目录号 | 产品详情 | 靶点 | |
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TQ0060 | Apoptosis CDK | ||
LY2857785 是 I 型可逆的 ATP 竞争性 CDK9、CDK8和 CDK7抑制剂,IC50分别为 11 nM、16 nM 和 246 nM。 | |||
T5358 | ERK Casein Kinase CDK | ||
Longdaysin 是一种 CK1α 和 CK1δ 的抑制剂,IC50为5.6和8.8 µM。它还抑制ERK2,IC50值为52 µM。它是Wnt/β-catenin 信号通路的抑制剂,通过阻断CK1δ/ε依赖性 Wnt 信号通路发挥抗肿瘤作用。 | |||
T2356 | Apoptosis ERK SGK PKA CDK PKC | ||
Ro 3306 是一种选择性 ATP 竞争性CDK1抑制剂,对 CDK1、CDK1/cyclin B1 和 CDK2/cyclin E 的Ki 值为分别为 20 nM、35 nM 和 340 nM。 | |||
T64373 | CDK | ||
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。 | |||
T60619 | CDK | ||
CDK9-IN-15 是一种有效的小分子CDK9抑制剂,可通过降解、抑制 CDK9 来阻断正性转录延长因子 P-TEFb (positive transcription elongation factor b) 对 RNA Poly-II C末端区域的磷酸化,抑制转录,迅速降低细胞内 mRNA 水平,从而引起肿瘤细胞凋亡。 | |||
T9632 | HIV Protease | ||
CDK9-IN-30 是 Tat 肽衍生物之一,可抑制 HIV-1 长末端重复激活转录。 | |||
T72048 | GSK-3 CDK | ||
CDK8-IN-12 是一种具有选择性、有效性和口服活性的 CDK8 抑制剂(Ki : 14 nM),是一种抗癌剂。CDK8-IN-12 对 GSK-3α、GSK-3β、PCK-θ 具有抑制作用,Ki 分别为 13 nM、4 nM、109 nM。CDK8-IN-12对 MV4-11 细胞显示出抗增殖活性。 | |||
T40353 | |||
CDK7/9-IN-1 is a specific inhibitor of cyclin-dependent kinases 7/9 (CDK7/9). It specifically targets CDK7, while also displaying inhibitory activity against CDK9. CDK7/9-IN-1 demonstrates excellent inhibitory potency against CDK7, with IC50 values of 0.0656 μM and 0.00574 μM without pre-incubation and after 3 hours pre-incubation, respectively. Furthermore, CDK7/9-IN-1 inhibits CDK9 with an IC50 of 2.14 μM after 3 hours pre-incubation. Its application in cancer research makes it valuable for such investigations. | |||
T16359 | CDK Aurora Kinase | ||
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。 | |||
T17069 | CDK PROTACs | ||
THAL-SNS-032 是一种选择性 CDK 降解剂,由 CereblonE3 连接酶 (CRBN) 的配体 thalidomide 衍生物、CDK 配体 SNS-032和 linker 组成的 PROTAC 连接体。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-04548 | CDK4 Protein, Human, Recombinant (GST) | Human | Baculovirus Insect Cells | ||
CDK4 is a member of the Ser/Thr protein kinase family. It is highly similar to the gene products of S. cerevisiae cdc28 and S. pombe cdc2. It is a catalytic subunit of the protein kinase complex that is important for cell cycle G1 phase progression. The activity of CDK4 is restricted to the G1-S phase, which is controlled by the regulatory subunits D-type cyclins and CDK inhibitor p16(INK4a). CDK4 was shown to be responsible for the phosphorylation of retinoblastoma gene product. CDK4 is the ser/Thr-kinase component of cyclin D-CDK4 (DC) complexes that phosphorylate and inhibit members of the retinoblastoma (RB) protein family including RB1 and regulate the cell-cycle during G(1)/S transition. Phosphorylation of RB1 allows dissociation of the transcription factor E2F from the RB/E2F complexes and the subsequent transcription of E2F target genes which are responsible for the progression through the G(1) phase. Hypophosphorylates RB1 in early G(1) phase. Cyclin D-CDK4 complexes are major integrators of various mitogenenic and antimitogenic signals. CDK4 has been shown to be mutated in some types of cancer, whilst a chromosomal rearrangement can lead to Cdk6 overexpression in lymphoma, leukemia and melanoma.Cancer ImmunotherapyImmune CheckpointImmunotherapyTargeted Therapy
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TMPY-04450 | CDK1 & CCNE1 Heterodimer Protein, Human, Recombinant (His & GST) | Human | Baculovirus Insect Cells | ||
CDK1 & CCNE1 Heterodimer Protein, Human, Recombinant (His & GST) is expressed in Baculovirus insect cells with His and GST tag. The predicted molecular weight is 109.7 kDa and the accession number is NP_001777.1&NP_001229.1.
