GlpBio

Deubiquitinase

Deubiquitinase(去泛素化酶)

Deubiquitinases (DUBs) are a large group of proteases that cleave ubiquitin from proteins and other molecules. Ubiquitin is attached to proteins in order to regulate the degradation of proteins via the proteasome and lysosome; coordinate thecellular localisation of proteins; activate and inactivate proteins; and modulate protein-protein interactions. DUBs can reverse these effects by cleaving the peptide or isopeptide bond between ubiquitin and its substrate protein. In humans there are nearly 100 DUB genes, which can be classified into two main classes: cysteine proteases and metalloproteases. The cysteine proteases comprise ubiquitin-specific proteases (USPs), ubiquitin C-terminal hydrolases (UCHs), Machado-Josephin domain proteases (MJDs) and ovarian tumour proteases (OTU). The metalloprotease group contains only the Jab1/Mov34/Mpr1 Pad1 N-terminal+ (MPN+) (JAMM) domain proteases. DUBs play several roles in the ubiquitin pathway. One of the best characterised functions of DUBs is the removal of monoubiqutin and polyubiquitin chainsfrom proteins.

Deubiquitinase 相关产品(76)

  • GC34083 structure
    GC34083EOAI3402143
    CAS: 1699750-95-2
    纯度: >99.00%

    EOAI3402143是一种新型的、多靶点的去泛素化酶抑制剂。

  • GC34354 structure
    GC34354GSK2643943A
    CAS: 2449301-27-1
    纯度: >98.00%

    GSK2643943A是一种靶向USP20的去泛素化酶（DUB）抑制剂，GSK2643943A通过抑制USP20/Ub-Rho（IC 50 =160nM）的活性来阻断蛋白质-泛素键的裂解。

  • GC34670 structure
    GC34670MF-094
    CAS: 2241025-68-1
    纯度: >99.50%

    MF-094, a potent and selective USP30 inhibitor (IC50=0.12 μM), accelerates diabetic wound healing by inhibiting the NLRP3 inflammasome.

  • GC35906 structure
    GC35906DUBs-IN-1
    CAS: 924296-18-4
    纯度: >99.50%

    DUBs-IN-1 是一种泛素特异性蛋白酶 (USP) 的活性抑制剂，对于 USP8 的 IC50 为 0.85 μM。

  • GC36211 structure
    GC36211HBX 19818
    CAS: 1426944-49-1
    纯度: >98.50%

    HBX19818 is a specific inhibitor of USP7 with an IC 50 of 28.1 μM.

  • GC37875 structure
    GC37875USP7-IN-1
    CAS: 1381291-36-6
    纯度: >98.50%

    USP7-IN-1 是一种选择性的，可逆的泛素蛋白特异性蛋白酶 (USP7) 抑制剂，IC50 值为 77 μM，可用于癌症研究。

  • GC38043 structure
    GC38043USP25/28 inhibitor AZ1
    CAS: 2165322-94-9
    纯度: >98.00%

    USP25/28 抑制剂 AZ1 (AZ1) 是一种具有口服活性、选择性、非竞争性的双重泛素特异性蛋白酶 (USP) 25/28 抑制剂，IC50 分别为 0.7 μM 和 0.6 μM 。

  • GC39172 structure
    GC39172GRL0617
    CAS: 1093070-16-6
    纯度: >99.50%

    GRL0617是一种选择性的、竞争性非共价的严重急性呼吸综合征冠状病毒木瓜样蛋白酶（SARS-CoV PLpro）抑制剂，其IC₅₀值为0.6μM，Kᵢ值为0.49μM。

  • GC39625 structure
    GC396256RK73
    CAS: 1895050-66-4
    纯度: >99.00%

    6RK73 是一种共价不可逆的特异性 UCHL1 抑制剂，IC50 为 0.23 µM。6RK73 对 UCHL3 几乎没有抑制效果 (IC50=236 µM)。6RK73 特异性抑制乳腺癌中 UCHL1 的活性。

  • GC60317 structure
    GC60317RA-9
    CAS: 919091-63-7
    纯度: >98.00%

    RA-9 is a cell-permeable, potent and selective inhibitor of proteasome-associated deubiquitinating enzymes (DUBs) with favorable toxicity profile and anticancer activity. RA-9 selectively induces apoptosis in ovarian cancer cell lines.

