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cereblon inhibitor

" in MedChemExpress (MCE) Product Catalog:

94

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1

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4

Isotope-Labeled Compounds

5

Click Chemistry

Cat. No. Nombre del producto Target Áreas de investigación Chemical Structure
  • HY-A0003
    Lenalidomide
    Maximum Cited Publications
    59 Publications Verification

    CC-5013

    		 Ligands for E3 Ligase Molecular Glues Apoptosis Inflammation/Immunology Cancer
    Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
    Lenalidomide
  • HY-14658
    Thalidomide
    20+ Cited Publications

    		 Ligands for E3 Ligase Autophagy Apoptosis Molecular Glues Inflammation/Immunology Cancer
    Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.
    Thalidomide
  • HY-101488
    CC-885
    15+ Cited Publications

    		 Molecular Glues Ligands for E3 Ligase Cancer
    CC-885 is a cereblon (CRBN) modulator with potent anti-tumour activity. CC-885 is also a known degrader of GSPT1, inhibiting protein translation.
    CC-885
  • HY-158101
    BMS-986365
    1 Publications Verification

    CC-94676

    		 PROTACs Androgen Receptor Cancer
    BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader (DC50 of 10-40 nM). BMS-986365 is capable of inducing cereblon (CRBN) E3 ligase-dependent ubiquitination and degradation of the androgen receptor (AR), as well as various AR mutants. BMS-986365 shows no degradation of the close AR family members estrogen receptor (ER), progesterone receptor (PR), and glucocorticoid receptor (GR). BMS-986365 shows significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. BMS-986365 can be used for the study of metastatic castration-resistant prostate cancer (mCRPC) .
    BMS-986365
  • HY-129602
    SD-36
    5+ Cited Publications

    		 PROTACs STAT Apoptosis Cancer
    SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase . SD-36 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    SD-36
  • HY-100507
    Avadomide
    5+ Cited Publications

    CC 122

    		 E1/E2/E3 Enzyme Apoptosis Molecular Glues NF-κB Inflammation/Immunology Cancer
    Avadomide is an orally active cereblon modulator. Avadomide modulates cereblon E3 ligase activity, inhibits NF-κB pathway, arrests the cell cycle at G1 phase, and thus induces apoptosis in cancer cell PDAC. Avadomide exhibits potent antitumor and immunomodulatory activities .
    Avadomide
  • HY-133120
    INY-03-041
    1 Publications Verification

    		 PROTACs Akt Cancer
    INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, Cereblon ligand). INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively .
    INY-03-041
  • HY-139039
    BSJ-4-116
    4 Publications Verification

    		 PROTACs CDK Cancer
    BSJ-4-116 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. BSJ-4-116 downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation). BSJ-4-116 exhibits potent antiproliferative effects, alone and in combination with the poly(ADP-ribose) polymerase inhibitor Olaparib (HY-10162) .
    BSJ-4-116
  • HY-170451
    Seldegamadlin

    KT-253

    		 PROTACs MDM-2/p53 Apoptosis Cancer
    Seldegamadlin (KT-253) is a selective p53 stabilizer and a MDM2 PROTAC degrader (DC50 = 0.4 nM). Seldegamadlin inhibits the proliferation of cancer cell RS4;11 with an IC50 of 0.3 nM, arrests the cell cycle at G2/M phase, and induces apoptosis. Seldegamadlin upregulates p53 activity and overcomes the p53-MDM2 feedback loop. Seldegamadlin can be used for the study of hematologic and solid tumors, such as acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL). (Pink: ligand for target protein MDM2 ligand 4 (HY-170452); Black: linker (HY-W001478); Blue: ligand for E3 ligase cereblon (HY-163927)) .
    Seldegamadlin
  • HY-138946
    XY028-140
    1 Publications Verification

    		 CDK PROTACs Cancer
    XY028-140 is a PROTAC connected by ligands for Cereblon and CDK. XY028-140 inhibits both CDK4/6 expression and CDK4/6 activity in cancer cells .
    XY028-140
  • HY-130665
    TL12-186
    1 Publications Verification

    		 PROTACs CDK Cancer
    TL12-186 is a Cereblon-dependent multi-kinase PROTAC degrader. Multi-kinases include CDK, BTK, FLT3, Aurora kinases, TEC, ULK, ITK, et al. TL12-186 inhibits CDK2/cyclin A (IC50=73 nM) and CDK9/cyclin T1 (IC50=55 nM) .
    TL12-186
  • HY-130709
    PROTAC CDK2/9 Degrader-1

