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lunresertib (RP-6306) is a potent, selective and orally active PKMYT1 inhibitor with an IC50 of 14 nM. lunresertib shows a high degree of selectivity over other kinases in cellular binding assays. lunresertib shows anticancer effects [1].
Cirtociclib (BLU-222) is an orally active and highly selective CDK2 inhibitor. Cirtociclib disrupts Rb signaling and causes G1 arrest and apoptosis in CCNE1-amplified endometrial cancer cells [1] .
CDK2 degrader 7 is an orally active CDK2 degrader, with DC50 values of 13 nM (MKN1cells) and 17 nM (TOV21G cells). CDK2 degrader 7 induces G1 phase arrest in MKN1 cells. CDK2 degrader 7 achieves tumor stasis in HCC1569 (CCNE1-amplified) xenograft models. CDK2 degrader 7 can be used for the study of CCNE1-amplified cancers [1].
CDK2 degrader 3 is a selective CDK2 molecular glue-like degrader. CDK2 degrader 3 induces G1 cell cycle arrest in CCNE1-amplified cancer cells. CDK2 degrader 3 is applicable to breast cancer-related research [1].
CDK2-IN-31 is a CCNE1:CDK2 complex inhibitor with an IC50 of 0.13 μM. CDK2-IN-31 binds to a cryptic allosteric pocket at the CCNE1:CDK2 interface, inducing structural rearrangements of the CDK2 A-loop that disrupt the kinase's active conformation and interfere with substrate binding. CDK2-IN-31 inhibits phosphorylation of retinoblastoma protein 1 (RB1) in CCNE1-dependent ovarian cancer cells. CDK2-IN-31 impairs coenrichment of protein PRC1 with CCNE1-N112C:CDK2 complexes. CDK2-IN-31 can be used for the research of ovarian cancer [1].
CDK2-IN-23 (Compound 17) is a kinase selective and highly potent CDK2 inhibitor (IC50 = 0.29 nM). CDK2-IN-23 shows the pharmacodynamic inhibition of CDK2 in CCNE1-amplified mouse models. CDK2-IN-23 can be used for the research of cancer [1].
CCNE1 Human Pre-designed siRNA Set A contains three designed siRNAs for CCNE1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
PD-166285 is a PKMYT1 inhibitor, with an IC50 value of 17 nM. PD166285 shows strong antiproliferative effects against CCNE1-amplified OVCAR3 cells (IC50= 0.14 μM) and HCC1569 cells (IC50 = 0.21 μM). PD166285 induces apoptosis and arrests CCNE1-amplified HCC1569 cells at the G1/S phase of the cell cycle. PD166285 can be used for the research of PKMYT1-targeted therapies for CCNE1-amplified cancers [1].
Ccne1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Ccne1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Ccne1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Ccne1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
ECI830 (CDK2-IN-37) is an orally active, ATP-competitive and highly selective CDK2 inhibitor. ECI830 shows high selectivity over other CDK family members. ECI830 can be used for the study of HR+/HER2- breast cancer and CCNE1-amplified tumors (such as ovarian cancer and lung cancer) [1].
CDK2 modulator 1 is a CDK2 modulator with an EC50 < 100 nM and an Emax > 100% of positive control in a TR-FRET proximity assay. CDK2 modulator 1 induces ternary complex formation with CDK2/CCNE1 and CRBN. CDK2 modulator 1 can be used for the research of cancer [1].
Anticancer agent 300 (compound P14) is a CCND1, CDK4, CDK6, and CCNE1 modulator, with anti-proliferative, cell-cycle modulatory, senescence-inducing, and apoptosis-inducing activity. Anticancer agent 300 can be used for the research of ER+/HER2− breast cancer and BRAF-mutant melanoma [1].
PKMYT1-IN-13 is a potent, orally active and selective PKMYT1 inhibitor that inhibits PKMYT1 with IC50 values < 10.0 nM in ADP-Glo assay and 19.9 nM in NanoBRET cellular assay. PKMYT1-IN-13 exhibits high selectivity over WEE1. PKMYT1-IN-13 shows selective antiproliferative activity in CCNE1-amplified cells, while showing minimal wild-type effects. PKMYT1-IN-13 shows antitumor efficacy in HCC1569 mouse xenografts. PKMYT1-IN-13 can be used for the research of CCNE1-amplified cancers, such as gastric, ovarian, and breast cancer [1].