  • GC60981 structure
    GC60981LDN-91946
    CAS: 439946-22-2
    纯度: >98.00%

    LDN-91946是一种有效的非竞争性的选择性泛素羧基末端水解酶-L1(UCH-L1)抑制剂，Kiapp为2.8μM.

  • GC62377 structure
    GC62377USP7-IN-8
    CAS: 2009273-60-1
    纯度: >98.50%

    USP7-IN-8 (example 81) 是一种选择性的泛素特异性蛋白酶 7 (USP7) 抑制剂，在 Ub-Rho110 分析中的 IC50 为 1.4 μM。USP7-IN-8 对 USP47 和 USP5 没有活性。USP7-IN-8 具有抗癌作用。

  • GC62410 structure
    GC62410USP30 inhibitor 18
    CAS: 2242582-40-5
    纯度: >99.50%

    USP30 inhibitor 18 是一种选择性 USP30 抑制剂，IC50 为 0.02 μM。USP30 inhibitor 18 增加蛋白质泛素化并加速线粒体自噬。

  • GC62460 structure
    GC62460LCAHA
    CAS: 117094-40-3
    纯度: >98.00%

    LCAHA (LCA hydroxyamide) 是一种脱泛素酶 USP2a 抑制剂，在 Ub-AMC 分析和 Di-Ub 分析中, IC50 分别为 9.7 μM 和 3.7 μM。LCAHA 通过抑制去泛素酶 USP2a 破坏细胞周期蛋白 D1 稳定性并诱导 G0/G1 期阻滞。

  • GC62509 structure
    GC62509STD1T
    CAS: 893075-58-6
    纯度: >98.50%

    An inhibitor of USP2a

  • GC62517 structure
    GC62517XL177A
    CAS: 2417089-74-6
    纯度: >98.50%

    XL177A is a potent, selective and irreversible inhibitor of Ubiquitin specific peptidase 7 (USP7) with IC50 of 0.34?nM.

  • GC62979 structure
    GC62979FT206
    CAS: 2278274-34-1
    纯度: >98.00%

    FT206 是羧胺类泛素特异性蛋白酶 (carboxamides as ubiquitin-specific protrase) 抑制剂，来自专利WO 2020033707 A1，示例11-1。

  • GC63027 structure
    GC63027IU1-248
    CAS: 2307472-03-1
    纯度: >99.00%

    Iu1-248, a derivative of IU1, is a potent and selective ubiquitin specific peptidase 14 (USP14) inhibitor with an IC50 of 0.83?μM.

  • GC64537 structure
    GC64537USP8-IN-1
    CAS: 2477650-96-5
    纯度: >99.00%

    USP8-IN-1 是一种 USP8 抑制剂，IC50 为 1.9 μM。USP8-IN-1 抑制 H1975 细胞生长，GI50 为 82.04 μM (CN111138358A; U10)。

  • GC64956 structure
    GC64956IU1-47
    CAS: 670270-31-2
    纯度: >99.00%

    An inhibitor of USP14

  • GC65259 structure
    GC65259BC-1471
    CAS: 896683-84-4
    纯度: >99.50% / >98.00%

    BC-1471是一种STAMBP去泛素化酶抑制剂，IC 50 值为0.33μM。

  • GC65275 structure
    GC65275USP7-IN-3
    CAS: 2202738-42-7
    纯度: >99.00%

    USP7-IN-3 (Compound 5) 是一种有效的选择性变构型泛素特异性蛋白酶7 (USP7) 抑制剂。

  • GC66438 structure
    GC66438USP5-IN-1

    USP5-IN-1 (compound 64) 是一种有效的去泛素酶 USP5 抑制剂，与 USP5 ZnF UBD 结合的 KD 值为 2.8 μM。USP5-IN-1对含有结构相似的 ZnF UBD 结构域的九种蛋白质具有选择性。USP5-IN-1 抑制 USP5 对双泛素底物的催化裂解。

  • GC67712 structure
    GC67712STAMBP-IN-1
    CAS: 896683-78-6
    纯度: >98.00%

    STAMBP-IN-1 是 STAMBP去泛素酶的小分子抑制剂，能中断 STAMBP-Ub-NALP7 的相互作用。在 Toll 样受体 (TLR) 激动后，STAMBP-IN-1 能够降低炎性小体底物 NALP7 的蛋白水平，抑制 IL-1b 释放。STAMBP- in -1 抑制了 STAMBP 裂解重组蛋白 di-Ub 的活性，IC50 为 0.33 mM。