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38

抑制剂 & 化合物

2

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Cat. No. Product Name Target Signaling Pathways
T7426 ALSTERPAULLONE

Apoptosis; GSK-3; CDK Apoptosis; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells
Alsterpaullone 是高效的 CDK 抑制剂,是一种 ATP 竞争性的 GSK-3alpha/GSK-3beta 抑制剂,且作用的 IC50值都为 4 nM。它有用于神经退行性和增生性疾病的研究潜力,具有抗肿瘤活性,诱导白血病细胞凋亡。
T10096L Voruciclib

CDK Cell Cycle/Checkpoint
Voruciclib 是一种具有口服活性和选择性 CDK 抑制剂,Ki 为 0.626 nM-9.1 nM。它在多种弥漫性大 B 细胞淋巴瘤模型中抑制 MCL-1 的表达。它有效阻断 MCL-1 的转录调节子 CDK9。
T7167 Purvalanol B

NG 95,(2R)-2-[[6-[(3-氯-4-羧基苯基)氨基]-9-(1-甲基乙基)-9H-嘌呤-2-基]氨基]-3-甲基-1-丁醇

CDK; Parasite Cell Cycle/Checkpoint; Microbiology/Virology
Purvalanol B (NG 95) 是选择性可逆的 ATP 竞争性 CDK 抑制剂。它在一系列其他蛋白激酶 (IC50>1000 nM) 中显示出对 CDK 的选择性。它抑制耐氯喹菌株 P. falciparum 的生长。
T2028 NG 52

NG52,NG-52,Compound 52

CDK Cell Cycle/Checkpoint
NG 52 (NG-52) 是可逆和 ATP 相容性且具有口服活性的Cdc28p 和Pho85p 激酶抑制剂,IC50分别为 7 μM 和 2 μM。它还抑制磷酸甘油酸激酶 1 的活性,IC50值为 2.5 μM。
T2095 Seliciclib

Roscovitine,R-roscovitine,CYC202

CDK Cell Cycle/Checkpoint
Seliciclib (Roscovitine) 是 Cdk2/cyclin E 的有效抑制剂,IC50为0.1 µM。它还抑制 Cdk7/cyclin H、Cdk5/p35 和 Cdc2/cyclin B,IC50为 0.49、0.16和0.65 µM。
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。
T14914 Cdk1/2 Inhibitor III

CDK Cell Cycle/Checkpoint
Cdk1/2 Inhibitor III 是一种具有选择性的 Cdk1/2抑制剂,对 CDK1/cyclin B 的 IC50值为2.1μM。
T14916 CDK2-IN-4

CDK Cell Cycle/Checkpoint
CDK2-IN-4 是选择性的CDK2抑制剂,对 CDK2/cyclin A 的IC50值为 44 nM,选择性高出 CDK1/cyclin B 的 2,000 倍 (IC50=86 μM)。
T5200 Indirubin-3'-monoxime

靛玉红-3' -单肟,Indirubin-3'-oxime

GSK-3; Lipoxygenase; CDK Cell Cycle/Checkpoint; Metabolism; PI3K/Akt/mTOR signaling; Stem Cells
Indirubin-3'-monoxime (Indirubin-3'-oxime) 是一种有效的 GSK3β 抑制剂,IC50值为 22 nM。它对 CDK5/p25、CDK1/cyclin B 和CDk2/cyclin E 也有作用,IC50值分别为 100、180 和 250 nM。
T6358 1-Azakenpaullone

1-氮杂坎帕罗酮,azakenpaullone

GSK-3 PI3K/Akt/mTOR signaling; Stem Cells
1-Azakenpaullone (azakenpaullone) 是一种 ATP 竞争性的、具有高度选择性的糖原合成酶激酶3 β (GSK-3β)的抑制剂,其 IC50=18 nM。
T6787 BIO-acetoxime

