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Results for "

retinoblastoma protein

" in MedChemExpress (MCE) Product Catalog:

24

Inhibitors & Agonists

1

Natural
Products

1

Recombinant Proteins

14

Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-124379
    TPCK
    1 Publications Verification

    L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK

    		 Ser/Thr Protease HPV Apoptosis PDK-1 Infection Neurological Disease Inflammation/Immunology Cancer
    TPCK (L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK) is an effective serine protease inhibitor and also a blocker of the PDK1/Akt pathway. TPCK can modify the E7 protein in actively keratinocyte cells. TPCK can induce cellular apoptosis, suppress tumor growth, reduce hypoxic-ischemic brain injury in rat pups, and affect vascular permeability in inflamed rats .
    TPCK
  • HY-B1165
    Cyproheptadine (hydrochloride sesquihydrate)
    3 Publications Verification

    		 p38 MAPK Checkpoint Kinase (Chk) Histamine Receptor 5-HT Receptor CDK PARP Apoptosis Cancer
    Cyproheptadine hydrochloride sesquihydrate acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine hydrochloride sesquihydrate mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine hydrochloride sesquihydrate induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine hydrochloride sesquihydrate inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine hydrochloride sesquihydrate can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia .
    Cyproheptadine (hydrochloride sesquihydrate)
  • HY-148214
    CDK2/4/6-IN-2

    		CDK Cancer
    CDK2/4/6-IN-2 is a selective CDK2/4/6 inhibitor with IC50 values <1 μM. CDK2/4/6-IN-2 inhibits cells proliferation and phosphorylation of retinoblastoma protein at Ser807/811 in breast cancer cells. CDK2/4/6-IN-2 can be used for the research of cancer, such as breast cancer .
    CDK2/4/6-IN-2
  • HY-142076
    CDK4/6-IN-15

    		CDK Cancer
    CDK4/6-IN-15 is an orally active and selective CDK4/6 inhibitor. CDK4/6-IN-15 potently inhibits cancer cells growth. CDK4/6-IN-15 arrests cell cycle at G1 phase and suppresses retinoblastoma tumour suppressor protein (Rb) phosphorylation at S780 and E2 factor (E2F)-regulated gene expression .
    CDK4/6-IN-15
  • HY-159805
    CDK2-IN-31

    		CDK Cancer
    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 .
    CDK2-IN-31
  • HY-W089922
    D-erythro-Sphingosine hydrochloride
    4 Publications Verification

    Erythrosphingosine hydrochloride; erythro-C18-Sphingosine hydrochloride; trans-4-Sphingenine hydrochloride

    		 TRP Channel Neurological Disease
    D-erythro-Sphingosine (Erythrosphingosine) hydrochloride is a specific TRPM3 activator. D-erythro-Sphingosine also induces retinoblastoma protein dephosphorylation .
    D-erythro-Sphingosine hydrochloride
  • HY-119715
    AG-012986

    		CDK Apoptosis Inflammation/Immunology Cancer
    AG-012986 is a pan-CDK inhibitor with Ki values of 44 nM (CDK1), 9.2 nM (CDK4), 94 nM (CDK2), and IC50 values of 22 nM (CDK5), 4 nM (CDK9). AG-012986 causes apoptosis of T-cells by targeting upstream kinases in the p38 Mitogen-activated protein kinase (MAPK) pathway and impairing cellular survival. AG-012986 induces cell cycle arrest, retinoblastoma protein hypophosphorylation, and reduces Ki-67 expression. AG-012986 exerts antiproliferative activity in tumor cells, demonstrates antitumor efficacy in human xenograft models, and causes retinal and peripheral neurotoxicity, plus immune cell toxicity. AG-012986 can be used for the research of colon carcinoma, non-small cell lung carcinoma, lung carcinoma, breast carcinoma, ovarian tumor, pancreatic carcinoma, osteosarcoma, lymphoma, leukemia, retinotoxicity .
    AG-012986
  • HY-117737A
    RRD-251

    		Raf Apoptosis Cancer
    RRD-251 is an inhibitor of retinoblastoma tumor suppressor protein (Rb)-Raf-1 interaction, with potent anti-proliferative, anti-angiogenic and anti-tumor activities .
    RRD-251
  • HY-142076A
    CDK4/6-IN-15 hydrochloride

    		CDK Cancer
    CDK4/6-IN-15 hydrochloride is an orally active and selective CDK4/6 inhibitor. CDK4/6-IN-15 hydrochloride potently inhibits cancer cells growth. CDK4/6-IN-15 hydrochloride arrests cell cycle at G1 phase and suppresses retinoblastoma tumour suppressor protein (Rb) phosphorylation at S780 and E2 factor (E2F)-regulated gene expression .
    CDK4/6-IN-15 hydrochloride
  • HY-201330
    GDC-4198