    		PROTACs CDK Cancer
    PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with Cereblon ligand .
    PROTAC CDK2/9 Degrader-1
  • HY-125877
    PROTAC Mcl1 degrader-1
    1 Publications Verification

    		 PROTACs Bcl-2 Family Cancer
    PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on Cereblon ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC50 of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC50 of 0.54 μM .
    PROTAC Mcl1 degrader-1
  • HY-114407
    TD-428

    		PROTACs Epigenetic Reader Domain Cancer
    TD-428 is a PROTAC connected by ligands for Cereblon and BRD4. TD-428 is a highly specific BRD4 degrader with a DC50 of 0.32 nM . TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation .
    TD-428
  • HY-168162
    ZLC491

    		PROTACs CDK Cancer
    ZLC491 is an orally active PROTAC degrader that selectively targets CDK12/CDK13 and exhibits certain oral bioavailability. ZLC491 induces cereblon- and proteasome-dependent selective degradation of CDK12 and CDK13. ZLC491 inhibits the transcription and expression of long genes, and mainly acts on a subset of DNA damage response genes. ZLC491 inhibits the proliferation of various triple-negative breast cancer cells. ZLC491 can be used in research related to triple-negative breast cancer .
    ZLC491
  • HY-125876
    PROTAC Bcl2 degrader-1
    1 Publications Verification

    		 PROTACs Bcl-2 Family Cancer
    PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC based on Cereblon ligand, which potently and selectively induces the degradation of Bcl-2 (IC50, 4.94 μM; DC50, 3.0 μM) and Mcl-1 (IC50, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1 (Blue: CRBN ligand, Black: linker；Pink: Mcl-1/Bcl-2 inhibitor, Nap-1).
    PROTAC Bcl2 degrader-1
  • HY-153386
    CPD-1224

    		Anaplastic lymphoma kinase (ALK) Cancer
    CPD-1224 is an orally effective ALK inhibitor, a derivative of an ALK inhibitor that connects to the cereblon ligand. CPD-1224 targets the EML4-ALK oncogenic fusion protein and degrades both ALK and the mutant forms L1196M/G1202R. CPD-1224 can slow down tumor growth .
    CPD-1224
  • HY-111546
    BI-3663
    1 Publications Verification

    		 PROTACs FAK Cancer
    BI-3663 is a highly selective PTK2/FAK PROTAC (DC50=30 nM), with Cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC50 of 18 nM. BI-3663 is a PROTAC that composes of BI-4464 (HY-124625) linked to Pomalidomide (HY-10984) with a linker . Anti-cancer activity .
    BI-3663
  • HY-159579
    CW-3308

    		PROTACs Epigenetic Reader Domain Cancer
    CW-3308 is an orally active BRD9 PROTAC degrader with an DC50 of 92 nM. CW-3308 forms a ternary complex with BRD9 and cereblon to mediate BRD9 degradation. CW-3308 inhibits the viability of synovial sarcoma and rhabdoid tumor cells. CW-3308 reduces BRD9 protein levels in xenograft tumor tissues and suppresses tumor growth in xenograft models. CW-3308 can be used for the research of synovial sarcoma and rhabdoid tumors .
    CW-3308
  • HY-131183
    PROTAC PD-1/PD-L1 degrader-1

    		PROTACs PD-1/PD-L1 Inflammation/Immunology
    PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner .
    PROTAC PD-1/PD-L1 degrader-1
  • HY-161574
    LLC0424

    		PROTACs Histone Methyltransferase Cancer
    LLC0424 is a potent and selective cereblon-based PROTAC nuclear receptor-binding SET domain-containing 2 (NSD2) degrader. LLC0424 effectively degraded NSD2 with a DC50 of 20 nM in RPMI-8402 cells. LLC0424 selectively induces NSD2 degradation in a cereblon- and proteasome-dependent fashion. (Blue: CRBN ligand (HY-14658), Black: linker (HY-40002); Pink: NSD2 inhibitor (HY-161575)) .
    LLC0424
  • HY-156111
    ARD-1676
    1 Publications Verification