BIA,GSK-3 Inhibitor X

Apoptosis; GSK-3; HSV Apoptosis; Microbiology/Virology; PI3K/Akt/mTOR signaling; Stem Cells
BIO-acetoxime (GSK-3 Inhibitor X) 是一种 GSK3α/β 抑制剂,IC50值均为 10 nM,具有抗惊厥和抗感染作用。
T69188 Aloisine B

AloisineB

GSK-3; CDK Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells
Aloisine B (AloisineB) inhibited cyclin-dependent kinase and glycogen synthase kinase with IC50 values of 0.85 µM and 0.75 µM, respectively. Aloisine B has antiviral activity and can be used to study Alzheimer's, diabetes, HIV and Parkinson's.
T22260 Aminopurvalanol A

CDK Cell Cycle/Checkpoint
Aminopurvalanol A 是一种竞争性、选择性和细胞渗透性的Cyclins/Cdk 复合物抑制剂,优先靶向G2/M 期转变进而抑制癌细胞分化。它通过抑制生理获能依赖性肌动蛋白聚合而抑制精子受精能力。
T2679 BMS-265246

BMS265246

CDK Cell Cycle/Checkpoint
BMS-265246 是一种有效的选择性 CDK1/2 抑制剂,对 CDK1/cyclin B 和 CDK2/cyclin E 的 IC50分别为6 nM 和9 nM。
T16359 NU6140

CDK; Aurora Kinase Cell Cycle/Checkpoint; Chromatin/Epigenetic
NU6140 是选择性CDK2-cyclin A 抑制剂,IC50为0.41 μM。它显示出比其他 CDK 高 10 到 36 倍的选择性。它还抑制Aurora A 和Aurora B 的活性,IC50值分别为 67 和 35 nM。它还增强细胞凋亡作用并具有抗癌活性。
T15732 Ribociclib succinate

LEE011 琥珀酸盐,瑞博西尼琥珀酸盐,LEE011 succinate

CDK Cell Cycle/Checkpoint
Ribociclib succinate (LEE011 succinate) 是一种高度特异性的CDK4/6抑制剂,IC50值分别为 10 nM 和 39 nM。它对细胞周期蛋白 B/CDK1 复合物的效力低 1000 倍。
T2247 KenPaullone

9-Bromopaullone,NSC-664704,9-溴-7,12-二氢吲哚并[3,2-D][1]苯并氮杂卓-6(5H)-酮

GSK-3; CDK Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells
KenPaullone (9-Bromopaullone) 是一种CDK1/cyclin B 和GSK-3β抑制剂,IC50值分别为 0.4 μM 和 23 nM。它也抑制 CDK2/cyclin A、CDK2/cyclin E 和 CDK5/p25 的活性,IC50值分别为 0.68 μM、7.5 μM 和 0.85 μM。。它通过增强 TGFβ-Smad3 信号通路增加和延长 foxp3 基因的转录来促进 iTreg 细胞分化。
T14943 CGP60474

VEGFR; CDK; PKC Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
CGP60474 是一种高效的抗内毒素药物,抑制细胞周期蛋白依赖激酶(CDK) ,抑制 CDK1/B、CDK2/E、CDK2/a、CDK4/D、CDK5/p25、CDK7/H 和 CDK9/T 的IC50分别为 26、3、4、216、10、200 和 13 nM。它是选择性和 ATP 竞争性PKC 抑制剂。
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。
T6187 TDZD-8

GSK-3β Inhibitor I,NP 01139

GSK-3 PI3K/Akt/mTOR signaling; Stem Cells
TDZD-8 (NP 01139) 是抑制GSK-3β的抑制剂,其 IC50=2 μM。它对 Cdk-1/cyclinB,CK-II,PKA 和 PKC 的作用较弱,IC50值均 >100 μM。
T35610 2,5-dimethyl Celecoxib

