Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
T64373 |
CDK1-IN-2
cdk1 inhibitor 2 |
CDK | Cell Cycle/Checkpoint |
CDK1-IN-2 (cdk1 inhibitor 2)是一种CDK1抑制剂,IC50为5.8μM。CDK1-IN-2的激酶谱显示了多种激酶的非选择性抑制。 | |||
T1778 |
AT7519 Hydrochloride
AT7519 HCl,AT 7519 hydrochloride salt |
Apoptosis; GSK-3; CDK | Apoptosis; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells |
AT7519 Hydrochloride (AT7519 HCl) 是一种多CDK 抑制剂,对 CDK1、CDK2、CDK4-CDK6 以及 CDK9 的IC50值分别为 210、47、100、13、170 和 <10 nM。 | |||
T12617 |
(R)-CR8 trihydrochloride
CR8, (R)-Isomer trihydrochloride |
Apoptosis; CDK | Apoptosis; Cell Cycle/Checkpoint |
(R)-CR8 trihydrochloride (CR8, (R)-Isomer trihydrochloride) 是一种 CDK1/2/5/7/9 抑制剂,可作为分子胶降解剂,具有神经保护活性,可诱导细胞凋亡。 | |||
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。 | |||
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。 | |||
T6525 |
GW 5074
GW5074,3-(3,5-二溴-4-羟基苯亚甲基)-5-碘-1,3-二氢吲哚-2-酮,Raf1 Kinase Inhibitor I |
Apoptosis; Raf | Apoptosis; MAPK |
GW 5074 (Raf1 Kinase Inhibitor I) 是一种有效且特异性的 c-Raf 抑制剂,IC50值为 9 nM。 它对 JNK1/2/3、MEK1、MKK6/7、CDK1/2、c-Src、p38 MAP、VEGFR2 或 c-Fms 的活性没有影响。 | |||
T6162 |
BS-181 hydrochloride
BS-181 HCl |
CDK | Cell Cycle/Checkpoint |
BS-181 hydrochloride (BS-181 HCl) 是一种高度选择性的CDK7抑制剂,IC50值为 21 nM。它对 CDK7 的选择性是对 CDK1、2、4、5、6 和 9 的 40 倍以上。 | |||
T6205 |
AT7519
|
Apoptosis; GSK-3; CDK | Apoptosis; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells |
AT7519 是一种CDK 抑制剂,对 CDK1,CDK2,CDK4-CDK6 以及 CDK9 的IC50值分别为 210,47,100,13,170 和 <10 nM。 | |||
T6612 |
NU6027
|
ATM/ATR; DNA-PK; CDK | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
NU6027 是一种有效的 ATR/CDK 抑制剂,抑制 CDK1/2、ATR 和 DNA-PK,Ki 为 2.5 μM/1.3 μM、0.4 μM 和 2.2 μM。它以 ATR 依赖性方式增强羟基脲和顺铂的细胞毒性。 | |||
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。 | |||
T6081 |
Milciclib
PHA-848125 |
Trk receptor; CDK; Autophagy | Autophagy; Cell Cycle/Checkpoint; Tyrosine Kinase/Adaptors |
Milciclib (PHA-848125) 是一种 ATP 竞争性的 CDK 和原肌球蛋白受体激酶双重抑制剂,作用于 CDK2,IC50 为 45 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/cyclin B,CK-II,PKA 和 PKC 的作用较弱,IC50值均 >100 μM。 | |||
T9014 |
SKI-178
|
Apoptosis; S1P Receptor | Apoptosis; GPCR/G Protein |
SKI-178 是一种鞘氨醇激酶-1(SphK1)和 SphK2抑制剂,以 CDK1 依赖性方式诱导人急性髓性白血病细胞凋亡。 | |||
T6940 |
PHA-767491 hydrochloride
CAY10572,PHA-767491,PHA767491 HCl,CAY-10572 hydrochloride |
Apoptosis; GSK-3; CDK | Apoptosis; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells |
PHA-767491 hydrochloride (CAY-10572 hydrochloride) 是一种Cdc7-Dbf4(DDK)/Cdk9的双重抑制剂,IC50值分别为 10 nM 和 34 nM。 | |||
