Cell Cycle

Items 551-600 of 1565

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  1. DYRK1A Inhibitor

    Dyrk1A-IN-15 is a selective, ATP-competitive inhibitor of DYRK1A with an IC50 of 19 nM. This compound demonstrates high selectivity for DYRK kinases and nanomolar potency across various kinase assays. In vitro studies reveal that Dyrk1A-IN-15 disrupts neurosphere self-renewal, inhibits cell invasion, and destabilizes EGFR. Additionally, it shows the ability to inhibit tumor growth and extend survival in vivo, indicating its potential utility in glioblastoma research.
  2. EGFR/CDK-2 Inhibitor

    EGFR/CDK2-IN-1 is an inhibitor targeting both the epidermal growth factor receptor (EGFR) and cyclin-dependent kinase 2 (CDK2). This compound exhibits significant cytotoxicity against breast cancer MCF7 cells and liver cancer HepG2 cells, making it a valuable tool in cancer research. Its dual inhibition profile allows for exploration of synergistic effects in therapeutic strategies targeting these critical pathways in cancer proliferation and survival.
  3. CDK9/PARP Inhibitor

    CDK9/PARP-IN-1 is a potent inhibitor of CDK9 and PARP1, demonstrating IC50 values of 118 nM and 107 nM, respectively. This dual inhibition results in significant antiproliferative effects across various cancer cell lines, making it a valuable tool for cancer research. CDK9/PARP-IN-1 is particularly relevant for studies investigating the therapeutic potential of targeting these pathways in oncology.
  4. PARP1/CDK12 Inhibitor

    Antitumor agent-104 is a potent inhibitor of PARP1 and CDK12, targeting critical pathways in DNA damage repair in tumors. By inhibiting PARP1 enzymatic activity, it effectively reduces PAR protein levels, thus impairing the cellular mechanisms that protect tumor cells. This compound serves as a valuable tool in cancer research, especially in studies focused on understanding tumor biology and exploring novel therapeutic strategies.
  5. CDK-1/PARP-1 Inhibitor

    UNPD139734 is a potent inhibitor of Cyclin-Dependent Kinase 1 (CDK-1) and Poly (ADP-ribose) polymerase 1 (PARP-1), forming stable complexes with both target proteins. This compound serves as a valuable lead for the structural optimization of dual-target anticancer agents, particularly in the context of breast cancer research. Its dual inhibition mechanism offers a promising avenue for investigating novel therapeutic strategies in oncology.
  6. ROCK/NET Inhibitor

    Netarsudil hydrochloride is a selective inhibitor of Rho-associated protein kinases (ROCK I and ROCK II) and a reversible inhibitor of the norepinephrine transporter (NET). It effectively lowers intraocular pressure by promoting relaxation of trabecular meshwork cells and dilation of episcleral veins, enhancing aqueous humor outflow while simultaneously reducing its production. This compound is primarily utilized in research related to ocular hypertension and primary open-angle glaucoma.
  7. CDK9-cyclin T1 Degrader

    LL-K9-3 is a small-molecule degrader specifically targeting the CDK9-cyclin T1 complex. This compound exhibits significant anti-proliferative and pro-apoptotic activities, effectively inhibiting downstream signaling pathways associated with CDK9 and androgen receptor (AR). LL-K9-3 is particularly relevant for research involving oncogenic transcriptional programs driven by AR and Myc, making it a valuable tool in cancer studies.
  8. Nur77 Modulator

    Nur77 Modulator 1 is an effective modulator of Nur77, characterized by a binding affinity of KD = 3.58 μM. This compound up-regulates Nur77 expression and influences its sub-cellular localization, leading to Nur77-dependent endoplasmic reticulum (ER) stress and autophagy, ultimately promoting apoptotic processes in cells. Its notable anti-hepatoma activity makes it a valuable tool for research in cancer biology and cellular stress responses.
  9. Chk-α Inhibitor

    V-11-0711 is a potent and selective inhibitor of Chk-α, exhibiting an IC50 value of 20 nM. This compound effectively reduces phosphocholine (PCho) levels and induces reversible growth arrest in various cancer cell lines. At elevated concentrations, V-11-0711 can promote apoptosis. It is particularly useful for research related to cervical cancer and triple-negative breast cancer, facilitating the exploration of therapeutic strategies targeting Chk-α pathways.
  10. CDK6/PIM1 Inhibitor