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TMPH-01173 | CDK7 Protein, Human, Recombinant | Human | E. coli | ||
CDK7 Protein, Human, Recombinant is expressed in E. coli.
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TMPH-01172 | CDK7 Protein, Human, Recombinant (His) | Human | Baculovirus Insect Cells | ||
CDK7 Protein, Human, Recombinant (His) is expressed in Baculovirus.
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TMPH-03456 | CAK1 Protein, S. cerevisiae, Recombinant (His & Myc) | Saccharomyces cerevisiae | Baculovirus Insect Cells | ||
CAK1 Protein, S. cerevisiae, Recombinant (His & Myc) is expressed in Baculovirus insect cells with N-10xHis and C-Myc tag. The predicted molecular weight is 46.1 kDa and the accession number is P43568.
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TMPH-03457 | CAK1 Protein, S. cerevisiae, Recombinant (E. coli, His & Myc) | Saccharomyces cerevisiae | E. coli | ||
CAK1 Protein, S. cerevisiae, Recombinant (E. coli, His & Myc) is expressed in E. coli expression system with N-10xHis and C-Myc tag. The predicted molecular weight is 49.6 kDa and the accession number is P43568.
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TMPY-04542 | CDK2 Protein, Human, Recombinant (His) | Human | Baculovirus Insect Cells | ||
CDK2 is a member of the Ser/Thr protein kinase family. This protein kinase is highly similar to the gene products of S. cerevisiae cdc28, and S. pombe cdc2. It is a catalytic subunit of the cyclin-dependent protein kinase complex, whose activity is restricted to the G1-S phase, and essential for cell cycle G1/S phase transition. Cdks (cyclin-dependent kinases) are heteromeric serine/threonine kinases that control progression through the cell cycle in concert with their regulatory subunits, the cyclins. Cdks are constitutively expressed and are regulated by several kinases and phosphastases, including Wee1, CDK-activating kinase and Cdc25 phosphatase. Although there are 12 different cdk genes, only 5 have been shown to directly drive the cell cycle (Cdk1, -2, -3, -4, and -6). Following extracellular mitogenic stimuli, cyclin D gene expression is upregulated. Cdk4 forms a complex with cyclin D and phosphorylates Rb protein, leading to liberation of the transcription factor E2F. E2F induces transcription of genes including cyclins A and E, DNA polymerase and thymidine kinase. Cdk4-cyclin E complexes form and initiate G1/S transition. Subsequently, Cdk1-cyclin B complexes form and induce G2/M phase transition. Cdk1-cyclin B activation induces the breakdown of the nuclear envelope and the initiation of mitosis. CDK2 associates with and regulated by the regulatory subunits of the complex including cyclin A or E, CDK inhibitor p21Cip1 (CDKN1A) and p27Kip1 (CDKN1B). Its activity is also regulated by its protein phosphorylation. CDK2 is involved in the control of the cell cycle. It also interacts with cyclins A, B1, B3, D, or E. Activity of CDK2 is maximal during S phase and G2.
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TMPH-01171 | CDK5 Protein, Human, Recombinant | Human | E. coli | ||
CDK5 Protein, Human, Recombinant is expressed in E. coli.