T6077 |
ZM-447439
|
Apoptosis; MEK; Src; Aurora Kinase | Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; MAPK; Tyrosine Kinase/Adaptors |
ZM 447439是一种极光激酶 (aurora) 抑制剂,对aurora A 和B 的IC50值分别为110和130 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。 | |||
T12617L |
(R)-CR8
(R)-CR8,(R)-Isomer,(2R)-2-[[9-异丙基-6-[[[4-(2-吡啶基)苯基]甲基]氨基]-9H-嘌呤-2-基]氨基]-1-丁醇,CR8 |
Apoptosis; CDK | Apoptosis; Cell Cycle/Checkpoint |
(R)-CR8 ((R)-Isomer) 是 Roscovitine 类似物,是CDK1/2/5/7/9抑制剂。它作为一种分子胶降解剂来消耗细胞周期蛋白 K。它诱导细胞凋亡并具有神经保护作用。 | |||
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。 | |||
T68555 |
Alsterpaullone, 2-Cyanoethyl
|
||
Alsterpaullone, 2-Cyanoethyl is a selective dual inhibitor of Cdk1/cyclin B and GSK-3β. | |||
T28493 |
R-547 mesylate
RO-4584820 mesylate,RG-547 mesylate |
||
R547 Mesylate is a potent ATP-competitive inhibitor of CDK1, CDK2, CDK4 with Ki value of 2 nM, 3 nM, 1 nM respectively. | |||
T60583 |
CDK1/2/4-IN-1
|
||
CDK1/2/4-IN-1 (compound 3a) 是 CDK 的有效抑制剂, 其对于 CDK1、CDK2 和 CDK4 的 IC50值分别为 1.47、0.78 和 0.87 μM。CDK1/2/4-IN-1 可用于癌症研究。CDK1/2/4-IN-1 可将细胞周期阻滞在 G2/M 期并诱导细胞凋亡。CDK1/2/4-IN-1 提高 Bax、caspase-3和 P53 的水平并降低 Bcl-2 水平。 | |||
T1947 |
BS-181
BS 181 |
Apoptosis; CDK | Apoptosis; Cell Cycle/Checkpoint |
BS-181 是一种高度选择性的 CDK7 抑制剂,IC50为21 nM。它抑制CDK2、CDK5 和 CDK9 的IC50值分别为 880 nM、3000 nM 和 4200 nM 。它诱导细胞凋亡,有癌症研究相关的研究潜力。 | |||
T69200 | CGP74514A | ||
CGP74514A is a CDK1 inhibitor with potential anticancer activity. In U937 cells, CGP74514A - induced apoptosis (5 microM) became apparent within 4 hr and approached 100% by 24 hr. The pan- caspase inhibitor Boc-fmk and the caspase-8 inhibitor lETD-fmk opposed CGP74514A -induced caspase-9 activation and PARP degradation, but not cytochrome c or Smac/DIABLO release. CGP74514A -mediated apoptosis was substantially blocked by ectopic expression of full-length Bel- 2, a loop-deleted mutant Bcl-2, and... | |||
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。 | |||
T61061 | JH295 hydrate | ||
JH295 hydrate 通过 Cys22 烷基化从而抑制细胞Nek2,它是有效的,不可逆和选择性的NIMA 相关激酶 2 (Nek2)抑制剂 (IC50 = 770 nM)。JH295 hydrate 对有丝分裂激酶 Cdk1,Aurora B 或 Plk1 不具有活性,不干扰双极纺锤体组件或纺锤体组件检查点。 | |||
T35650 | Samuraciclib trihydrochloride | ||
Samuraciclib (CT7001) trihydrochloride is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib trihydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib trihydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib trihydrochloride has anti-tumor effects[1][2]. | |||
T62695 |
GFB-12811
|
||