    CDK6/PIM1-IN-1 hydrochloride is a potent dual inhibitor targeting CDK6 and PIM1, exhibiting IC50 values of 39 nM and 88 nM, respectively, along with significant inhibition of CDK4 (IC50=3.6 nM). This compound effectively inhibits the proliferation of acute myeloid leukemia (AML) cells, induces G1 phase cell cycle arrest, and promotes apoptosis. CDK6/PIM1-IN-1 hydrochloride is a valuable tool for research investigating the role of CDK6 and PIM1 in cancer biology, particularly in the context of AML.
  11. Wee1 Inhibitor

    WEE1-IN-7 is a selective Wee1 inhibitor with an IC50 value of 2.1 nM. This compound induces apoptosis and facilitates cell cycle arrest during the S phase, making it valuable in the study of tumor biology. WEE1-IN-7 demonstrates significant antitumor activity, providing a useful tool for cancer research and therapeutic development.
  12. PLK1 Inhibitor

    Volasertib trihydrochloride is a potent, ATP-competitive inhibitor of Polo-like kinase 1 (PLK1) with an IC50 of 0.87 nM. This compound also exhibits inhibitory activity against PLK2 and PLK3 with IC50s of 5 nM and 56 nM, respectively. Volasertib trihydrochloride induces mitotic arrest and apoptosis in cancer cells, demonstrating significant antitumor efficacy across various cancer models. It is a valuable tool for research focused on cell division and the development of cancer therapeutics.
  13. CDK1/Cyc B Inhibitor

    CDK1/Cyc B-IN-1 is a selective inhibitor of the CDK1/cyclin B complex, demonstrating an IC50 of 97 nM. This compound effectively induces apoptosis and facilitates G2/M phase cell cycle arrest, making it a valuable tool for studying cell proliferation. CDK1/Cyc B-IN-1 exhibits broad-spectrum cytotoxic activity against various cancer cell lines, supporting its potential in cancer research applications.
  14. CDK/CRK Inhibitor

    RGB-286147 is a selective ATP-competitive inhibitor of cyclin-dependent kinases (CDKs) and CDK-related kinases (CRKs), exhibiting IC50 values between 9 to 839 nM. This compound demonstrates minimal activity against non-CDK/CRK kinases. RGB-286147 induces apoptosis in cancer cells and shows significant anti-tumor effects, making it a valuable tool for research in cancer biology and therapeutic development targeting CDK pathways.
  15. CDK4/6 Degrader

    LA-CB1 is a CDK4/6 degrader that promotes the degradation of cyclin-dependent kinases 4 and 6 through the ubiquitin-proteasome pathway. This action disrupts the CDK4/6-Cyclin D1-Rb-E2F signaling axis, leading to G0/G1 cell cycle arrest and apoptosis. LA-CB1 demonstrates potent anti-proliferative effects against MDA-MB-231 cells, with an IC50 of 0.27 µM, and effectively inhibits epithelial-mesenchymal transition, cell migration, invasion, and angiogenesis. In models of triple-negative breast cancer, LA-CB1 significantly inhibits tumor growth in a dose-dependent manner, making it a valuable compound for research in breast cancer therapeutics.
  16. CHK1 Inhibitor

    Prexasertib Mesylate Hydrate is a selective, ATP-competitive inhibitor of checkpoint kinase 1 (CHK1) with a Ki of 0.9 nM and an IC50 of <1 nM. It also inhibits checkpoint kinase 2 (CHK2) with an IC50 of 8 nM and ribosomal S6 kinase 1 (RSK1) with an IC50 of 9 nM. By inducing double-stranded DNA breakage and replication catastrophe, Prexasertib Mesylate Hydrate promotes apoptotic cell death, exhibiting significant anti-tumor activity. This reagent is primarily utilized in cancer research to explore mechanisms of DNA damage response and therapeutic resistance.
  17. c-MYC Inhibitor

    IZTZ-1 is an imidazole-benzothiazole conjugate that functions as a c-MYC inhibitor by stabilizing the G-quadruplex (G4) structure of c-MYC. This stabilization results in the downregulation of c-MYC expression, leading to induction of cell cycle arrest and apoptosis in various cell lines, including B16 melanoma cells. Due to its ability to inhibit cell proliferation and exhibit antitumor activity, IZTZ-1 is a valuable tool for researchers studying melanoma and related cancer pathways.
  18. ROCK Inhibitor

