2. Search Result
Search Result
Results for "

TMDs

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-153321
    Bexobrutideg
    1 Publications Verification

    NX-5948; BTK-IN-24

    		 PROTACs Btk Inflammation/Immunology Cancer
    Bexobrutideg (NX-5948) 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. Bexobrutideg mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. Bexobrutideg is efficacious in a mouse collageninduced arthritis (CIA) model. Bexobrutideg can cross the blood brain barrier (BBB). Bexobrutideg is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
    Bexobrutideg
  • 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-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-160142
    UBX-382

    		PROTACs Btk Syk MEK ERK Cancer
    UBX-382 is an orally active BTK PROTAC degrader with a DC50 of 4.56 nM. UBX-382 inhibits B-cell receptor signaling by targeting BTK. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins. UBX-382 inhibits tumor growth in murine xenograft models harboring wild-type or C481S mutant BTK-expressing TMD-8 cells. UBX-382 can be used for the study of B-cell-related blood cancers .
    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-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-174850
    CFON-026

    		Btk Cancer
    CFON-026 is a selective, orally active and non-covalent BTK inhibitor with an IC50 of 0.27  nM. CFON-026 has significant antitumor activity against wild-type BTK (TMD8 and REC-1) and all clinically relevant BTK resistance mutations (BTK C481S, T474I, L528W and V416L). CFON-026 induces complete tumor regression in TMD8 xenograft mice model. CFON-026 can be used for research of hematological cancers like chronic lymphocytic leukemia and waldenström macroglobulinemia .
    CFON-026
  • HY-156095
    F7H
    2 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-175541
    TQ-3959

    		PROTACs Btk Cancer
    TQ-3959 is an orally active BTK PROTAC degrader, with a DC50 of 14.6 nM. TQ-3959 exerts antiproliferative activity against both wild-type BTK and C481S mutant BTK cell lines. TQ-3959 exhibits tumor growth inhibition in female NOD-SCID mice bearing TMD-8 xenografts. TQ-3959 can be used in the research on B-cell malignancies such as lymphoma.(Pink: BTK ligand (HY-150885), Blue: CRBN Ligand (HY-W733888), Black: Linker (HY-W061884), E3 ligase ligand-linker conjugate (HY-175545)) .
    TQ-3959
  • HY-177750
    TD-522

    		Molecular Glues Apoptosis Cancer
    TD-522 is a potent and selective molecular glue GSPT1 degrader, with a DC50 of 0.269 nM. TD-522 exhibits strong anti-proliferative effects and induces apoptosis in acute myeloid leukemia (AML) and diffuse large B-cell lymphoma (DLBCL) cells. TD-522 suppresses tumor growth in a TMD-8 xenograft model. TD-522 can be used for AML and DLBCL research .
    TD-522
  • HY-113918
    SW-106

    		PTHR Metabolic Disease
    SW-106 is a parathyroid hormone receptor 1 (PTHR1) antagonist. SW106 antagonizes PTHR1-mediated cAMP signaling induced by the peptide analog, M-PTH (1-11), as well as by the native PTH (1-9) sequence, as tethered to the extracellular end of transmembrane domain (TMD) helix-1 of the receptor. SW-106 can be used for the research of metabolic disease .
    SW-106
  • 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-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-178966
    STING agonist-48

    		STING Infection Inflammation/Immunology
    STING agonist-48 is a potent STING agonist that exhibits STING-dependent activity in vitro (EC50 = 4.02 μM). STING agonist-48 prefers to bind with the transmembrane domain (TMD) over the cytosolic cyclic dinucleotide (CDN) domain. STING agonist-48 shows adjuvant efficacy, enhancing IgG and Th1/Th2 cytokine responses in humanized STING mice. STING agonist-48 can be used for the study of inflammation-related diseases .
    STING agonist-48
  • HY-11074
    CE-326597

    		Cholecystokinin Receptor Metabolic Disease
    CE-326597 is a small molecule agonist of the cholecystokinin A receptor (CCKAR). CE-326597 occupies only the lower half of the TMD pocket and cannot mimic the crucial interaction between CCK-8 and ECL1-3. CE-326597 can be used to study metabolic diseases and gastrointestinal dysfunction .
    CE-326597
  • 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-153321A
    (R,R)-Bexobrutideg

    (R,R)-NX-5948; (R,R)-BTK-IN-24

    		 Drug Isomer PROTACs Btk Inflammation/Immunology Cancer
    (R,R)-Bexobrutideg is the (R,R)-enantiomer of Bexobrutideg (HY-153321). Bexobrutideg (NX-5948) is an orally active PROTAC that induces specific BTK protein degradation via a cereblon E3 ligase (CRBN) complex without degrading other cereblon neo substrates. Bexobrutideg mediates potent anti-inflammatory activity through BTK degradation, thereby inhibiting B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models containing wild-type BTK or BTKi resistance mutations. Bexobrutideg is effective in a mouse model of collagen-induced arthritis (CIA). Bexobrutideg can cross the blood-brain barrier. NX-5948 consists of a target protein ligand, a linker, and a VHL E3 ubiquitin ligase (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
    (R,R)-Bexobrutideg
  • 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

Inquiry Online

Your information is safe with us. * Required Fields.

Salutation

  

Country or Region *

Applicant Name *

 

Organization Name *

Department *

     

Email Address *

 

Product Name *

Cat. No.

  

Requested quantity *

Phone Number *

     

Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: