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Results for "

Ser2

" in MedChemExpress (MCE) Product Catalog:

27

Inhibitors & Agonists

4

Peptides

1

Recombinant Proteins

2

Antibodies

1

Oligonucleotides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-103019
    Enitociclib
    2 Publications Verification

    (+)-BAY-1251152; (+)-VIP152; (S)-Enitociclib

    		 Drug Isomer CDK Apoptosis DNA/RNA Synthesis Inflammation/Immunology Cancer
    Enitociclib ((+)-BAY-1251152; (+)-VIP152) is a selective CDK9 inhibitor (IC50=3 nM) that inhibits transcriptional elongation by blocking Ser2/Ser5 phosphorylation of RNA polymerase II. Enitociclib specifically depletes key short-lived proteins such as c-MYC, MCL-1 and induces tumor cell apoptosis. Enitociclib also interferes with the production of enhancer RNAs (eRNA) and enhancer-promoter interactions, and downregulates oncogene expression at the epigenetic level. Enitociclib exerts synergistic effects with agents including Bortezomib (HY-10227), Lenalidomide (HY-A0003), Pomalidomide (HY-10984), Venetoclax (HY-15531) and Paclitaxel (HY-B0015), and even reverses paclitaxel resistance. Enitociclib serves as a vital research tool for various malignancies such as double-hit diffuse large B-cell lymphoma, multiple myeloma and pancreatic ductal adenocarcinoma [2] .
    Enitociclib
  • HY-103019A
    (±)-Enitociclib

    (±)-BAY-1251152; (±)-VIP152

    		 CDK Apoptosis DNA/RNA Synthesis Cancer
    (±)-Enitociclib ((±)-BAY-1251152) is the racemic mixture of Enitociclib (HY-103019E). Enitociclib is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase Pol II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1. Enitociclib has anti-proliferative activity targeting MYC + lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies [2].
    (±)-Enitociclib
  • HY-137478
    KB-0742
    3 Publications Verification

    		 CDK Cancer
    KB-0742 is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 has potent anti-tumor activity [2].
    KB-0742
  • HY-143584
    AZ5576

    		CDK Apoptosis Cancer
    AZ5576 is a potent and highly selective CDK9 inhibitor (IC50: <5 nM). AZ5576 inhibits the phosphorylation of RNA polymerase II at Ser2, thereby inhibiting transcriptional elongation. AZ5576 can be used for hematological Malignancy research [2].
    AZ5576
  • HY-163944
    LL-K12-18

    		DNA/RNA Synthesis Molecular Glues CDK Apoptosis RAD51 ATM/ATR PARP Cancer
    LL-K12-18 is a CDK12 kinase inhibitor and a dual-site molecular glue. LL-K12-18 inhibits human CDK12 with an IC50 value of 283.9 nM, and selectively degrades cyclin K via the ubiquitin-proteasome system by stabilizing the CDK12-DDB1 complex. LL-K12-18 downregulates DNA damage response genes, reduces the phosphorylation level of CTD Ser2 in RNA polymerase II, and modulates biomarkers such as ATM, RAD51, γ-H2AX and cleaved PARP, thereby effectively inducing apoptosis and inhibiting proliferation of breast cancer cells. LL-K12-18 exhibits high target selectivity and serves as a research tool for studies on triple-negative breast cancer [2].
    LL-K12-18
  • HY-112626
    CDK12-IN-2
    1 Publications Verification

    		 CDK Cancer
    CDK12-IN-2 is a potent, selective and nanomolar CDK12 inhibitor (IC50=52 nM) with good physicochemical properties. CDK12-IN-2 is also a strong CDK13 inhibitor due to CDK13 is the closest homologue of CDK12. CDK12-IN-2 shows excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7. CDK12-IN-2 inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II. CDK12-IN-2 can be used an excellent chemical probe for functional studies of CDK12 .
    CDK12-IN-2
  • HY-137478A
    KB-0742 dihydrochloride
    3 Publications Verification

    		 CDK Cancer
    KB-0742 dihydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 dihydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity [2].
    KB-0742 dihydrochloride
  • HY-132941
    CFT-2718

