdk2-cyclin E、cdk4-cyclin D1 和 cdk5-p35 的IC50值分别为 4、70、35、850 和 75 nM。
T3207	Briciclib ON 014185	CDK; PERK; Autophagy	Apoptosis; Autophagy; Cell Cycle/Checkpoint
	Briciclib (ON 014185) 是一种 ON 013100 衍生物，是一种抑制 Y 细胞中 cyclin D1 积累的小分子。它可靶作用于eIF4E，有抑制实体瘤的潜力。
T21720	GP-82996 Cdk4/6 Inhibitor IV,CINK4	CDK	Cell Cycle/Checkpoint
	GP-82996 (CINK4) (CINK4) 是 CDK4/6的药理学抑制剂。GP-82996 对 CDK4/cyclin D1、CDK6/cyclin D1 和 Cdk5/p35 的 IC50s 分别为 1.5、5.6 和 25 μM。GP-82996 诱导肿瘤细胞 U2OS 的凋亡，可用于癌症研究。
T60485	DIF-3
	DIF-3 is a chemical compound that acts by activating GSK-3β to facilitate the degradation of cyclin D1 and c-Myc, resulting in reduced expression levels of these proteins. In addition, DIF-3 inhibits Wnt/β-catenin signaling pathway-related proteins in DLD-1 cells. This compound exerts a potent antiproliferative effect on the HeLa human cervical cancer cell line by inducing cyclin D1 degradation and inhibiting cyclin D1 mRNA expression [1].
T39957	CDK4/6-IN-6	CDK	Cell Cycle/Checkpoint
	CDK4/6-IN-6 是CDK4/CDK6的有效抑制剂，结合CDK4/Cyclin D1 和 CDK6/Cyclin D3 的 Ki 为 0.6 nM 和 13.9 nM。
T15137	DK419	Wnt/beta-catenin; AMPK	Chromatin/Epigenetic; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Stem Cells
	DK419 是一种具有口服活性的 Wnt/β-catenin 信号通路抑制剂，IC50 为 0.19 μM。 DK419 降低 Axin2、β-catenin、c-Myc、Cyclin D1 和 Survivin 的蛋白质水平。它还诱导 pAMPK 的产生。
T16391	ON-013100	CDK	Cell Cycle/Checkpoint
	ON-013100 是有丝分裂的抑制剂，具有抗肿瘤活性。ON-013100能够抑制细胞周期蛋白 D1 的表达。
T11826	LCH-7749944 GNF-PF-2356	Apoptosis; PAK	Apoptosis; Cytoskeletal Signaling
	LCH-7749944 (GNF-PF-2356) 是一种 PAK4抑制剂，IC50为 14.93 μM。它通过下调 PAK4/c-Src/EGFR/cyclin D1 途径有效抑制人胃癌细胞的增殖，并诱导凋亡。
T2615	Flavopiridol hydrochloride Alvocidib Hydrochloride,NSC 649890,MDL 107826A,HL 275,FLAVOPIRIDOL HCL,NSC 649890 HCl	HIV Protease; CDK; Autophagy	Autophagy; Cell Cycle/Checkpoint; Microbiology/Virology; Proteases/Proteasome
	Flavopiridol hydrochloride (MDL 107826A) 是一种CDK 的广谱抑制剂，与 ATP 竞争性地抑制 CDK1，CDK2 和 CDK4 的活性，IC50值分别为 30, 170, 100 nM。
T14665L	Motixafortide TFA(664334-36-5,Free) TF 14016 TFA,BKT140 TFA,BL-8040 TFA,T140 TFA	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	Motixafortide TFA(664334-36-5,Free) (BKT140 TFA) 是 CXCR4 的拮抗剂，IC50 为～1 nM。它通过改变 miR-15a/16-1 表达下调 ERK、BCL-2、MCL-1 和 cyclin-D1 来诱导 AML 原始细胞凋亡。
T3708	BP-1-102	STAT	JAK/STAT signaling; Stem Cells
	BP-1-102 是可口服的转录因子Stat3小分子抑制剂，IC50值为 6.8 μM。
T6312	R547 Ro 4584820	Apoptosis; GSK-3; PKA; CDK	Apoptosis; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors
	R547 (Ro 4584820) 是一种口服有效，选择性， ATP 竞争性CDK 抑制剂，对 CDK1/cyclin B、 CDK2/cyclin E 和 CDK4/cyclin D1 作用的Ki 值分别为 2 nM、3 nM、1 nM。
T6924	Riviciclib hydrochloride P276-00	Apoptosis; CDK	Apoptosis; Cell Cycle/Checkpoint
	Riviciclib hydrochloride (P276-00) 是一种CDK 抑制剂，抑制CDK9-cyclinT1、CDK4-cyclin D1、CDK1-cyclinB 的IC50值分别为 20 nM、63 nM、79 nM。它对 Cisplatin 耐药性细胞具有抗肿瘤活性。
T2082	CDK4-IN-1	CDK	Cell Cycle/Checkpoint
	CDK4-IN-1 是一种新型的特异性 CDK4/Cyclin D1 抑制剂，IC50 为 10 nM；分别是 CDK1/Cyclin B (IC50>15 uM) 和 CDK2/Cyclin A (IC50=5.265 uM) 的 1500 倍和 500 倍。
T27804	LCAHA
	LCAHA is a USP2a inhibitor. LCAHA inhibits growth of cyclin D1-dependent cells.
T27128	DCB-3503 NSC716802,NSC 716802,NSC-716802,DCB3503,DCB 3503
	Tylophorine analog DCB-3503 is a potential anticancer and immunosuppressive agent. DCB-3503 suppresses the translation of cellular regulatory proteins, including cyclin D1, at the elongation step. DCB-3503 allosterically regulates the ATPase and chaperone activities of HSC70 by promoting ATP hydrolysis in the presence of specific RNA binding motifs (AUUUA) of cyclin D1 mRNA.