EGFR-IN-187 (Compound 4d) is a selective EGFR inhibitor with an IC50 of 25.41 μM. EGFR-IN-187 can cause cancer cells S amd G2/M phase arrest and induce apoptosis and autophagy. EGFR-IN-187 upregulates CCNE1, Bax, LC3B-II and P27 expression and downregulates CCNA1 and Bcl-2 levels. EGFR-IN-187 can be used for the research of cancer, such as lung cancer [1].
CDK2-IN-28 (compound 22) is a CDK2 inhibitor with good selectivity and cellular effects against other CDKs. CDK2-IN-28 has anti-proliferative effects on MKN1 cells (EC50: 0.31 μM) [1].
PROTAC CDK2-pRb degrader-1 is an orally active PROTAC-class degrader of CDK2. PROTAC CDK2-pRb degrader-1 effectively inhibits the phosphorylation of retinoblastoma protein (Rb) at serine residues 807/811 by inducing ubiquitination and proteasomal degradation of CDK2. PROTAC CDK2-pRb degrader-1 exhibits significant activity against human cells (with EC50 values of 12 nM and 125 nM, respectively). In xenograft models, PROTAC CDK2-pRb degrader-1 effectively inhibits tumor growth and induces tumor stasis, making it suitable for research related to CCNE1-amplified cancers (such as ovarian cancer, gastric cancer, and breast cancer) [1].
PKMYT1-IN-12 (Compound 4) is a selective inhibitor of PKMYT1, with an IC₅₀ of 2.6 nM. PKMYT1-IN-12 can effectively inhibit the phosphorylation of CDK1, with an IC₅₀ of 44 nM. PKMYT1-IN-12 is a target protein ligand that can be used for the synthesis of PROTAC D16-M1P2 (HY-180485) [1].
PROTAC D16-M1P2 is an orally active PKMYT1 PROTAC degrader with a DC50 of 0.7 nM. PROTAC D16-M1P2 also inhibits the activity of PKMYT1 with an IC50 of 7.6 nM. PROTAC D16-M1P2 inhibits pCDK1 with an IC50 of 9 nM. PROTAC D16-M1P2 has demonstrated significant anti-tumor efficacy in mouse models and can be used for research on breast cancer [1].
Cyclin E controls the G1/S transition of the cell cycle. Cyclin E Protein, Human (sf9) is the recombinant human-derived Cyclin E, expressed by Sf9 insect cells , with tag Free labeled tag.
The FGF-9 protein undergoes autoproteolysis and cholesterol attachment in the endoplasmic reticulum. It acts as a morphogen during development, inducing ventral cell fate, participating in limb bud patterning, and aiding in axon guidance. FGF-9 binds to the PTCH1 receptor and activates target gene transcription when in association with SMO, while PTCH1 represses SMO signaling in the absence of FGF-9. CDK1-CCNE1 Heterodimer Protein, Human (sf9, His-GST) is a recombinant protein dimer complex containing human-derived CDK1-CCNE1 Heterodimer protein, expressed by Sf9 insect cells , with N-10*His, N-GST labeled tag. CDK1-CCNE1 Heterodimer Protein, Human (sf9, His-GST), has molecular weight of ~109.7 (60.4+49.3) kDa.
Cyclin E controls the G1/S transition of the cell cycle. Cyclin E Protein, Human (SF9, His-GST) is the recombinant human-derived Cyclin E protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag.
Cyclin E, a vital regulator in cell cycle control, governs the G1/S transition by forming a potent serine/threonine kinase complex with CDK2. This complex, featuring UHRF2, CDK2, and CCNE1, involves Cyclin E's direct interaction with UHRF2, leading to CCNE1 ubiquitination independently of phosphorylation. Cyclin E's intricate dance with CDK2, CABLES1, and CCNA1 highlights its crucial role in tightly regulated cell cycle progression. Cyclin E Protein, Mouse (sf9, His-GST) is the recombinant mouse-derived Cyclin E protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag.