    PT-262 is a selective ROCK inhibitor with an IC50 of approximately 5 μM. This compound induces loss of mitochondrial membrane potential and enhances caspase-3 activation, leading to apoptosis. PT-262 also inhibits phosphorylation of ERK and CDC2 through a p53-independent mechanism, disrupts cytoskeletal dynamics, and impairs cell migration. Its efficacy in promoting anti-cancer activity makes PT-262 a valuable reagent for cancer research.
  19. Aurora kinase Inhibitor

    Aurora kinase-IN-8 is an orally active inhibitor of Aurora kinases, specifically targeting Aurora A and B kinases with IC50 values of 2.8 nM and 28.1 nM, respectively. This compound effectively disrupts spindle formation, induces G2/M phase arrest, and promotes apoptosis in cancer cells. It is particularly relevant for research applications focused on malignancies, including triple-negative breast cancer.
  20. CDK6/PIM1 Inhibitor

    CDK6/PIM1-IN-1 is a potent dual inhibitor targeting CDK6 and PIM1, with IC50 values of 39 nM and 88 nM, respectively, and an additional inhibition of CDK4 at an IC50 of 3.6 nM. This reagent significantly inhibits the proliferation of acute myeloid leukemia (AML) cells, induces G1 phase cell cycle arrest, and promotes apoptosis. CDK6/PIM1-IN-1 demonstrates strong anti-AML activity, making it a valuable tool for research in cancer biology and therapeutic development.
  21. CDK Inhibitor

    1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC is a cyclin-dependent kinase (CDK) inhibitor that plays a crucial role in cancer research. This compound induces apoptosis and effectively inhibits the proliferation of a variety of cancer cell lines, making it a valuable tool for studying cancer biology and therapeutic responses. Its ability to impact CDK activity provides insights into cell cycle regulation and potential cancer treatment strategies.
  22. Aurora A Kinase Inhibitor

    Alisertib sodium is a selective inhibitor of Aurora A kinase, exhibiting an IC50 of 1.2 nM. This compound disrupts mitotic spindle formation and leads to mitotic accumulation, thereby inducing apoptosis and autophagy in leukemic cells via the AKT/mTOR/AMPK/p38 signaling pathway. Alisertib sodium demonstrates significant antitumor activity, making it a valuable reagent for cancer research and therapeutic applications.
  23. CHK1 Inhibitor

    Prexasertib mesylate is a selective ATP-competitive inhibitor of checkpoint kinase 1 (CHK1), demonstrating a Ki of 0.9 nM and an IC50 of less than 1 nM. It also inhibits CHK2 and RSK1 with IC50 values of 8 nM and 9 nM, respectively. By inducing double-stranded DNA breaks and triggering replication catastrophe, Prexasertib mesylate leads to apoptosis. Its potent anti-tumor activity makes it valuable for cancer research applications, particularly in studies focusing on DNA damage response and cell cycle regulation.
  24. Selective ROCK Inhibitor

    Y-27632 hydrochloride hydrate is a selective inhibitor of Rho-associated protein kinases (ROCK-I and ROCK-II), exhibiting ATP-competitive activity with IC50 values of 220 nM and 300 nM, respectively. This compound has been shown to reduce Doxorubicin-induced apoptosis in human cardiac stem cells and suppress apoptosis in dissociation-induced murine prostate stem/progenitor cells. Additionally, Y-27632 hydrochloride hydrate enhances the differentiation of human induced pluripotent stem cells (hIPSCs) towards a mesendodermal lineage by modulating epithelial-mesenchymal transition.
  25. HDAC1/2 and CDK2 Inhibitor

    HDAC1/2 and CDK2-IN-1 is a dual inhibitor targeting HDAC1, HDAC2, and CDK2, with IC50 values of 70.7 μM, 23.1 μM, and 0.80 μM, respectively. This compound effectively disrupts the cell cycle and promotes apoptosis in tumor cells, demonstrating significant in vivo antitumor activity. It is suitable for research applications focused on cancer biology and therapeutic interventions targeting histone deacetylases and cyclin-dependent kinases.
  26. CDK2/9 Inhibitor