T63362	Ulecaciclib
	Ulecaciclib 是口服具有活力的、能够透过血脑屏障的、表现出良好的药代动力学特征的细胞周期蛋白依赖激酶 (CDK) 抑制剂，对CDKs 的ki 为 0.62 μM (CDK2/Cyclin A)、3 nM (CDK6/Cyclin D3) 、0.2 nM (CDK4/Cyclin D1)和 0.63 μM (CDK7/Cyclin H)。
T39956	CDK4/6-IN-5 CDK4/6-IN-5
	CDK4/6-IN-5 is a highly effective inhibitor of CDK4 and CDK6, with Ki values of 0.2 and 4.4 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively (WO2019207463A1, example A93).
T28266	Org-6906 Org6906,Org 6906,Org-6906 free
	Tylophorine analog Org-6906 is a potential anticancer and immunosuppressive agent. Org-6906 suppresses the translation of cellular regulatory proteins, including cyclin D1, at the elongation step. Org-6906 allosterically regulates the ATPase and chaperone activities of HSC70 by promoting ATP hydrolysis in the presence of specific RNA binding motifs (AUUUA) of cyclin D1 mRNA.
T72829	β-catenin-IN-4
	β-catenin-IN-4 是一种β-catenin 抑制剂，Ki 值为 0.64 μM。β-catenin-IN-4 降低 cyclin D1 和c-Myc 的蛋白表达水平。
T12737	Riviciclib P276-00 (free base)	Others	Others
	Riviciclib is a potent inhibitor of cyclin-dependent kinase (CDK)(CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively),with antitumor activity on cisplatin-resistant cells.
T11653	Indirubin-5-sulfonate	Others	Others
	Indirubin-5-sulfonate shows inhibitory activity against GSK-3β. Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1,
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.
T30807	CG0009 CG-0009,CG 0009
	CG0009 is a potent and highly selective glycogen synthase kinase 3 (GSK3) inhibitor that inhibitions proliferation, induces apoptosis, and activates the p53-Bax pathway in breast cancer cells through cyclin D1 depletion. CG0009 inhibit breast cancer cell
T38927	SR-1277
	SR-1277 is a highly potent, selective, and ATP competitive inhibitor of CK1δ/ε, with IC50 values of 49 nM and 260 nM, respectively. Additionally, SR-1277 exhibits inhibitory effects on FLT3, CDK4/cyclin D1, CDK6/cyclin D3, and CDK9/cyclin K, with IC50 values of 305 nM, 1340 nM, 311 nM, and 109 nM, respectively. Taken together, SR-1277 represents a valuable tool for cancer research.
T61266	CA224
	CA224 (Compound 1) 是一种选择性的、具有口服活性的Cdk4–cyclin D1抑制剂，IC50值为 6.2 μM。CA224 诱导细胞凋亡 (apoptosis)，具有抗肿瘤活性。
T73196	RGB-286638
	RGB-286638 是一种有效的 CDK 抑制剂，抑制cyclin T1-CDK9，cyclin B1-CDK1，cyclin E-CDK2，cyclin D1-CDK4，cyclin E-CDK3和p35-CDK5活性，IC50分别为 1，2，3，4，5 和 5 nM；同时可抑制GSK-3β，TAK1，Jak2和MEK1，IC50值分别为 3，5，50，和 54 nM。
T62192	CDK4/6-IN-9
	CDK4/6-IN-9 (compound 10) 是一种 CDK4/6 的选择性抑制剂，能够作用于 CDK6/cyclin D1 (IC50: 905 nM)。CDK4/6-IN-9 对多发性骨髓瘤 (MM) 具有潜在的研究价值。
T82762	Cdc25A (80-93) (human)
	Cdc25A (80-93) (human)为调控细胞周期蛋白D1及G1/S转换中相关蛋白表达，进而控制细胞增殖与肿瘤发生的多肽。该化合物在癌症研究中具应用价值。
T63982	Anticancer agent 50
	Anticancer agent 50 (compound 6) 是 ABCB1 外排泵的有效调节剂，具有细胞毒活性和抗增殖活性。Anticancer agent 50 能够减少细胞周期蛋白 D1 的表达，并诱导 p53 表达。Anticancer agent 50 对 T 淋巴瘤表现出研究潜力。
T41278	Obatoclax
	Obatoclax (GX15-070) 是一种 BH3 模拟物，是泛BCL-2家族蛋白抑制剂，对 BCL-2 的Ki 值为 220 nM。Obatoclax 诱导依赖自噬 (autophagy)的细胞死亡，并靶向细胞周期蛋白 D1 进行蛋白酶体降解。Obatoclax 具有抗癌和广谱抗寄生虫 (antiparasitic) 活性。
T83433	1D228	c-Met/HGFR	Tyrosine Kinase/Adaptors
	1D228为c-Met/TRK抑制剂，显示出抗肿瘤活性。该化合物通过抑制细胞周期蛋白D1，诱导G0/G1停滞，进而抑制癌细胞的增殖和迁移。该化合物适用于胃肿瘤、肝肿瘤和血管肿瘤研究领域。
T62514	HDAC-IN-46