GFB-12811,一种具有高选择性的口服活性CDK5抑制剂,其IC50为2.3 nM。该化合物对其他CDK激酶(CDK1/2/6/7/9)表现出显著的选择性。 | |||
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. | |||
T63664 |
CDK/HDAC-IN-2
|
||
CDK/HDAC-IN-2 是有效的 HDAC/CDK 双重抑制剂,能够作用于 HDAC1 (IC50: 6.4 nM)、HDAC2 (IC50: 0.25 nM)、HDAC3 (IC50: 45 nM)、HDAC6,8 (IC50>1000 nM)、CDK1 (IC50: 8.63 nM)、CDK2 (IC50: 0.30 nM)、CDK4,6,7 (IC50>1000 nM)。CDK/HDAC-IN-2 能够将细胞周期停滞在 G2/M 期,并诱导细胞凋亡 (apoptosis)。CDK/HDAC-IN-2 具有优异的抗增殖效果,显示出显著的抗肿瘤作用。 | |||
T38710 |
JH295
|
||
JH295 is a highly potent and selective inhibitor of NIMA-related kinase 2 (Nek2), exhibiting irreversible inhibition activity with an IC 50 value of 770 nM. This compound effectively inhibits cellular Nek2 using the alkylation of Cys22. Importantly, JH295 does not exhibit any inhibitory effects toward Cdk1, Aurora B, or Plk1, which are kinases involved in mitotic processes. Furthermore, JH295 has no impact on bipolar spindle assembly or the spindle assembly checkpoint mechanism. | |||
T61835 |
Samuraciclib
|
||
Samuraciclib (CT7001) is a potent, selective, and orally active inhibitor of CDK7, with an ATP-competitive nature. It effectively inhibits CDK7 with an IC 50 value of 41 nM. Furthermore, Samuraciclib demonstrates remarkable selectivity ratios, with 45-fold, 15-fold, 230-fold, and 30-fold selectivity over CDK1, CDK2 (IC 50 of 578 nM), CDK5, and CDK9, respectively. Notably, Samuraciclib has been found to inhibit the growth of breast cancer cell lines, exhibiting GI 50 values ranging between 0.2-0.... | |||
T83936 |
LL-K9-3
|
||
LL-K9-3是一种基于选择性疏水标记技术(HyT)的CDK9-cyclin T1复合物降解剂(DC50值分别为cyclin T1的589 nM和CDK9的662 nM)。它由CDK9抑制剂SNS 032和一个糖基连接器连接到疏水标记组成。LL-K9-3不会降解其他CDKs(CDK1、2、4、5、6和7)。在22RV1细胞中,LL-K9-3通过诱导CDK9和cyclin T1的选择性和同步降解,降低雄激素受体(AR)和cMyc的表达。 | |||
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。 | |||
T72951 |
CDK4/6-IN-14
|
||
CDK4/6-IN-14 是一种有效且高度选择性的 CDK4和 CDK6(CDK) 抑制剂,IC50分别为 10 nM 和 16 nM。CDK4/6-IN-14 的选择性是 CDK1、2、7 和 9 的 60 多倍,并且在其他 205 种激酶中表现出高选择性。 | |||
T35696 |
Olomoucine II
|
||
Olomoucine II is an inhibitor of cyclin-dependent kinases (CDKs; IC50s = 7.6, 0.1, 19.8, 0.45, and 0.06 μM for Cdk1, -2, -4, -7, and -9, respectively).1It is selective for CDKs over 10 additional kinases (IC50s = >100 μM for all) but does inhibit ERK2 (IC50= 32 μM) and the ATP-binding cassette transporter B1 (ABCB1; IC50= 6.4 μM).1,2Olomoucine II inhibits proliferation of a variety of cancer cells, including those expressing wild-type p53 or mutant p53 (mean IC50s = 7.4 and 10.1 μM, respectively... |