    		 PROTACs Androgen Receptor Cancer
    ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand. ARD-1676 has AR-degrading activity in vitro and in vivo and inhibits VCaP tumor growth in mouse xenograft tumor models .
    ARD-1676
  • HY-125835
    CP-10
    1 Publications Verification

    		 PROTACs CDK Cancer
    CP-10 is a PROTAC connected by ligands for Cereblon and CDK, with highly selective, specific, and remarkable CDK6 degradation (DC50=2.1 nM). It inhibits proliferation of several haematopoietic cancer cells with impressive potency including multiple myeloma, and can still degrades mutated and overexpressed CDK6 .
    CP-10
  • HY-153821
    PROTAC KRAS G12C degrader-2

    		Ras PROTACs Cancer
    PROTAC KRAS G12C degrader-2 (compound 432) is a modulator of K-Ras protein hydrolysis. PROTAC KRAS G12C degrader-2 is a bifunctional compound, which contain on one end a cereblon inhibitor of apoptosis proteins (IAP) and on the other end a moiety which binds KRAS .
    PROTAC KRAS G12C degrader-2
  • HY-163759
    HuR degrader 2

    		Molecular Glues HuR Cancer
    HuR degrader 2 (Compound 3) is a molecule glue, which targets RNA-binding protein Hu antigen R (HuR) and degrades 30% HuR at 0.1 μM. HuR degrader 2 inhibits the proliferation of cancer cell Colo-205, with IC50≤200 nM. HuR degrader 2 exhibits a high affinity with cereblon, with an HTRF ratio < 0.02 .
    HuR degrader 2
  • HY-123919
    TL13-112
    2 Publications Verification

    		 PROTACs Anaplastic lymphoma kinase (ALK) Cancer
    TL13-112 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.14 nM. TL13-112 also prompts the degradation of additional kinases including Aurora A, FER, PTK2 and RPS6KA1 with IC50 values of 8550 nM, 42.4 nM, 25.4 nM, and 677 nM, respectively. TL13-112 is comprised of the conjugation of Ceritinib?(HY-15656) and the Cereblon ligand of Pomalidomide (HY-10984) .
    TL13-112
  • HY-141512
    JB170
    3 Publications Verification

    		 PROTACs Aurora Kinase Cancer
    JB170 is a potent and highly specific PROTAC-mediated AURORA-A (Aurora Kinase) degrader (DC50=28 nM) by linking Alisertib, to the Cereblon-binding molecule Thalidomide. JB170 preferentially binds AURORA-A (EC50=193 nM) over AURORA-B (EC50=1.4 µM). JB170-mediated S-phase arrest is caused specifically by AURORA-A depletion. JB170 has excellent ability to inhibit non-catalytic function of AURORA-A kinase .
    JB170
  • HY-103636
    PROTAC Sirt2 Degrader-1
    1 Publications Verification

    		 Sirtuin PROTACs Cancer
    PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide Cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s>100 μM) .
    PROTAC Sirt2 Degrader-1
  • HY-122582
    TL13-12

    		PROTACs Anaplastic lymphoma kinase (ALK) Cancer
    TL13-12 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.69 nM. TL13-12 also prompts the degradation of additional kinases including Aurora A, FER, PTK2, and RPS6KA1 with IC50 values of 13.5 nM, 5.74 nM, 18.4 nM, and 65 nM, respectively. TL13-12 is comprised of the conjugation of TAE684 (HY-10192) and the Cereblon ligand of Pomalidomide (HY-10984) .
    TL13-12
  • HY-A0003B
    Lenalidomide hemihydrate
    Maximum Cited Publications
    59 Publications Verification

    CC-5013 hemihydrate

    		 Ligands for E3 Ligase Molecular Glues Apoptosis Cancer
    Lenalidomide hemihydrate (CC-5013 hemihydrate), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hemihydrate is an orally active immunomodulator. Lenalidomide hemihydrate (CC-5013 hemihydrate) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hemihydrate (CC-5013 hemihydrate) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
    Lenalidomide hemihydrate
  • HY-130122
    MG-277
    1 Publications Verification

    		 Molecular Glues PROTACs Apoptosis Cancer
    MG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor based on Cereblon E3 ligand, GSPT1, with a DC50 of 1.3 nM. MG-277 potently inhibits tumor cell growth in a p53-independent manner, with IC50s of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells, respectively. Anticancer activity .
    MG-277
  • HY-171860
    FC-14369