	HDAC-IN-46 (compound 12c) 是一种 HDAC 的有效抑制剂，能够作用于 HDAC1 (IC50: 0.21 μM) 和 HDAC6 (IC50: 0.021 μM)的。HDAC-IN-46 在 MDA-MB-231 细胞中可以上调 p-p38，下调 Bcl-xL 和 cyclin D1。HDAC-IN-46 能够将细胞周期阻滞在 G2 期，并诱导细胞凋亡 (apoptosis)。HDAC-IN-46 能够用于三阴性乳腺癌 (TNBC) 的研究。
T68980	MRK003
	MRK003 is a γ-secretase inhibitor exhibits promising in vitro pre-clinical activity in multiple myeloma and non-Hodgkin's lymphoma. MRK003 treatment induced caspase-dependent apoptosis and inhibited proliferation of MM and NHL cell lines and patient cells. Examination of signaling events after treatment showed time-dependent decrease in levels of the notch intracellular domain, Hes1 and c-Myc. MRK003 downregulated cyclin D1, Bcl-Xl and Xiap levels in NHL cells and p21, Bcl-2 and Bcl-Xl in MM cel...
T70273	APTO-253 HCl
	APTO-253, also known as LOR-253, LT-253, is a small molecule inhibitor of human metal-regulatory transcription factor 1 (MTF-1) with potential antitumor activity. MTF-1 inhibitor LOR-253 inhibits MTF-1 activity and thereby induces the expression of MTF-1 dependent tumor suppressor factor Kruppel like factor 4 (KLF4). This subsequently leads to the downregulation of cyclin D1, blocking cell cycle progression and proliferation. This agent also causes decreased expression of genes involved in tumor...
T70706	APTO-253 isomer
	APTO-253 isomer is an isomer of APTO-253 with the Fluoro-atom in 6-position. APTO-253 also known as LOR-253, LT-253, is a small molecule inhibitor of human metal-regulatory transcription factor 1 (MTF-1) with potential antitumor activity. MTF-1 inhibitor LOR-253 inhibits MTF-1 activity and thereby induces the expression of MTF-1 dependent tumor suppressor factor Kruppel like factor 4 (KLF4). This subsequently leads to the downregulation of cyclin D1, blocking cell cycle progression and prolifer...
T72522	Aurora kinase-IN-1
	Aurora kinase-IN-1 是aurora kinase 的有效抑制剂。Aurora kinase-IN-1 上调 G1 细胞周期抑制蛋白 (包括 p21 和 p27) 以及 G1 进行性细胞周期蛋白 D1 的表达，并下调 G1-to-S 进行性细胞周期蛋白，导致细胞周期停滞在 G1/S 边界。Aurora 激酶-IN-1 还诱导细胞凋亡 (apoptosis）。Aurora 激酶-IN-1 是化疗药物的先导化合物。
T29172	YD277 YD 277,YD-277
	YD277 is a small molecule derived from ML264, a KLF5 inhibitor that elicits cytotoxic effects in colon cancer cell lines. YD277 significantly induced G1 cell cycle arrest and apoptosis in MDA-MB-231 and MDA-MB-468 TNBC cells, independent of KLF5 inhibitio
T69221	BMS-554417
	BMS-554417 is a novel inhibitor of IGF-IR, which inhibits IGF-IR and insulin receptor kinase activity and proliferation in vitro, and reduces tumor xenograft size in vivo. In a series of carcinoma cell lines, the IC50 for proliferation ranged from 120 nmol/L (Colo205) to >8.5 micromol/L (OV202). BMS-554417 treatment inhibited IGF-IR and insulin receptor signaling through extracellular signal-related kinase as well as the phosphoinositide 3-kinase/Akt pathway, as evidenced by decreased Akt phosph...
T36844	Inostamycin A
	Inostamycin A is a bacterial metabolite that has been found inStreptomycesand has anticancer activity.1It is an inhibitor of CDP-diacylglycerol:inositol 3-phosphatidyltransferase (IC50= 0.02 μg/ml in A431 cell membranes) and is selective for CDP-diacylglycerol:inositol 3-phosphatidyltransferase over phospholipase C (PLC) and phosphatidylinositol kinase at 10 μg/ml.2Inostamycin A decreases viability of YCU-T892, KCC-TC873, KB, HSC-4, and YCU-T891 oral squamous cell carcinoma (OSCC) cells in a con...