    		PROTACs Epigenetic Reader Domain c-Myc Apoptosis Cancer
    CFT-2718 is a selective CRBN-dependent BRD4 PROTAC degrader. CFT-2718 mediates rapid, selective BRD4 degradation, reduces total and phosphorylated Ser2 RPB1 levels, and reduces MYC protein levels. CFT-2718 can inhibit cancer cells proliferation and induce apoptosis. CFT-2718 reduces growth of lung cancer and pancreatic patient-derived xenograft models. CFT-2718 can be used for the research of cancer, such as small-cell lung cancer and pancreatic cancer .
    CFT-2718
  • HY-103019B
    (-)-Enitociclib
    2 Publications Verification

    (R)-Enitociclib; (-)-BAY-1251152; (-)-VIP152

    		 Drug Isomer CDK Apoptosis DNA/RNA Synthesis Cancer
    (-)-Enitociclib ((R)-Enitociclib) is an enantiomer of Enitociclib (HY-103019E) with an optical rotation of (-). Enitociclib is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase Pol II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1. Enitociclib has anti-proliferative activity targeting MYC + lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies [2].
    (-)-Enitociclib
  • HY-173059
    CDK12/13-IN-3

    		CDK Cancer
    CDK12/13-IN-3 (Compound 12b) is the orally active inhibitor for CDK that inhibits CDK12 and CDK13 with IC50 of 107.4 nM and 79.4 nM. CDK12/13-IN-3 inhibits the phosphorylation of Ser2 on the CTD of RNA polymerase II, induces DNA damage, and downregulates the gene expression of DNA damage response (DDR). CDK12/13-IN-3 exhibits antiproliferative activity against multiple cancer cells with IC50 of nanomolar levels. CDK12/13-IN-3 exhibits antitumor effect in mouse models, exhibits good pharmacokinetic properties with an oral bioavailability of 53.6% .
    CDK12/13-IN-3
  • HY-177780
    Cyclin K degrader 2

    		Molecular Glues CDK Apoptosis Cancer
    Cyclin K degrader 2 is a molecular glucose degrading agent that targets the cyclin K protein. Cyclin K degrader 2 has inhibitory activity against CDK1 and CDK9. Cyclin K degrader 2 causes a decrease in RNA polymerase II Ser2 phosphorylation levels, downregulation of DNA damage response gene expression, accumulation of DNA damage, G1 phase arrest of the cell cycle, and apoptosis. Cyclin K degrader 2 can be used for cancer research .
    Cyclin K degrader 2
  • HY-P10053
    sPLA2-IIA Inhibitor

    		Phospholipase Metabolic Disease
    sPLA2-IIA Inhibitor is a cyclic pentapeptide analog of FLSYK (cyclic 2-Nal-Leu-Ser-2-Nal-Arg (c2)), that binds to hGIIA (human IIA phospholipase A2) and inhibits its hydrolytic ability. sPLA2 is a member of the esterase superfamily that catalyzes the hydrolysis of the ester bond at the sn-2 position of glycerophospholipids, releasing free fatty acids such as arachidonic acid and lysophospholipids .
    sPLA2-IIA Inhibitor
  • HY-P1332
    DSLET

    [D-Ser2, Leu5, Thr6]-enkephalin

    		 Opioid Receptor Neurological Disease
    DSLET ([D-Ser2, Leu5, Thr6]-enkephalin) is a highly specific agonist of the δ-receptor. DSLET is an enkephalin-related peptide selectively bound to the δ opioid receptor [2].
    DSLET
  • HY-176484
    CDK9-IN-39

    		CDK Apoptosis Cancer
    CDK9-IN-39 (1-7a-B1) is an orally active cyclin-dependent kinase 9 (CDK9) inhibitor with an IC50 of 6.51 nM. CDK9-IN-39 induces cell apoptosis by inhibiting the phosphorylation of RNA polymerase II at Ser2 and can be used for study of colorectal cancer .
    CDK9-IN-39
  • HY-177786
    CDK12 ligand-3