    ZLMT-12 is a potent CDK2/9 inhibitor, demonstrating IC50 values of 0.002 μM and 0.011 μM against CDK9 and CDK2, respectively. This compound is derived from tacrine and exhibits weak inhibition of acetylcholinesterase (IC50 = 19.023 μM) and butyrylcholinesterase (IC50 = 2.768 μM). ZLMT-12 is characterized by low toxicity and notable antiproliferative activity, effectively inducing apoptosis and facilitating cell cycle arrest in the S and G2/M phases. This compound serves as a valuable tool for research in cell cycle regulation and therapeutic development in cancer biology.
  27. Aurora B Inhibitor

    Barasertib dihydrochloride is a selective inhibitor of Aurora B kinase, exhibiting an IC50 of 0.37 nM in cell-free assays. This compound effectively induces growth arrest and apoptosis in various cancer cell lines, making it a valuable tool for cancer research. Its mechanism of action provides insights into the role of Aurora B in cell cycle regulation and tumorigenesis.
  28. Aurora/JAK Inhibitor

    AT9283 lactic acid is a multi-targeted kinase inhibitor primarily targeting Aurora A/B and JAK2/3. It demonstrates potent biological activity against various cancers, exhibiting IC50 values between 1 to 30 nM for its targets. AT9283 lactic acid effectively inhibits the growth and survival of multiple solid tumors in both in vitro and in vivo models, making it a valuable reagent for cancer research applications.
  29. CDK7 Inhibitor

    CDK7-IN-30 is a potent CDK7 inhibitor with an IC50 value of 7.21 nM, targeting the phosphorylation of RNA Polymerase II and CDK2. This compound demonstrates significant pro-apoptotic effects and exhibits anti-cancer activity, making it a valuable tool for cancer research. Its mechanism of action offers insights into cell cycle regulation and transcriptomic processes, facilitating the exploration of therapeutic strategies in oncology.
  30. CDK9 Inhibitor

    A-1592668 is a selective inhibitor of cyclin-dependent kinase 9 (CDK9), which plays a critical role in transcriptional regulation. This compound induces apoptosis in various cancer cell lines and demonstrates synergistic effects when combined with Venetoclax, effectively inhibiting the growth of Jeko-1 tumors. A-1592668 is a valuable tool for research in cancer biology and therapeutic development targeting CDK9 pathways.
  31. CDK6/BRD4 Inhibitor

    BC13 is a selective inhibitor of CDK6 and BRD4, demonstrating IC50 values of 234 nM and 36 nM, respectively. This compound exhibits notable antiproliferative effects, facilitating cell apoptosis and inducing DNA damage in various cell lines. Additionally, BC13 has been shown to elevate reactive oxygen species (ROS) levels, making it a valuable tool for research in cancer biology and therapeutic development targeting cell cycle regulation.
  32. Aurora A/Aurora B/HDAC1/HDAC2 Inhibitor

    Aurora kinase/HDAC-IN-1 is a potent dual inhibitor targeting Aurora A, Aurora B, HDAC1, and HDAC2. This compound promotes histone H3 acetylation, inhibits Aurora A phosphorylation and downstream signaling, and induces apoptosis through G2/M cell-cycle arrest. It demonstrates significant antiproliferative activity in colorectal cancer cells, with an IC50 of 30.2 nM in HCT-116 cells, and effectively suppresses tumor growth in HCT-116 colorectal cancer xenograft mouse models. This reagent is valuable for research in cancer biology and therapeutic application development.
  33. HDAC1/CDK7 Inhibitor

    HDAC1/CDK7-IN-1 is a dual inhibitor targeting HDAC1 and CDK7, exhibiting IC50 values of 893 nM and 248 nM, respectively. This compound effectively inhibits the proliferation of cancer cell lines, including MDA-MB-231, MCF-7, A549, and HCT-116. Additionally, HDAC1/CDK7-IN-1 induces cell cycle arrest and apoptosis specifically in HCT-116 cells, while also disrupting their migratory capacity. These properties make it a valuable tool for cancer research, particularly in exploring therapeutic strategies that target epigenetic regulation and cell cycle dynamics.
  34. PLK1 Inhibtor

    PLK1-IN-13 is a selective inhibitor of polo-like kinase 1 (PLK1) with an IC50 of 0.27 nM, exhibiting oral bioavailability. It also demonstrates inhibitory activity against PLK2 and PLK3, with IC50 values of 12.72 nM and 4.12 nM, respectively. PLK1-IN-13 effectively induces G2 phase cell cycle arrest, promotes apoptosis, and down-regulates the c-MYC oncogene, which is associated with tumor proliferation. This compound is particularly relevant for research on acute myeloid leukemia (AML) and other cancer models.
  35. PLK1 Inhibitor

