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Thalidomide 5-fluoride

" in MedChemExpress (MCE) Product Catalog:
製品番号 製品名 Target 研究分野 構造式
  • HY-153220
    Zelebrudomide

    NX-2127

    		 PROTACs Btk Inflammation/Immunology Cancer
    Zelebrudomide (NX-2127) (Compound 28) is an orally active PROTAC deggrader, targeting to Bruton’s Tyrosine Kinase (Btk). Zelebrudomide inhibits proliferation of BTK C481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). Zelebrudomide catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. Zelebrudomide stimulates T cell activation and increases IL-2 production in primary human T Cells . (Pink: BTK ligand 10 (HY-168302); Black: (R)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168348); Blue: Thalidomide 5-fluoride (HY-W087383)
    Zelebrudomide
  • HY-W087383
    Thalidomide 5-fluoride

    		Ligands for E3 Ligase Autophagy Apoptosis Cancer
    Thalidomide 5-fluoride is a thalidomide-based Cereblon ligand used to recruit Cereblon protein. Thalidomide 5-fluoride can be linked to target protein ligands (e.g. IRAK4) through a linker to form PROTAC molecules (e.g. PROTAC IRAK4 degrader-1). PROTAC IRAK4 degrader-1 caused <20%, >20-50%, and >50% IRAK4 protein degradation in OCI-LY-10 cells at concentrations of 0.01, 0.1, and 1 μM, respectively .
    Thalidomide 5-fluoride
  • HY-153357
    NRX-0492

    		PROTACs Btk Cancer
    NRX-0492 is an orally active PROTAC-class BTK degrader. NRX-0492 catalyzes BTK ubiquitination and proteasome degradation (DC50 ≤ 0.2 nM, DC90 ≤ 0.5 nM). NRX-0492 inhibits B cell receptor (BCR) mediated signaling, transcription programs, and chemokine secretion. NRX-0492 has antitumor effects against chronic lymphocytic leukemia.NRX-0492 consists of a target protein ligand (red part) BTK-IN-40 (HY-170324), an E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383), and a PROTAC linker (black part) (3R)-3-Pyrrolidinemethanol (HY-60263).
    NRX-0492
  • HY-W145436
    Thalidomide-Piperazine 5-fluoride hydrochloride

    		E3 Ligase Ligand-Linker Conjugates Autophagy Apoptosis Cancer
    Thalidomide-Piperazine 5-fluoride hydrochloride is a derivative of cereblon (CRBN) inhibitor Thalidomide (HY-14658), which can be used as ligands for E3 ubiquitin ligase (Ligands for E3 Ligase) for PROTACs Synthesis .
    Thalidomide-Piperazine 5-fluoride hydrochloride
  • HY-134983
    Thalidomide-Piperazine 5-fluoride

    		E3 Ligase Ligand-Linker Conjugates Apoptosis Autophagy Cancer
    Thalidomide-piperazine hydrochloride is a synthetic E3 ligase ligand-linker conjugate, containing a cereblon ligand based on Thalidomide (HY-14658) and one linker. Thalidomide-piperazine hydrochloride can be used in studies related to PROTAC synthesis .
    Thalidomide-Piperazine 5-fluoride
  • HY-153220A
    (R)-Zelebrudomide

    (R)-NX-2127

    		 PROTACs Btk Inflammation/Immunology Cancer
    (R)-Zelebrudomide ((R)-NX-2127) ((R)-Compound 28) is an isomer of the BTK PROTAC degrader Zelebrudomide (HY-153220) . (Pink: BTK ligand 10 (HY-168302); Black: (S)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168303); Blue: Thalidomide 5-fluoride (HY-W087383).
    (R)-Zelebrudomide
  • HY-149917
    ITK degrader 1

    		PROTACs Itk Cancer
    ITK degrader 1 is a highly selective degrader of interleukin-2-inducible T-cell kinase (ITK; DC50=3.6 nM in vivo in mice), with good plasma exposure levels. ITK degrader 1 induces rapid, and prolonged ITK degradation and suppresses IL-2 secretion (EC50=35.2 nM, Jurkat cells) stimulated by anti-CD3 antibodyin vivo. ITK degrader 1 consists of target protein ligand (red part) ITK ligand 1 (HY-168387), PROTAC linker (black part) Piperidine-C2-piperazine-Boc (HY-168388) and E3 ubiquitinase ligand (blue part) Thalidomide 5-fluoride (HY-W087383). E3 ubiquitinase and PROTAC linker can form Thalidomide-piperidine-C2-piperazine-Boc (HY-168389) .
    ITK degrader 1
  • HY-W998239
    Thalidomide 5-fluoride 6-piperidine-C-OH

    		E3 Ligase Ligand-Linker Conjugates Cancer
    Thalidomide 5-fluoride 6-piperidine-C-OH is an E3 ligase ligand-linker conjugate containing a CRBN-based ligand and linker, which can be used to synthesize PROTAC.
    Thalidomide 5-fluoride 6-piperidine-C-OH
  • HY-176808
    Thalidomide-amine-C11-acid

    		E3 Ligase Ligand-Linker Conjugates Cancer
    Thalidomide-amine-C11-acid is an E3 ligase ligand-linker conjugate which consists of Thalidomide 5-fluoride (HY-W087383) and a linker (HY-W105740). Thalidomide-amine-C11-acid can be used to synthesize JQAD1 (HY-145765) .
    Thalidomide-amine-C11-acid
  • HY-161708
    PROTAC FLT3/CDKs degrader-1

    		PROTACs CDK FLT3 Cancer
    PROTAC FLT3/CDKs degrader-1 (Compound C3) is a degrader for cyclin-dependent kinases (DC50 is 18.73 nM for CDK2) and the FMS-like tyrosine kinase 3 (FLT3). PROTAC FLT3/CDKs degrader-1 induces differentation of HL-60 (72.77% differentation at 6.25 nM), inhibits proliferation of AML cells, with IC50s of 2.9-37 nM. PROTAC FLT3/CDKs degrader-1 is potential for ameliorating acute myeloid leukemia. (Pink: ligand for target protein FLT3/CDKs ligand-1 (HY-161709); Black: linker (HY-W012935); Black: ligand for E3 ligase Thalidomide 5-fluoride (HY-W087383))
    PROTAC FLT3/CDKs degrader-1

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