    		Molecular Glues CDK Cancer
    CDK12 ligand-3 is a molecular glucose degrading agent that targets the CDK12 protein (DC50 = 35 nM). CDK12 ligand-3 degrades CDK12, CDK13 and their regulatory subunit Cyclin K in a concentration dependent manner, and inhibits RNA polymerase II CTD (Ser2) phosphorylation. CDK12 ligand-3 exhibits potent anti proliferative activity against Jurkat cells. CDK12 ligand-3 can be used for research on cancers such as leukemia .
    CDK12 ligand-3
  • HY-173273
    YJZ5118

    		CDK Apoptosis DNA/RNA Synthesis Akt Cancer
    YJZ5118 is a selective CDK12/CDK13 inhibitor with IC50 values of 39.5 nM and 26.4 nM. YJZ5118 suppresses transcription of DNA damage response genes and induces DNA damage in tumor cells. YJZ5118 inhibits proliferation and triggers apoptosis. YJZ5118 inhibits RNA polymerase II Ser2 phosphorylation and increases Akt pathway activity. YJZ5118 exhibits synergistic effects with Akt inhibitors. YJZ5118 can be used for the research of cancer, such as prostate cancer .
    YJZ5118
  • HY-156296
    CDK9-Cyclin T1 PPI-IN-1

    		CDK Apoptosis Cancer
    CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective CDK9-Cyclin T1 protein-protein interaction (PPI) inhibitor. CDK9-Cyclin T1 PPI-IN-1 inhibits cell proliferation in TNBC MDA-MB-231 cells (IC50: 0.044 μM), and induces apoptosis. CDK9-Cyclin T1 PPI-IN-1 inhibits CDK9 transcription activity, reduces the phosphorylation of RNA Pol II CTD ser2. CDK9-Cyclin T1 PPI-IN-1 inhibits tumor growth in a TNBC 4T1 mouse model .
    CDK9-Cyclin T1 PPI-IN-1
  • HY-162619
    CDK9-IN-33

    		Apoptosis CDK Cancer
    CDK9-IN-33 (compound C35) is a potent, selective and orally active CDK9 inhibitor with IC50 values of 17.44, 160, 316.30, 1771.00, >10000 nM for CDK9, CDK7, CDK2, CDK4, CDK6 respectively. CDK9-IN-33 induces apoptosis. CDK9-IN-33 decreases the protein expression of RPB1 CTD Ser2, RPB1, MCL1. CDK9-IN-33 shows anti-tumor activity .
    CDK9-IN-33
  • HY-P1933A
    [pSer2, pSer5, pSer7]-CTD TFA

    		CDK Cancer
    [pSer2, pSer5, pSer7]-CTD (TFA), a substrate for CDK7 (cyclin dependent protein kinase), is a phosphorylated polypeptide at ser2, ser5 and ser7 sites of RNA polymerase II carboxy-terminal domain (CTD) .
    [pSer2, pSer5, pSer7]-CTD TFA
  • HY-137478B
    KB-0742 hydrochloride

    		CDK Cancer
    KB-0742 hydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 hydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 hydrochloride has potent anti-tumor activity .
    KB-0742 hydrochloride
  • HY-123034
    CDKI-83

    		CDK Bcl-2 Family Apoptosis Cancer
    CDKI-83 is a potent CDK9 and CDK1 inhibitor with Ki values of 21 nM and 72 nM for CDK9/T1 and CDK1/B, respectively. CDKI-83 demonstrates effective anti-proliferative activity in human tumour cell lines with a GI50<1 μM. CDKI-83 effectively induces apoptosis in A2780 human ovarian cancer cells. CDKI-83 reduces phosphorylation at Ser-2 of RNA polymerase II (RNAPII) by inhibiting cellular CDK9 activity, and down-regulates Mcl-1 and Bcl-2. CDKI-83 has the potential for anti-cancer research .
    CDKI-83
  • HY-173481
    CDK9-IN-37

    		CDK Cancer
    CDK9-IN-37 (Compound 24) is a CDK9 inhibitor (EC50: 5.5 nM) with weak inhibition on other CDK isoforms, showing high selectivity. CDK9-IN-37 has significant antiproliferative activity against acute myeloid leukemia MOLM-13 cells (IC50: 0.034 μM). CDK9-IN-37 inhibits the CDK9 signaling pathway, reduces the phosphorylation level of RNAP II CTD (Ser2), downregulates the anti-apoptotic protein McI-1, induces cell apoptosis, and arrests the cell cycle at the G2/M phase. CDK9-IN-37 can be used in the study of acute myeloid leukemia (AML) .
    CDK9-IN-37
  • HY-183710
    CDK9-IN-50

