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TMDs

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-150210
    FSHR agonist 1

    		Estrogen Receptor/ERR Endocrinology
    FSHR agonist 1 is a high affinity and allosteric follicle stimulating hormone receptor (FSHR) agonist with a pEC50 of 7.72. FSHR agonist 1 formes extensive interactions with the TMD to directly activate FSHR .
    FSHR agonist 1
  • HY-129527
    GNE-9278

    		iGluR Neurological Disease
    GNE-9278 is a highly selective positive allosteric modulator of NMDAR that acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activated NMDARs to increase peak current and agonist affinity .
    GNE-9278
  • HY-160142
    UBX-382

    		Btk Cancer
    UBX-382 is an orally available proteolysis-targeting chimeras (PROTACs) that target BTK to inactivate B-cell receptor signaling. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins and shows anti-cancer activity in murine xenograft models of TMD-8 cells .
    UBX-382
  • HY-15805
    KIN-8194

    		Src Btk Cancer
    KIN-8194 is an orally active dual inhibitor of HCK and BTK, with IC50 values of 0.915 and <0.495 nM, respectively. KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma (MCL). KIN-8194 overcomes ibrutinib (HY-10997) resistance with a survival benefit in TMD-8 ABC DLBCL xenografted mice .
    KIN-8194
  • HY-119165
    GSM-1

    		γ-secretase Neurological Disease
    GSM-1 is a potent γ-secretase modulator. GSM-1 directly targets the transmembrane domain (TMD) 1 of presenilin 1 (PS1) .
    GSM-1
  • HY-156095
    F7H
    1 Publications Verification

    		 Wnt Cancer
    F7H is a Frizzled receptor FZD7 antagonist (IC50: 1.25 μM). Frizzled receptors (FZDs) influence Wnt signaling, mediating embryonic development and tissue homeostasis. F7H is a potent ligand for the FZD7 transmembrane domain (TMD) .
    F7H
  • HY-145416
    G247

    		Bacterial Infection
    G247 is a specific MsbA inhibitor. G247 acts as a transmembrane domains (TMDs) wedge, symmetrically increasing nucleotide-binding domains (NBDs) separation and preventing conformational transition of MsbA. G247 suppresses ATPase activity by increasing inter-NBD distance .
    G247
  • HY-172217
    DNMT1-IN-5

    		DNA Methyltransferase Apoptosis Cancer
    DNMT1-IN-5 (Compound 55) is the inhibitor for DNMT that inhibits DNMT1 and DNMT3A with IC50 of 2.42 μM and 14.4 μM. DNMT1-IN-5 exhibits antiproliferative activity in a variety of cancer cell lines (IC50s for TMD-8, DOHH2, MOLM-13, THP-1, RPIM-8226 and HCT116 are 0.19-2.37 μM), arrests the cell cycle at G2/M phase, and induces apoptosis in TMD-8 and DOHH2 cells. DNMT1-IN-5 exhibits antitumor efficacy in TMD-8 xenograft mouse models .
    DNMT1-IN-5
  • HY-173143
    BTK-IN-42

    		Btk Cancer
    BTK-IN-42 (Compound 11a) is a Btk inhibitor. BTK-IN-42 can effectively inhibit the growth and migration of tumor cells TMD8, with IC50 values of 2.61 and 5.34 μM for TMD8 and T9 cells respectively. It shows promise for research in the field of anti-cancer .
    BTK-IN-42
  • HY-156553
    BTK-IN-27

    		Btk Inflammation/Immunology Cancer
    BTK-IN-27 (example 8) is a BTK inhibitor (IC50: 0.2 nM). BTK-IN-27 shows anti-proliferative activity in TMD8 cells (IC50: < 5 nM). BTK-IN-27 can be used for research of cancer, lymphoma, leukemia and immunological diseases .
    BTK-IN-27
  • HY-164462
    BHA536

    		PKC NF-κB Apoptosis Cancer
    BHA536 is an orally active selective inhibitor for PKCα/β and NF-kB signaling pathway. BHA536 inhibits the proliferation of CD79-mutated ABC DLBCL cell, arrests cell cycle at G1 phase, and induces apoptosis in TMD8 cell. BHA536 exhibits antitumor efficacy in mice .
    BHA536
  • HY-150593
    IRAK4-IN-16

    		IRAK Cancer
    IRAK4-IN-16 (compound 4) is a potent IRAK4 (interleukin-1 receptor associated kinase 4) inhibitor, with an IC50 of 2.5 nM. IRAK4-IN-16 shows cytotoxicity activity against OCI-LY10, TMD8, Ramos and HT cells, with IC50 values of 0.2, 0.2, 0.6, and 2.7 μM, respectively .
    IRAK4-IN-16
  • HY-107506
    Ro 67-4853

    		mGluR Neurological Disease
    Ro 67-4853 is a positive allosteric modulator (PAM) of mGluR1 (pEC50=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation .
    Ro 67-4853
  • HY-153321
    NX-5948

    BTK-IN-24

    		 Btk PROTACs Inflammation/Immunology Cancer
    NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker) .
    NX-5948
  • 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 . NX-2127 is composed of PROTAC target protein ligand (red part) BTK ligand 10 (HY-168302), E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383) and PROTAC Linker (black part) (S)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168303). Among which, the conjugate of E3 ubiquitin ligase ligand + Linker compose of Thalidomide-pyrrolidine-C-piperidine-Ph-NH2 (HY-168304).
    NX-2127

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