    RGT-419B

    		 CDK Cancer
    GDC-4198 (RGT-419B) is an orally active CDK4/2 inhibitor with desired degrees of selectivity against kinases such as CDK6, CDK9 and GSK3β. GDC-4198 inhibits the activity of cyclin-CDK complexes, blocks phosphorylation of the retinoblastoma protein (pRb), arresting the cell cycle transition from G1 to S phase. GDC-4198 is promising for research of cancers, such as breast cancer (especially hormone receptor-positive, HER2-negative type), lung cancer, and colorectal cancer .
    GDC-4198
  • HY-150641
    CDK-IN-9

    		CDK Apoptosis DNA/RNA Synthesis Molecular Glues Cancer
    CDK-IN-9 (compound 24) is a potent CDK inhibitor, also as a molecular glue inducing an interaction between CDK12 and DDB1, with an IC50 values of 4 nM for CDK2/E. CDK-IN-9 leads to polyubiquitination of cyclin K and its subsequent degradation. CDK-IN-9 induce apoptosis through dephosphorylation of retinoblastoma protein and RNA polymerase II .
    CDK-IN-9
  • HY-121881
    PU3

    		HSP Cancer
    PU3 is an Hsp90 inhibitor that competes with geldanamycin (GM) and others for the conserved ATP/ADP pocket of Hsp90. PU3 also induces degradation of proteins such as Her2 and inhibits breast cancer cell growth by causing retinoblastoma protein hypophosphorylation, G1 arrest, and cell differentiation. PU3 has the potential to be a cancer inhibitor. .
    PU3
  • HY-E70678
    CDK3/CycE1 Recombinant Human Active Protein Kinase

    		CDK Cancer
    CDK3 is a major player driving retinoblastoma (Rb) phosphorylation during the G0/G1 transition and in the early G1 phase of the cell cycle. CDK3 interacts with various transcription factors involved in cell proliferation, differentiation, and transformation driven by the EGFR/Ras signaling pathway. CDK3/CycE1 Recombinant Human Active Protein Kinase is an ortholog of CDK3 .
    CDK3/CycE1 Recombinant Human Active Protein Kinase
  • HY-178112
    CDK2-IN-47

    		CDK Apoptosis Cancer
    CDK2-IN-47 is a potent CDK2 inhibitor with an IC50 of 0.21 μM. CDK2-IN-47 exhibits outstanding anticancer activity against MCF-7, HCT-116, and MGC-803 cell lines. CDK2-IN-47 effectively induces G1 cell cycle arrest, retinoblastoma protein (Rb) dephosphorylation, and significant apoptosis. CDK2-IN-47 can be used for the studies of breast cancer, colorectal cancer and gastric cancer .
    CDK2-IN-47
  • HY-118310
    Xylocydine

    		CDK Cancer
    Xylocydine is an inhibitor of CDK1/2, inhibiting CDK function in various apoptotic processes. Xylocydine specifically blocks CDK1 and CDK2 activity with IC50 of 1.4 nM and 61 nM, respectively. In addition, Xylocydine downregulates phosphorylated nucleolin and retinoblastoma protein levels. .
    Xylocydine
  • HY-120625
    BMS-358233

    		HSP Cancer
    PU3 is a small molecule inhibitor of Hsp90 that competes with geldanamycin for Hsp90. PU3 induces degradation of proteins, including Her2, similar to geldanamycin. PU3 inhibits the growth of breast cancer cells, causing retinoblastoma protein hypophosphorylation, G1 arrest, and differentiation. PU3 represents a novel class of synthetic compounds that bind to Hsp90 and inhibit the proliferation of cancer cells. PU3 could provide a new strategy for the treatment of cancers .
    BMS-358233
  • HY-E70677
    CDK3/CycC Recombinant Human Active Protein Kinase

    		CDK Cancer
    CDK3 is a major player driving retinoblastoma (Rb) phosphorylation during the G0/G1 transition and in the early G1 phase of the cell cycle. CDK3 interacts with various transcription factors involved in cell proliferation, differentiation, and transformation driven by the EGFR/Ras signaling pathway. CDK3/CycC Recombinant Human Active Protein Kinase is an ortholog of CDK3 .
    CDK3/CycC Recombinant Human Active Protein Kinase
  • HY-E70680
    CDK3/CycO Recombinant Human Active Protein Kinase