    PLK1-IN-15 is a potent inhibitor of Polo-like Kinase 1 (PLK1) with an IC50 of 38.5 nM. It demonstrates significant antiproliferative effects in various cancer cell lines, including HepG2, Huh7, H1299, and A549, with IC50 values of 2.03, 2.08, 4.79, and 17.11 μM, respectively. PLK1-IN-15 is known to induce cell cycle arrest at the G2/M phase and trigger apoptosis, underscoring its potential as an effective agent in cancer research and therapeutic development.
  36. CDK Inhibitor

    5,6-Dichlorobenzimidazole riboside (DRB) functions as a selective inhibitor of several carboxyl-terminal domain kinases, notably casein kinase II and cell cycle-dependent kinases (CDKs). This nucleoside analog exhibits antitumor activity and has been shown to induce apoptosis in targeted cancer cells. Its role in modulating kinase activity makes DRB valuable for research in cancer biology and cell cycle regulation.
  37. CDK9 Inhibitor

    Enitociclib is a highly selective CDK9 inhibitor, with an IC50 value of 3 nM, that disrupts transcriptional elongation by inhibiting Ser2/Ser5 phosphorylation of RNA polymerase II. This compound specifically targets and depletes short-lived oncogenic proteins such as c-MYC and MCL-1, thereby inducing apoptosis in tumor cells. Enitociclib also impairs enhancer RNA production and enhancer-promoter interactions, leading to downregulation of oncogene expression at the epigenetic level. Its efficacy is demonstrated through synergistic interactions with agents like Bortezomib, Lenalidomide, Pomalidomide, Venetoclax, and Paclitaxel, providing a valuable research tool for studying malignancies such as double-hit diffuse large B-cell lymphoma, multiple myeloma, and pancreatic ductal adenocarcinoma.
  38. PLK2 Inhibitor

    ON1231320 is a selective inhibitor of polo-like kinase 2 (PLK2), exhibiting an IC50 of 0.31 μM. This compound disrupts tumor cell cycle progression specifically at the G2/M phase during mitosis, leading to apoptotic cell death. The arylsulfonyl pyrido-pyrimidinone structure contributes to its significant antitumor activity, making ON1231320 a valuable tool for research in cancer biology and therapeutic development.
  39. BRCA2-RAD51 Interaction Inhibitor

    CAM833 is a potent orthosteric inhibitor of the BRCA2-RAD51 interaction, exhibiting a Kd of 366 nM against ChimRAD51 protein. This compound also disrupts RAD51 oligomerization, leading to enhanced progression of G2/M-arrested cells into apoptosis. CAM833 is valuable for research applications aimed at studying DNA repair mechanisms and therapeutic strategies in BRCA2-related cancers.
  40. CDK Inhibitor

    Borrelidin is a CDK inhibitor that acts by targeting threonyl-tRNA synthetase, isolating from the bacterium Streptomyces rochei. This compound demonstrates potent angiogenesis inhibition with an IC50 of 0.8 nM and induces apoptosis in endothelial tube-forming cells. Additionally, Borrelidin possesses significant antimalarial activity, exhibiting IC50 values of 1.9 nM and 1.8 nM against the K1 and FCR3 strains of Plasmodium falciparum, respectively. These properties make Borrelidin a valuable tool for research in cancer and malaria biology.
  41. CDK9 Inhibitor

    NSC 107512 is a potent inhibitor of cyclin-dependent kinase 9 (CDK9). As a member of the sangivamycin-like molecule class, it demonstrates significant biological activity by inhibiting cellular growth and inducing apoptosis in multiple myeloma tumors. This compound is valuable for research applications focused on cancer biology and the exploration of therapeutic strategies targeting CDK9-mediated pathways.
  42. CDK9 Inhibitor

    AZ5576 is a potent and highly selective inhibitor of cyclin-dependent kinase 9 (CDK9), with an IC50 value of less than 5 nM. This compound effectively inhibits the phosphorylation of RNA polymerase II at Ser2, leading to a reduction in transcriptional elongation. AZ5576 is applicable in the research of hematological malignancies, aiding in the understanding of transcription regulation in cancer biology.
  43. CDK1 Inhibitor

