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Thalidomide 5-fluoride

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-134983
    Thalidomide-Piperazine 5-fluoride

    		E3 Ligase Ligand-Linker Conjugates Autophagy Apoptosis Cancer
    Thalidomide-Piperazine 5-fluoride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology .
    Thalidomide-Piperazine 5-fluoride
  • 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-162704
    JMV7048

    		PROTACs Cancer
    JMV7048 is an effective PROTAC degrader targeting PXR (Pregnane X Receptor) with a DC50 of 379 nM. JMV7048 induces the polyubiquitination and degradation of PXR protein by recruiting E3 CRBN ubiquitin ligase and the 26S proteasome. JMV7048 significantly enhances the sensitivity of colon cancer stem cells to chemotherapy by reducing the expression of PXR protein in these cells, thereby significantly delaying cancer recurrence in vivo. JMV7048 is composed of the PXR agonist JMV6944 (HY-162738), linker (HY-162736), and Thalidomide 5-fluoride (HY-W087383) (Red: JMV6944; Blue: Thalidomide 5-fluoride ligand; Black: linker) .
    JMV7048
  • HY-153220A
    (R)-NX-2127

    		PROTACs Btk Inflammation/Immunology Cancer
    (R)-NX-2127 ((R)-Compound 28) is an isomer of the BTK PROTAC degrader NX-2127 (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)-NX-2127
  • 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-153220
    NX-2127

    		PROTACs Btk Cancer
    NX-2127 (Compound 28) is an orally active PROTAC deggrader, targeting to Bruton’s Tyrosine Kinase (Btk) . NX-2127 inhibits proliferation of BTK C481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). NX-2127 catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. NX-2127 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)
    NX-2127
  • 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-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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