Apoptosis; Wnt/beta-catenin; Prostaglandin Receptor Apoptosis; Cytoskeletal Signaling; GPCR/G Protein; Immunology/Inflammation; Stem Cells
2,5-dimethyl Celecoxib 是塞来昔布衍生物和微粒体前列腺素 E 合酶 1 (mPGES-1) 的靶向抑制剂,mPGES-1 是炎症介质 PGE2 合成途径中的关键酶。
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。
T24734 RP-106

RP 106

RP-106 is an ATP-competitive inhibitor of CDK5/p25, CDK1/cyclin B, and GSK-3.
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,
T68555 Alsterpaullone, 2-Cyanoethyl

Alsterpaullone, 2-Cyanoethyl is a selective dual inhibitor of Cdk1/cyclin B and GSK-3β.
T27033 CKD-712

CKD 712,CKD712

CKD-712 is a nuclear factor NF-kappa B inhibitor. CKD-712 suppressed MMP-9, but not MMP-2 and other NF-κB-regulated proteins involved in cancer metastasis such as VEGF. CKD-712 induced cell cycle arrest at G2M phase by suppressing cyclin A, cyclin B and C
T21377 Aloisine A

Aloisine A is a potent and selective CDK/GSK-3 inhibitor. IC50 data of Aloisine A: Cdk1/cyclin B (IC50: 150nM), Cdk2/cyclin A (IC50: 120nM), Cdk2/cyclin E (IC50: 400nM), Cdk5/p25 (IC50: 200nM), Cdk5/p35 (IC50: 160nM), GSK-3α (IC50: 500nM), GSK-3β (IC50: 6
T61890 (E/Z)-BIO-acetoxime

(E/Z)-BIO-acetoxime 是有效的,选择性的GSK-3α/β 抑制剂。对于GSK-3α/β,CDK5/p25,CDK2/cyclin A 和CDK1/cyclin B 的IC50分别为10nM,2.4μM, 4.3μM, 63μM。
T15730 Ribociclib hydrochloride

LEE011 hydrochloride,瑞博西尼盐酸盐

CDK Cell Cycle/Checkpoint
Ribociclib hydrochloride is a highly specific CDK4/6 inhibitor (IC50: 10 nM and 39 nM, respectively). It is over 1,000-fold less potent against the cyclin B/CDK1 complex.
T13454 (S)-Purvalanol B

(S)-NG 95

BCL Apoptosis
(S)-Purvalanol B 是 Purvalanol B 的 S 对映体,Purvalanol B 是一种细胞周期蛋白依赖性激酶(CDK)抑制剂。
T21950 K 00546

K00546 是一种有效的细胞周期蛋白依赖性激酶CDK1和CDK2抑制剂,对CDK1/cyclin B 和CDK2/cyclin A 的IC50分别为 0.6 nM 和 0.5 nM。K00546 也是一种有效的 CDC2 样激酶 1 (CLK1) 和CLK3抑制剂,IC50分别为 8.9 nM 和 29.2 nM。
T10172 5-Iodo-indirubin-3'-monoxime

GSK-3; CDK Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells
5-Iodo-indirubin-3'-monoxime 是一种 GSK-3β、CDK5/P25和CDK1/cyclin B 抑制剂,IC50值分别为 9、20 和 25 nM,与 ATP 竞争性地结合酶的催化位点。
T15731 Ribociclib succinate hydrate

LEE011 succinate hydrate

CDK Cell Cycle/Checkpoint
Ribociclib succinate hydrate is a highly specific CDK4/6 inhibitor (IC50s: 10 nM and 39 nM, respectively). It also is over 1,000-fold less potent against the cyclin B/CDK1 complex.
T40546 3-Methylthienyl-carbonyl-JNJ-7706621

3-Methylthienyl-carbonyl-JNJ-7706621 is a highly potent and selective inhibitor of cyclin-dependent kinase (CDK). It exhibits impressive IC50 values of 6.4 nM and 2 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. Additionally, 3-Methylthienyl-carbonyl-JNJ-7706621 demonstrates potent inhibition against GSK-3 (IC50 = 0.041 μM) and moderate potency towards CDK4, VEGF-R2, and FGF-R2 (IC50 = 0.11 μM, 0.13 μM, and 0.22 μM, respectively). Its applications in cancer research are noteworthy.
T10436L AZD4573 HCl (2057509-72-3 free base)