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TMPH-01169 | CDK4 Protein, Human, Recombinant (His) | Human | E. coli | ||
CDK4 Protein, Human, Recombinant (His) is expressed in E. coli.
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TMPH-01167 | CDK1 Protein, Human, Recombinant (His) | Human | E. coli | ||
CDK1 Protein, Human, Recombinant (His) is expressed in E. coli.
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TMPY-04556 | CDK5 Protein, Human, Recombinant (GST) | Human | Baculovirus Insect Cells | ||
Cell division protein kinase 5, also known as Cyclin-dependent kinase 5, Serine/threonine-protein kinase PSSALRE, Tau protein kinase II catalytic subunit, TPKII catalytic subunit and CDK5, is a cytoplasm protein which belongs to theprotein kinase superfamily, CMGC Ser/Thr protein kinase family and CDC2 / CDKX subfamily. Cyclin-dependent kinases (Cdks) are a family of proline-directed Ser/Thr kinases known for their role in the control of cell cycle progression. In 1992, this family was joined by CDK5, which is an atypical member in that it uses its own activators and is multifunctional, playing important regulatory roles in multiple cellular functions. CDK5, unlike other Cdks, is not regulated by cyclins, and its activity is primarily detected in postmitotic neurons in developing and adult nervous systems. CDK5 is activated by association with a neuron-specific activator, p35 or its isoform p39. CDK5 is probably involved in the control of the cell cycle. It interacts with D1 and D3-type G1 cyclins. CDK5 can phosphorylate histone H1, tau, MAP2 and NF-H and NF-M. It also interacts with p35 which activates the kinase. CDK5 plays important roles in various neuronal activities, including neuronal migration, synaptic activity, and neuronal cell death.
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TMPY-04775 | CDK1 Protein, Mouse, Recombinant (His & GST) | Mouse | Baculovirus Insect Cells | ||
CDK1 Protein, Mouse, Recombinant (His & GST) is expressed in Baculovirus insect cells with His and GST tag. The predicted molecular weight is 61.9 kDa and the accession number is P11440.
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TMPY-04549 | CDK1 Protein, Human, Recombinant (GST) | Human | Baculovirus Insect Cells | ||
CDK1 Protein, Human, Recombinant (GST) is expressed in Baculovirus insect cells with GST tag. The predicted molecular weight is 60 kDa and the accession number is P06493-1.
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TMPH-01170 | CDK5R1 Protein, Human, Recombinant (His) | Human | E. coli | ||
CDK5R1 Protein, Human, Recombinant (His) is expressed in E. coli.
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TMPY-02921 | CDK2AP2 Protein, Human, Recombinant (His) | Human | E. coli | ||
CDK2AP2 belongs to the CDK2AP family. Members of this family of proteins are cell-growth suppressors, associating with and influencing the biological activities of important cell cycle regulators in the S phase including monomeric non-phosphorylated cyclin-dependent kinase 2 (CDK2) and DNA polymerase alpha/primase. CDK2AP2 contains 5 distinct gt-ag introns. Transcription produces 7 different mRNAs, 6 alternatively spliced variants and 1 unspliced form. There are 2 non overlapping alternative last exons and 4 validated alternative polyadenylation sites. The mRNAs appear to differ splicing versus retention of 3 introns. CDK2AP2 plays a role in regulating self-renewal of mouse embryonic stem cells (mESC) under permissive conditions, and cell survival during differentiation of the mESC into terminally differentiated cell types.
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TMPY-04449 | CDK7 & CCNH & MNAT1 Protein, Human, Recombinant (His) | Human | Baculovirus Insect Cells | ||
CDK7 & CCNH & MNAT1 Protein, Human, Recombinant (His) is expressed in Baculovirus insect cells with His tag. The predicted molecular weight is 118.8 kDa and the accession number is P50613&P51946&P51948.