化合物

1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy)phenyl)urea

Cat.No: T22424

Target: Apoptosis, STAT

Cat.No: T5994

Synonym: 2-[[4-[[[4-(叔丁基)苯基]磺酰基]亚氨基]-1-氧代-1,4-二氢-2-萘基]硫基]乙酸

Target: Others

RGB-286638 free base

Cat.No: T2378

Target: GSK-3, MEK, JAK, CDK

Cat.No: T15335

Target: FLT, CDK

Cat.No: T2059

Synonym: NG-60

Target: Apoptosis, CDK, Autophagy

Cat.No: T3207

Synonym: ON 014185

Target: CDK, PERK, Autophagy

Cat.No: T21720

Synonym: Cdk4/6 Inhibitor IV,CINK4

Target: CDK

Cat.No: T60485

Cat.No: T39957

Target: CDK

Cat.No: T15137

Target: Wnt/beta-catenin, AMPK

Cat.No: T16391

Target: CDK

Cat.No: T11826

Synonym: GNF-PF-2356

Target: Apoptosis, PAK

Flavopiridol hydrochloride

Cat.No: T2615

Synonym: Alvocidib Hydrochloride,NSC 649890,MDL 107826A,HL 275,FLAVOPIRIDOL HCL,NSC 649890 HCl