CDK3 protein is a serine/threonine protein kinase that plays a key role in regulating the eukaryotic cell cycle, especially affecting the G0-G1 and G1-S transitions. It interacts with CCNC/cyclin-C during interphase and phosphorylates substrates such as histone H1, ATF1, RB1, and CABLES1. CDK3-CCNE1 Heterodimer Protein, Human (sf9) is a recombinant protein dimer complex containing human-derived CDK3-CCNE1 Heterodimer protein, expressed by sf9 insect cells , with tag free.
CDK3 protein is a serine/threonine protein kinase that plays a key role in regulating the eukaryotic cell cycle, especially affecting the G0-G1 and G1-S transitions. It interacts with CCNC/cyclin-C during interphase and phosphorylates substrates such as histone H1, ATF1, RB1, and CABLES1. CDK3-CCNE1 Heterodimer Protein, Human (sf9, GST, FLAG, His) is a recombinant protein dimer complex containing human-derived CDK3-CCNE1 Heterodimer protein, expressed by sf9 insect cells , with N-6*His, N-Flag, N-GST labeled tag.
CDK3 protein is a serine/threonine protein kinase that plays a key role in regulating the eukaryotic cell cycle, especially affecting the G0-G1 and G1-S transitions. It interacts with CCNC/cyclin-C during interphase and phosphorylates substrates such as histone H1, ATF1, RB1, and CABLES1. CDK3-CCNC Protein, Human (Active, sf9, GST, Flag, His) is the recombinant human-derived CDK3-CCNC, expressed by Sf9 insect cells, with N-Flag, N-His, N-GST labeled tag.
CDK3 protein is a serine/threonine protein kinase that plays a key role in regulating the eukaryotic cell cycle, especially affecting the G0-G1 and G1-S transitions. It interacts with CCNC/cyclin-C during interphase and phosphorylates substrates such as histone H1, ATF1, RB1, and CABLES1. CDK3-CCNE2 Protein, Human (sf9, GST, Flag, His) is the recombinant human-derived CDK3-CCNE2, expressed by Sf9 insect cells, with N-His, N-GST, N-Flag labeled tag.
CDK2 is an important serine/threonine protein kinase that plays a critical regulatory role in the cell cycle, especially during meiosis. It phosphorylates various substrates (CTNNB1, USP37, p53/TP53, NPM1, CDK7, RB1, BRCA2, MYC, NPAT, EZH2) and coordinates centrosome duplication and initiation of DNA synthesis at the G1-S transition. CDK2-CCNE1 Protein, Human (sf9, GST, His, Flag) is the recombinant human-derived CDK2-CCNE1, expressed by Sf9 insect cells, with N-His, N-GST, N-Flag labeled tag.
CDK1; cyclin-dependent kinase 1; CDC2, cell division cycle 2, G1 to S and G2 to M; CDC28A; p34 protein kinase; cell cycle controller CDC2; cell division protein kinase 1; cell division control protein 2 homolog; cell division cycle 2, G1 to S and G2 to M; CDC2; P34CDC2; MGC111195; DKFZp686L20222
The CDK1/CDC2-cyclin-B complex is a key regulator in the cell cycle. It plays an important role in cell division and development and regulates a variety of cellular activities, including chromosome segregation, nuclear membrane rupture, cytokinesis, etc. The activity of CDK1 is regulated by a variety of phosphorylation and dephosphorylation, thereby controlling the progression of the cell cycle and the DNA repair process. CDK1-CCNE1 Heterodimer Protein, Human (sf9, GST, His, Flag) is the recombinant human-derived CDK1-CCNE1, expressed by Sf9 insect cells, with N-GST, N-Flag, N-His labeled tag.
CCNE1 Human Pre-designed siRNA Set A contains three designed siRNAs for CCNE1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Ccne1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Ccne1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Ccne1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Ccne1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
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Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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