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TMPJ-00963 | CDKN2C Protein, Human, Recombinant (His) | Human | E. coli | ||
Cyclin-Dependent Kinase 4 Inhibitor C (CDKN2C) is a member of the INK4 family of cyclin dependent kinase inhibitors. CDKN2C contains 4 ANK repeats and interacts with CDK4 or CDK6. Highest levels of CDKN2C can be found in skeletal muscle, pancreas, and heart. CDKN2C inhibits cell growth and proliferation with a correlated dependence on endogenous retinoblastoma protein RB and prevent the activation of the CDK kinases. Studies have been shown the roles of CDKN2C gene in regulating spermatogenesis, as well as in suppressing tumorigenesis.
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TMPY-02495 | p19 INK4d Protein, Human, Recombinant (GST) | Human | E. coli | ||
Cyclin-dependent kinase inhibitor 2D(also known as CDKN2D or p19ink4d), a member of the INK4 family of cyclin-dependent kinase (CDK) inhibitors, negatively regulates the cyclin D-CDK4/6 complexes, which promote G1/S transition by phosphorylating the retinoblastoma tumor-suppressor gene product. It is clearly shown that DNA repair is the main target of p19ink4d effect and that diminished apoptosis is a downstream event. Experiments has uncovered a role of p19INK4d as a regulator of DNA-damage-induced apoptosis and suggest that it protects cells from undergoing apoptosis by allowing a more efficient DNA repair. It has been demonstrated that p19INK4d expression enhances cell survival under genotoxic conditions. Previous work has shown that inactivation of the cyclin-dependent kinase inhibitor (CKI) p19(Ink4d) leads to progressive hearing loss attributable to inappropriate DNA replication and subsequent apoptosis of hair cells. It may also involved in male reproductive function including testicular atrophy, alteration in serum follicle stimulating hormone, qualitative increase in germ cell apoptosis, and delayed kinetics of meiotic prophase markers.
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TMPY-02796 | KIAA0101 Protein, Human, Recombinant (His) | Human | E. coli | ||
KIAA11, also known as p15(PAF), is a proliferating cell nuclear antigen-associated factor that interacts with proliferating cell nuclear antigen(PCNA). It was initially isolated in a yeast two-hybrid screen for PCNA binding partners and was shown to bind PCNA competitively with the cell cycle regulator p21(WAF). KIAA11 is localized primarily in the nucleus. It shares the conserved PCNA binding motif with several other PCNA binding proteins including CDK inhibitor p21. KIAA11 is involved in cell proliferation and plays a role in early tumor recurrence (ETR), and prognosis of hepatocellular carcinoma (HCC). KIAA11 is expressed predominantly in the liver, pancreas, and placenta. It cannot be detected in the heart or brain. It is highly expressed in some tumors, especially esophageal tumors, in anaplastic thyroid carcinomas, and non-small-cell lung cancer lines. Overexpression of KIAA11 predicts high stage, early tumor recurrence, and poor prognosis of hepatocellular carcinoma. It also may be involved in the protection of cells from UV-induced cell death.
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TMPJ-00936 | CCND2 Protein, Human, Recombinant (His) | Human | E. coli | ||
CCND2,also known as G1/S-specific cyclin-D2,is a member of the highly conserved cyclin family. Different cyclins exhibit distinct expression and degradation patterns which contribute to the temporal coordination of each mitotic event. Cyclins function as regulators of CDK kinases. This cyclin forms a complex with and functions as a regulatory subunit of CDK4 or CDK6, whose activity is required for cell cycle G1/S transition. CCND2 is involved in a number of fundamental biological processes such as phosphorylating and inhibiting members of the retinoblastoma (RB) protein family including RB1 and regulating the cell-cycle during G1/S transition. It is also substrate for SMAD3, phosphorylating SMAD3 in a cell-cycle-dependent manner and repressing its transcriptional activity. Phosphorylation of RB1 allows dissociation of the transcription factor E2F from the RB/E2F complex and the subsequent transcription of E2F target genes which are responsible for the progression through the G1 phase. Cyclin D-CDK4 complexes are major integrators of various mitogenenic and antimitogenic signals. Component of the ternary complex, cyclin D2/CDK4/CDKN1B, required for nuclear translocation and activity of the cyclin D-CDK4 complex.
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