AZD4573 hydrochloride,AZD4573,AZD4573 HCl,AZD-4573,AZD 4573

AZD-4573 is a selective and short-acting inhibitor of the serine/threonine cyclin-dependent kinase 9, the catalytic subunit of the RNA polymerase II elongation factor positive transcription elongation factor b. It also has a potential antineoplastic activ
T69091 CBP501

CBP501 is a peptide with G2 checkpoint-abrogating activity. G2 checkpoint inhibitor CBP501 inhibits multiple serine/threonine kinases, including MAPKAP-K2, C-Tak1, and CHK1, that phosphorylate serine 216 of the dual-specific phosphatase Cdc25C (cell division checkpoint 25 C); disruption of Cdc25C activity results in the inhibition of Cdc25C dephosphorylation of the mitotic cyclin-dependent kinase complex Cdc2/cyclin B, preventing entry into the mitotic phase of the cell cycle.
T37065 6-Chloro-2-fluoropurine

6-Chloro-2-fluoropurine is a heterocyclic building block.1,2It has been used in the synthesis of purine nucleosides that inhibit cyclin-dependent kinases (CDKs)in vitro.16-Chloro-2-fluoropurine has also been used in the synthesis of purine nucleosides that are active against HIV-1 and hepatitis B virus (HBV)in vitro.2 1.Wilson, S.C., Atrash, B., Barlow, C., et al.Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitorsBioorg. Med. Chem.19(22)6949-6965(2011) 2....
T83890 Flavokawain 1i

Flavokavain 1i

Flavokawain 1i是chalcones的派生物,包括flavokawain A、flavokawain B和flavokawain C,具有抗癌和抗病毒活性。在30 µM浓度下,Flavokawain 1i能够抑制gefitinib抵抗性的H1975非小细胞肺癌(NSCLC)细胞的增殖率达到36%,同时降低热休克蛋白90(Hsp90)客体蛋白EGFR、c-Met、HER2、Akt和细胞周期依赖性激酶4(Cdk4)的蛋白水平,并提高Hsp70蛋白水平,这是Hsp90抑制的标志。肌肉内给药的Flavokawain 1i能够降低感染猪生殖与呼吸综合征病毒(PRRSV)猪只的病毒滴度。