    		PROTACs HIV Infection Cancer
    FC-14369 is a PROTAC degrader targeting the HIV-1 Nef protein, with a DC50 value of 160 nM. Through its bifunctional structure, FC-14369 binds to Nef and the Cereblon E3 ubiquitin ligase, induces Nef ubiquitination and proteasomal degradation, restores the expression of cell-surface CD4 and MHC-I, and inhibits HIV-1 replication. FC-14369 can be used in research on HIV infection and AIDS. FC-14369 is applicable to studies related to HIV-1 infection .
    FC-14369
  • HY-173679
    RBN012811

    		PROTACs PARP Interleukin Related STAT Integrin HSV VSV Infection Cancer
    RBN012811 is a highly selective PROTAC-based PARP14 degrader. RBN012811 forms a ternary complex with cereblon by binding to the NAD + site of PARP14, and mediates the specific degradation of PARP14 via the ubiquitin-proteasome pathway (IC50=10 nM). RBN012811 effectively depletes endogenous PARP14 in various cell lines and primary human macrophages, thereby downregulating IL-10 production and IFN-β mRNA levels, increasing phosphorylated STAT1 levels to enhance inflammatory signaling, and inhibiting interferon-induced ADPr condensate formation. RBN012811 also modulates viral replication, exhibiting increased HSV1 replication while reducing VSV replication. RBN012811 has important application value in research related to cancer and viral infections .
    RBN012811
  • 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-111870
    PROTAC RIPK degrader-6

    		PROTACs RIP kinase Cancer
    PROTAC RIPK degrader-6 (example 1) is a Cereblon-based PROTAC targeting RIP Kinase degradation wherein the RIP2 kinase inhibitor is linked via a linker to a cereblon binder .
    PROTAC RIPK degrader-6
  • HY-160506
    PRO-6E

    		PROTACs c-Met/HGFR Apoptosis Cancer
    PRO-6E is an oral active PROTAC based on Cereblon ligand, and induces the degradation of MET with maximum degradation of 81.9% at 1 μM in MKN-45 cells. PRO-6E inhibits tumor growth in vivo and in vitro. PRO-6E induces cell apoptosis and induces cell arrest (Sturcture Note:(Blue: Cereblon ligand (HY-103596), Black: linker；Pink: ALK/c-Met inhibitor Crizotinib (HY-50878)) .
    PRO-6E
  • HY-154860
    PTD10

    		PROTACs Btk Apoptosis Caspase Bcl-2 Family NF-κB Akt Inflammation/Immunology Cancer
    PTD10 is a selective and potent BTK PROTAC degrader (DC50 = 0.5 nM, KD = 2.28 nM). PTD10 can recruit cereblon (CRBN) E3 ligase and form a ternary complex with BTK, thereby mediating the ubiquitination and proteasome-dependent degradation of BTK. PTD10 inhibits cancer cells proliferation, and induces cell apoptosis via activation of the caspase-dependent pathway and mitochondrial pathway. PTD10 potently inhibits the BCR, AKT and NF-κB signaling pathway. PTD10 can be used for researches of B-cell malignancies and autoimmune disease .
    PTD10
  • HY-155218
    TMX-2172

    		PROTACs CDK Cancer
    TMX-2172 is a selective bivalent cereblon-recruiting PROTAC-based dual CDK2 and CDK5 degrader with IC50 values of 6.5 nM and 6.8 nM, respectively. TMX-2172 shows selectivity for CDK2 and CDK5 over other cell cycle CDKs (CDK1, CDK4, and CDK6) and transcriptional CDKs (CDK7 and CDK9). TMX-2172 inhibits CDK2/CDK5 enzymatic activity, induces their proteasomal degradation, reduces ASCL1 protein levels and half-life, induces cancer cell death, and exerts antiproliferative effects. TMX-2172 can be used for the research of ovarian cancer and small cell lung cancer .
    TMX-2172
  • HY-148063
    DB0614

    		PROTACs AAK1 Aurora Kinase CaMK CDK Ferroptosis Salt-inducible Kinase (SIK) LIM Kinase (LIMK) ULK Metabolic Disease
    DB0614 is a PROTAC based on Cereblon ligand, which is a selective and potent targeted protein degrader of NEK9 inhibitor. DB0614 can degrade ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2 and ULK1. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity .(Blue: Thalidomide-4-OH (HY-103596), Black: linker, Pink: FLT3-IN-17 (HY-148070))
    DB0614
  • HY-14658R
    Thalidomide (Standard)