    		CDK Cancer
    CDK3 is a major player driving retinoblastoma (Rb) phosphorylation during the G0/G1 transition and in the early G1 phase of the cell cycle. CDK3 interacts with various transcription factors involved in cell proliferation, differentiation, and transformation driven by the EGFR/Ras signaling pathway. CDK3/CycO Recombinant Human Active Protein Kinase is an ortholog of CDK3 .
    CDK3/CycO Recombinant Human Active Protein Kinase
  • HY-118447
    RO0505124

    		CDK Survivin Cancer
    RO0505124 is a selective CDK4 inhibitor with an IC50 of 20 nM. RO0505124 reversibly binds the ATP pocket of the kinase. RO0505124 induces G1 phase arrest in cancer cells via reduced retinoblastoma protein (Rb) phosphorylation, blocking S phase progression. RO0505124 exhibits anti-proliferative activity against various cancer cells. RO0505124 delays mitotic entry, induces aberrant mitosis with lagging chromosomes, driving mitotic slippage and formation of multinucleated or micronucleated cells. RO0505124 inhibits G2/M phase accumulation of survivin and borealin. RO0505124 can be used for the research of cancer .
    RO0505124
  • HY-182447
    Contragestazol

    DL111-IT

    		 CDK Apoptosis Endocrinology Cancer
    Contragestazol (DL111-IT) is a non-hormonal antifertility agent. Contragestazol reduces the expression of Cyclin D1 and CDK4, increases the expression of total retinoblastoma protein (pRb), and decreases the level of hyperphosphorylated pRb. Contragestazol induces G0/G1 phase cell cycle arrest. Contragestazol inhibits embryonic development by inducing luteal cell apoptosis and reducing intrauterine polyamine levels. Contragestazol exhibits antitumor activity against prostate cancer, S180 tumor and H22 tumor. Contragestazol shows extremely potent activity in terminating early pregnancy in animals .
    Contragestazol
  • HY-186132
    PROTAC CDK2-pRb degrader-1

    		PROTACs CDK Cancer
    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) .
    PROTAC CDK2-pRb degrader-1
  • HY-E70679
    CDK3/CycE2 Recombinant Human Active Protein Kinase

    		CDK Cancer
    CDK3 is a major player driving retinoblastoma (Rb) phosphorylation during the G0/G1 transition and in the early G1 phase of the cell cycle. CDK3 interacts with various transcription factors involved in cell proliferation, differentiation, and transformation driven by the EGFR/Ras signaling pathway. CDK3/CycE2 Recombinant Human Active Protein Kinase is an ortholog of CDK3 .
    CDK3/CycE2 Recombinant Human Active Protein Kinase
  • HY-179633
    ZLMT-72

    		CDK Apoptosis DNA/RNA Synthesis Bcl-2 Family IAP Cancer
    ZLMT-72 is an orally active dual CDK2 and CDK9 inhibitor with IC50s of 0.741 nM and 1.03 nM, respectively. ZLMT-72 shows good selectivity in kinase profiling andcholinesterase inhibition activity. ZLMT-72 has strong antiproliferative effects in the colorectal cancer (CRC) cell line HCT116 (GI50 < 0.1 nM). ZLMT-72 induces apoptosis by inhibiting thephosphorylation of retinoblastoma and RNA polymerase II, resulting in downregulation of antiapoptotic proteins (Mcl-1 and XIAP). ZLMT-72 can be used for the study of colorectal cancer (CRC) .
    ZLMT-72
  • HY-182470
    AG-012986 dihydrochloride

    		CDK
    AG-012986 (dihydrochloride) is a pan-CDK inhibitor with Ki values of 44 nM (CDK1), 9.2 nM (CDK4), 94 nM (CDK2), and IC50 values of 22 nM (CDK5), 4 nM (CDK9). AG-012986 (dihydrochloride) causes apoptosis of T-cells by targeting upstream kinases in the p38 Mitogen-activated protein kinase (MAPK) pathway and impairing cellular survival. AG-012986 (dihydrochloride) induces cell cycle arrest, retinoblastoma protein hypophosphorylation, and reduces Ki-67 expression. AG-012986 (dihydrochloride) exerts antiproliferative activity in tumor cells, demonstrates antitumor efficacy in human xenograft models, and causes retinal and peripheral neurotoxicity, plus immune cell toxicity. AG-012986 (dihydrochloride) can be used for the research of colon carcinoma, non-small cell lung carcinoma, lung carcinoma, breast carcinoma, ovarian tumor, pancreatic carcinoma, osteosarcoma, lymphoma, leukemia, retinotoxicity .
    AG-012986 dihydrochloride

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