    		CDK Androgen Receptor c-Myc Apoptosis DNA/RNA Synthesis Cancer
    CDK9-IN-50 is a selective and orally active CDK9 inhibitor with an IC50 of 2.2 nM. CDK9-IN-50 targets a distinct CDK9-specific subpocket to disrupt RNA polymerase II Ser2 phosphorylation and downregulate short-lived oncoproteins, including AR-V7 and Myc. CDK9-IN-50 exhibits antiproliferative activity against cancer cells, induces apoptosis and induces tumor growth inhibition in CRPC orthotopic mice models. CDK9-IN-50 can be used for the research of cancer, such as prostate cancer .
    CDK9-IN-50
  • HY-103019AR
    (±)-Enitociclib (Standard)

    (±)-BAY-1251152 (Standard); (±)-VIP152 (Standard)

    		 Reference Standards CDK Apoptosis DNA/RNA Synthesis Cancer
    (±)-Enitociclib (Standard) is the analytical standard of (±)-Enitociclib (HY-103019A). This product is intended for research and analytical applications. (±)-Enitociclib ((±)-BAY-1251152) is the racemic mixture of Enitociclib (HY-103019E). Enitociclib is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase Pol II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1. Enitociclib has anti-proliferative activity targeting MYC+ lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies [2].
    (±)-Enitociclib (Standard)
  • HY-103019BR
    (-)-Enitociclib (Standard)

    (R)-Enitociclib (Standard); (-)-BAY-1251152 (Standard); (-)-VIP152 (Standard)

    		 Reference Standards Drug Isomer CDK Apoptosis DNA/RNA Synthesis Cancer
    (-)-Enitociclib (Standard) is the analytical standard of (-)-Enitociclib (HY-103019B). This product is intended for research and analytical applications. (-)-Enitociclib ((R)-Enitociclib) is an enantiomer of Enitociclib (HY-103019E) with an optical rotation of (-). Enitociclib is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase Pol II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1. Enitociclib has anti-proliferative activity targeting MYC+ lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies [2].
    (-)-Enitociclib (Standard)
  • HY-103019R
    Enitociclib (Standard)

    (+)-BAY-1251152 (Standard); (+)-VIP152 (Standard); (S)-Enitociclib (Standard)

    		 Reference Standards Drug Isomer Apoptosis DNA/RNA Synthesis CDK Cancer
    Enitociclib (Standard) is the analytical standard of Enitociclib (HY-103019). This product is intended for research and analytical applications. Enitociclib ((+)-BAY-1251152; (+)-VIP152) is a selective CDK9 inhibitor (IC50=3 nM) that inhibits transcriptional elongation by blocking Ser2/Ser5 phosphorylation of RNA polymerase II. Enitociclib specifically depletes key short-lived proteins such as c-MYC, MCL-1 and induces tumor cell apoptosis. Enitociclib also interferes with the production of enhancer RNAs (eRNA) and enhancer-promoter interactions, and downregulates oncogene expression at the epigenetic level. Enitociclib exerts synergistic effects with agents including Bortezomib (HY-10227), Lenalidomide (HY-A0003), Pomalidomide (HY-10984), Venetoclax (HY-15531) and Paclitaxel (HY-B0015), and even reverses paclitaxel resistance. Enitociclib serves as a vital research tool for various malignancies such as double-hit diffuse large B-cell lymphoma, multiple myeloma and pancreatic ductal adenocarcinoma [2] .
    Enitociclib (Standard)
  • HY-RS07013
    JAG2 Human Pre-designed siRNA Set A

    		Small Interfering RNA (siRNA) Others

    JAG2 Human Pre-designed siRNA Set A contains three designed siRNAs for JAG2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    JAG2 Human Pre-designed siRNA Set A
    JAG2 Human Pre-designed siRNA Set A

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