    Avotaciclib is an orally active inhibitor of cyclin-dependent kinase 1 (CDK1). It effectively inhibits tumor cell proliferation and induces apoptosis, making it a valuable compound for cancer research. This reagent is particularly relevant in the study of cancers, including pancreatic and lung cancer, where CDK1 plays a critical role in cell cycle regulation and tumor growth.
  44. DYRKs/CLKs Inhibitor

    Leucettine L41 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs) and CDC-like kinases (CLKs). This compound also modulates GSK-3 signaling, demonstrating significant effects on cellular processes by inhibiting apoptosis and reducing reactive oxygen species (ROS) production. Leucettine L41 promotes cell cycle progression and proliferation in β-cells, enhancing insulin secretion. It is a valuable tool for research focused on neurological disorders, including Alzheimer’s disease, and metabolic diseases such as diabetes.
  45. CHK1 Inhibitor

    Prexasertib dimesylate is a selective checkpoint kinase 1 (CHK1) inhibitor that functions as an ATP-competitive agent. With a Ki of 0.9 nM and an IC50 of less than 1 nM, it effectively inhibits CHK2 and RSK1, exhibiting IC50 values of 8 nM and 9 nM, respectively. This compound induces double-stranded DNA breaks and replication catastrophe, leading to apoptosis. Prexasertib dimesylate demonstrates significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic development.
  46. Cyclins/Cdk Inhibitor

    Aminopurvalanol A is a selective inhibitor of Cyclins/Cdk complexes, primarily targeting the G2/M-phase transition. This compound effectively inhibits cancer cell differentiation and proliferation, making it a valuable tool for cancer research. Additionally, Aminopurvalanol A has been shown to disrupt sperm fertilizing ability by inhibiting capacitation-dependent actin polymerization, highlighting its potential in reproductive biology studies.
  47. CDK9 Inhibitor

    (-)-Enitociclib is a selective inhibitor of cyclin-dependent kinase 9 (CDK9), with demonstrated capacity to induce apoptosis in various cancer cell lines. By inhibiting CDK9, it effectively reduces phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase II, leading to downregulation of critical oncogenes such as MYC and MCL1. This compound exhibits significant anti-proliferative effects against MYC-positive lymphoma and multiple myeloma cells, and shows synergistic potential when combined with therapies such as Bortezomib and Lenalidomide, making it a valuable tool in hematological cancer research.
  48. CDK4/6 PROTAC Degrader

    PROTAC CDK4/6 degrader 1 is a dual-targeted degrader designed to selectively degrade cyclin-dependent kinases CDK4 and CDK6. With DC50 values of 10.5 nM and 2.5 nM, this compound effectively inhibits cell proliferation in Jurkat cells, demonstrating an IC50 of 0.18 μM. The compound promotes G1 phase cell cycle arrest and triggers apoptosis, making it a valuable tool for studying cancer biology and potential therapeutic applications in CDK-related malignancies.
  49. CDK12/CCNK Molecular Glue

    NCT02 is a molecular glue degrader that targets CDK12 through the E3 ubiquitin ligase DDB1, resulting in the ubiquitination and subsequent proteasomal degradation of its partner protein CCNK. This mechanism leads to the downregulation of CDK12, inhibiting its downstream signaling pathways. NCT02 exhibits significant biological activity by inducing apoptosis in tumor cells, arresting the cell cycle, and selectively inhibiting the proliferation of colorectal cancer cells with TP53 mutations or belonging to the CMS4 molecular subtype. Additionally, NCT02 demonstrates potential in suppressing tumor growth in both in vitro and in vivo models.
  50. KRAS Inhibitor

    KRAS inhibitor-9 is a selective inhibitor of the KRAS protein, primarily targeting KRAS G12D, G12C, and Q61H mutations with a moderate binding affinity (Kd=92 μM). This compound effectively disrupts the formation of the GTP-bound active form of KRAS, leading to subsequent inactivation of downstream signaling pathways. Biological assays demonstrate that KRAS inhibitor-9 induces G2/M cell cycle arrest and promotes apoptosis in non-small cell lung cancer (NSCLC) cells harboring KRAS mutations, while sparing normal lung cells. Its application is significant in cancer research, particularly in studying KRAS-driven malignancies.

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