    		Ligands for E3 Ligase Autophagy Apoptosis Reference Standards Inflammation/Immunology Cancer
    Thalidomide (Standard) is the analytical standard of Thalidomide. This product is intended for research and analytical applications. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.
    Thalidomide (Standard)
  • HY-175652
    AZD9750

    		PROTACs Adenosine Receptor Cancer
    AZD9750 is an orally active, Cereblon (CRBN)-recruiting, androgen receptor (AR)-targeted PROTAC degrader. AZD9750 induces the proteasome-dependent degradation of both wild-type AR and the drug-resistant mutant AR L702H, thereby inhibiting the AR signaling pathway. AZD9750 suppresses tumor growth in mouse prostate cancer xenograft models and has been utilized in prostate cancer research .
    AZD9750
  • HY-143715
    Cereblon inhibitor 1

    		Ligands for E3 Ligase Cancer
    Cereblon inhibitor 1, an isoindoline derivative, is a cereblon E3 ubiquitin ligase modulating agent. Cereblon inhibitor 1 has the potential for cancer research.
    Cereblon inhibitor 1
  • HY-44103
    Desmethyl-QCA276

    PROTAC BRD4-binding moiety 4

    		 Ligands for Target Protein for PROTAC Cancer
    Desmethyl-QCA276 (PROTAC BRD4-binding moiety 4), the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade BET. QCA276 is a BET inhibitor with an IC50 of 10 nM, and with a Ki of 2.3 nM . Desmethyl-QCA276 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Desmethyl-QCA276
  • HY-153661
    Cereblon inhibitor 2

    		Ligands for E3 Ligase Autophagy Apoptosis Cancer
    Cereblon inhibitor 2 (compound 8) is a Cereblon inhibitor useful in solid tumor research, especially breast cancer .
    Cereblon inhibitor 2
  • HY-A0003R
    Lenalidomide (Standard)

    CC-5013 (Standard)

    		 Reference Standards Ligands for E3 Ligase Molecular Glues Apoptosis Inflammation/Immunology Cancer
    Lenalidomide (Standard) is the analytical standard of Lenalidomide. This product is intended for research and analytical applications. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
    Lenalidomide (Standard)
  • HY-162589
    Lw13

    		PROTACs HSP Apoptosis Cancer
    Lw13 is a Hsp90-targeting PROTAC and achieves maximum degradation at a concentration of 0.05 μM in Siha cells. Lw13 induces cell apoptosis and exhibits potent anti-tumor activity both in vitro and in vivo(Sturcture Note:(Blue: Cereblon ligand (HY-A0003), Black: linker；Pink: Hsp90 inhibitor SNX-5422 (HY-10213)) .
    Lw13
  • HY-170405
    YB-3–17

    		PROTACs mTOR Cancer
    YB-3-17 is a bifunctional molecule, that inhibits mTOR (IC50=0.22 nM) or degrades G1 to S phase transition 1 gene (GSPT1, DC50=5 nM) in a PROTAC mechanism. YB-3-17 exhibits antiproliferative activity in multi glioblastoma cell lines with IC50 of nanomolare levels. YB-3-17 exhibits antitumor efficacy in mouse models . (Pink: ligand for target protein (HY-170407); Black: linker (HY-A0102); Blue: ligand for E3 ligase Cereblon (HY-14658))
    YB-3–17
  • HY-115568
    BETd-246
    2 Publications Verification

    		 PROTACs Epigenetic Reader Domain Cancer
    BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and BET, exhibiting superior selectivity, potency and antitumor activity .
    BETd-246
  • HY-130612
    PROTAC BRD2/BRD4 degrader-1

    		Epigenetic Reader Domain PROTACs Cancer
    PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A .
    PROTAC BRD2/BRD4 degrader-1
  • HY-14658S
    Thalidomide-d4

    		Molecular Glues Ligands for E3 Ligase Autophagy Apoptosis Inflammation/Immunology Cancer
    Thalidomide-d4 is a deuterium labeled Thalidomide. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ~250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties .
    Thalidomide-d4

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