1. Signaling Pathways
  2. PROTAC
  3. PROTAC

PROTAC (PROTAC)

PROTACs (Proteolysis Targeting Chimeric Molecules) are heterobifunctional nanomolecules that structurally comprised of two functional motifs linked by a linker. One motif is a small molecule ligand for the target protein of interest, while the other recognizes a specific E3 ligase. By recruiting an E3 ligase to a target protein and formation of a ligase:PROTAC:target ternary complex, A PROTAC leads to polyubiquitylation and subsequent degradation of target through ubiquitin-proteasome system (UPS). PROTACs have desirable features such as the ability to target the “undruggable” proteome and overcome the accumulation of the drug targets and will be promising targeted therapeutics for cancers.

Among the hundreds of E3 ligases, VHL (von Hippel-Lindau disease tumor suppressor protein), CRBN (Cereblon), MDM2 (the mouse double minute 2 homologue) and cIAP (cellular inhibitor of apoptosis 1) are reported to target kinases (such as MEK, KRAS, CDK and Bcr/Abl), transcription factors (such as p53, STAT, RAR, ER and AR), and epigenetic readers (BET bromodomain such as BRD family) and are most widely used in the development of PROTACs. There are also some specific types of PROTACs, such as homo-PROTACs and general PROTACs for tagged fusion proteins. Homo-PROTACs intend to dimerize an E3 ligase and then induce its self-degradation, while general PROTACs for tagged fusion proteins can bind to general tags(such as HaloTag and FKBP12) and then induce the degradation of fusion proteins.

PROTAC Isoform Specific Products:

  • von Hippel-Lindau (VHL)

  • cIAP1

PROTAC 相关产品 (7):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-137516
    LC-2 2502156-03-6
    LC-2 是首创的内源性 KRAS G12C 的 PROTAC 降解剂,DC50 在 0.25 和 0.76 μM 之间。LC-2 是一种 PROTAC,与 MRTX849 共价结合 KRAS G12C 并招募 E3 连接酶 VHL,诱导 KRAS G12C 快速持续降解,导致纯合和杂合子 KRAS G12C 细胞系 MAPK 信号的抑制。
    LC-2
  • HY-128359
    ACBI1 2375564-55-7 98.21%
    ACBI1 是一种有效的,基于 PROTAC 技术的 BAF ATPase 亚基 SMARCA2SMARCA4 降解剂,也是 PBAF 成员 PBRM1 的降解剂, 对 SMARCA2、SMARCA4 和 PBRM1 作用的 DC50 值分别为 6 nM、11 nM 和 32 nM。ACBI1 由一个 bromodomain 配体、linker 和 E3 泛素连接酶 VHL 构成,能诱导抗增殖作用和凋亡。
    ACBI1
  • HY-114322
    VZ185 2306193-61-1
    VZ185 是高效,快速,选择性的 BRD7/9 PROTAC 降解剂,DC50 分别为 4.5 和 1.8 nM。VZ185对 EOL-1 和 A-402 细胞具有细胞毒性,EC50 分别为 3nM 和 40nM。
    VZ185
  • HY-111848A
    PROTAC AR Degrader-4 TFA ≥98.0%
    PROTAC AR Degrader-4 包含 cIAP1 配体结合基团,linker 和雄激素受体 (AR) 配体结合基团。基于 cIAP1 的降解剂也被称为 SNIPER
    PROTAC AR Degrader-4 TFA
  • HY-136250
    BSJ-03-204 2349356-09-6 98.34%
    BSJ-03-204 是一种有效的,选择性的基于 Palbociclib (HY-50767) 的 CDK4/6 双重降解剂 (PROTAC),对 CDK4/D1 和 CDK6/D1 的 IC50 分别为 26.9 nM 和 10.4 nM。BSJ-03-204 不诱导 IKZF1/3 降解,具有抗癌活性。
    BSJ-03-204
  • HY-133737
    PROTAC BRD4 Degrader-5 2409538-70-9 99.51%
    PROTAC BRD4 Degrader-5 是一种基于 PROTAC 的 BRD4 降解剂,可有效降解 HER2 阳性和阴性乳腺癌细胞系中的 BRD4
    PROTAC BRD4 Degrader-5
  • HY-111848
    PROTAC AR Degrader-4 1351169-31-7
    PROTAC AR Degrader-4 包含 cIAP1 配体结合基团,linker 和雄激素受体 (AR) 配体结合基团。基于 cIAP1 的降解剂也被称为 SNIPER
    PROTAC AR Degrader-4
Isoform Specific Products

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