化合物

ALSTERPAULLONE
Cat.No: T7426
Synonym:
Target: Apoptosis, GSK-3, CDK
Voruciclib
Cat.No: T10096L
Synonym:
Target: CDK
Purvalanol B
Cat.No: T7167
Synonym: NG 95,(2R)-2-[[6-[(3-氯-4-羧基苯基)氨基]-9-(1-甲基乙基)-9H-嘌呤-2-基]氨基]-3-甲基-1-丁醇
Target: CDK, Parasite
NG 52
Cat.No: T2028
Synonym: NG52,NG-52,Compound 52
Target: CDK
Seliciclib
Cat.No: T2095
Synonym: Roscovitine,R-roscovitine,CYC202
Target: CDK
Purvalanol A
Cat.No: T2059
Synonym: NG-60
Target: Apoptosis, CDK, Autophagy
Cdk1/2 Inhibitor III
Cat.No: T14914
Synonym:
Target: CDK
CDK2-IN-4
Cat.No: T14916
Synonym:
Target: CDK
Indirubin-3'-monoxime
Cat.No: T5200
Synonym: 靛玉红-3' -单肟,Indirubin-3'-oxime
Target: GSK-3, Lipoxygenase, CDK
1-Azakenpaullone
Cat.No: T6358
Synonym: 1-氮杂坎帕罗酮,azakenpaullone
Target: GSK-3
BIO-acetoxime
Cat.No: T6787
Synonym: BIA,GSK-3 Inhibitor X
Target: Apoptosis, GSK-3, HSV
Aloisine B
Cat.No: T69188
Synonym: AloisineB
Target: GSK-3, CDK
Aminopurvalanol A
Cat.No: T22260
Synonym:
Target: CDK
BMS-265246
Cat.No: T2679
Synonym: BMS265246
Target: CDK
NU6140
Cat.No: T16359
Synonym:
Target: CDK, Aurora Kinase
Ribociclib succinate
Cat.No: T15732
Synonym: LEE011 琥珀酸盐,瑞博西尼琥珀酸盐,LEE011 succinate
Target: CDK
KenPaullone
Cat.No: T2247
Synonym: 9-Bromopaullone,NSC-664704,9-溴-7,12-二氢吲哚并[3,2-D][1]苯并氮杂卓-6(5H)-酮
Target: GSK-3, CDK
CGP60474
Cat.No: T14943
Synonym:
Target: VEGFR, CDK, PKC
R547
Cat.No: T6312
Synonym: Ro 4584820
Target: Apoptosis, GSK-3, PKA, CDK
TDZD-8
Cat.No: T6187
Synonym: GSK-3β Inhibitor I,NP 01139
Target: GSK-3
2,5-dimethyl Celecoxib
Cat.No: T35610
Synonym:
Target: Apoptosis, Wnt/beta-catenin, Prostaglandin Receptor
CDK4-IN-1
Cat.No: T2082
Synonym:
Target: CDK
RP-106
Cat.No: T24734
Synonym: RP 106
Target:
Indirubin-5-sulfonate
Cat.No: T11653
Synonym:
Target: Others
Alsterpaullone, 2-Cyanoethyl
Cat.No: T68555
Synonym:
Target:
CKD-712
Cat.No: T27033
Synonym: CKD 712,CKD712
Target:
Aloisine A
Cat.No: T21377
Synonym:
Target:
(E/Z)-BIO-acetoxime
Cat.No: T61890
Synonym:
Target:
Ribociclib hydrochloride
Cat.No: T15730
Synonym: LEE011 hydrochloride,瑞博西尼盐酸盐
Target: CDK
(S)-Purvalanol B
Cat.No: T13454
Synonym: (S)-NG 95
Target: BCL
K 00546
Cat.No: T21950
Synonym:
Target:
5-Iodo-indirubin-3'-monoxime
Cat.No: T10172
Synonym:
Target: GSK-3, CDK
Ribociclib succinate hydrate
Cat.No: T15731
Synonym: LEE011 succinate hydrate
Target: CDK
3-Methylthienyl-carbonyl-JNJ-7706621
Cat.No: T40546
Synonym:
Target:
AZD4573 HCl (2057509-72-3 free base)
Cat.No: T10436L
Synonym: AZD4573 hydrochloride,AZD4573,AZD4573 HCl,AZD-4573,AZD 4573
Target:
CBP501
Cat.No: T69091
Synonym:
Target:
6-Chloro-2-fluoropurine
Cat.No: T37065
Synonym:
Target:
Flavokawain 1i
Cat.No: T83890
Synonym: Flavokavain 1i
Target:
Cat. No. Product Name Target Signaling Pathways
T6169 Indirubin

Indigopurpurin,Indigo red,NSC 105327,Couroupitine B,靛玉红

Apoptosis; Raf; GSK-3; CDK Apoptosis; Cell Cycle/Checkpoint; MAPK; PI3K/Akt/mTOR signaling; Stem Cells
Indirubin (Couroupitine B) 是一种具有抗炎症和抗癌活性的天然产物。
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。

天然产物

Indirubin
Cat.No: T6169
Synonym: Indigopurpurin,Indigo red,NSC 105327,Couroupitine B,靛玉红
Target: Apoptosis, Raf, GSK-3, CDK
Schisandrol B
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
TargetMol Loading
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