Target: HIV Protease, CDK, Autophagy

Motixafortide TFA(664334-36-5,Free)

Cat.No: T14665L

Synonym: TF 14016 TFA,BKT140 TFA,BL-8040 TFA,T140 TFA

Target: CXCR

Cat.No: T3708

Target: STAT

Cat.No: T6312

Synonym: Ro 4584820

Target: Apoptosis, GSK-3, PKA, CDK

Riviciclib hydrochloride

Cat.No: T6924

Synonym: P276-00

Target: Apoptosis, CDK

Cat.No: T2082

Target: CDK

Cat.No: T27804

Cat.No: T27128

Synonym: NSC716802,NSC 716802,NSC-716802,DCB3503,DCB 3503

Cat.No: T63362

Cat.No: T39956

Synonym: CDK4/6-IN-5

Cat.No: T28266

Synonym: Org6906,Org 6906,Org-6906 free

β-catenin-IN-4

Cat.No: T72829

Cat.No: T12737

Synonym: P276-00 (free base)

Target: Others

Indirubin-5-sulfonate

Cat.No: T11653

Target: Others

[Ala92]-p16 (84-103)

Cat.No: TP2133

Cat.No: T30807

Synonym: CG-0009,CG 0009

Cat.No: T38927

Cat.No: T61266

Cat.No: T73196

Cat.No: T62192

Cdc25A (80-93) (human)

Cat.No: T82762

Anticancer agent 50

Cat.No: T63982

Cat.No: T41278

Cat.No: T83433

Target: c-Met/HGFR

Cat.No: T62514

Cat.No: T68980

Cat.No: T70273

APTO-253 isomer

Cat.No: T70706

Aurora kinase-IN-1

Cat.No: T72522

Cat.No: T29172

Synonym: YD 277,YD-277

Cat.No: T69221

Cat.No: T36844

Cat. No.	Product Name	Target	Signaling Pathways
TN1637	Eurycomalactone	Anti-infection; NF-κB	Microbiology/Virology; NF-κB
	Eurycomalactone 是一种NF-κB 抑制剂，IC50=0.5 μM，是一种天然产物。它可抑制蛋白合成，降低 cyclin D1 蛋白水平，但对 TNFα 诱导的 IκBα 降解或 IKKα/β 和 IκBα 的磷酸化水平没有作用。
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。
TN1674	Garcinone D 伽升沃 D	Reactive Oxygen Species; Nrf2; STAT	Immunology/Inflammation; JAK/STAT signaling; Metabolism; NF-κB; Stem Cells
	Garcinone D 是来自山竹的一种呫吨酮，可促进 C17.2 神经干细胞的增殖。它以浓度和时间依赖的方式增加磷酸化信号转导和转录激活因子 3 (p-STAT3)、Cyclin D1 和核因子红细胞 2 相关因子 (Nrf2)、以及血红素加氧酶-1 (HO-1) 的蛋白质水平。
T27305	Fascaplysin chloride NSC622398,NSC 622398,Fascaplysin,NSC-622398
	Fascaplysin is a cyclin D kinase 4/ cyclin D1 inhibitor (IC50 = 0.35 μM). Fascaplysin induces caspase mediated crosstalk between autophagy and apoptosis through the inhibition of PI3K/AKT/mTOR signaling cascade in human leukemia HL-60 cells.
TN6198	Mahanine
	Mahanine has effects on the activation of the apoptotic pathway in human leukemia U937 cells, causes the mitochondrial membranes to lose their permeability, resulting in caspase-3 activation and apoptosis. Mahanine can reverse an epigenetically silenced g

天然产物

Eurycomalactone

Cat.No: TN1637

Target: Anti-infection, NF-κB

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

Cat.No: TN1674

Synonym: 伽升沃 D

Target: Reactive Oxygen Species, Nrf2, STAT

Fascaplysin chloride

Cat.No: T27305

Synonym: NSC622398,NSC 622398,Fascaplysin,NSC-622398

Cat.No: TN6198

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