1. Signaling Pathways
  2. PROTAC
  3. PROTACs

PROTACs

PROTAC (PROteolysis-TArgeting Chimera) is a heterobifunctional nanomolecule containing two different ligands, ligand for ubiquitin E3 and ligand for target protein. The two parts are connected by linker to form a "three-unit" polymer, target protein ligand-linker-E3 ligase ligand. Building blocks of PROTAC molecules include PROTAC Linker, Ligand for Target Protein for PROTAC, Ligand for E3 Ligase, E3 Ligase Ligand-Linker Conjugate, Target Protein Ligand-Linker Conjugate, etc.

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-114323
    PROTAC FLT-3 degrader 1 2230826-81-8 99.19%
    PROTAC FLT-3 degrader 1 is an effective and selective FLT-3 PROTAC degrader with an IC50 of 0.6 nM. PROTAC FLT-3 degrader 1 inhibits both FLT-3 and FLT-3 ITD mutants. PROTAC FLT-3 degrader 1 has the activity of anti-proliferation and induction of apoptosis, which can be used in the study of tumor.
    PROTAC FLT-3 degrader 1
  • HY-111593
    Homo-PROTAC pVHL30 degrader 1 2244684-49-7 99.40%
    Homo-PROTAC pVHL30 degrader 1 is a potent pVHL30 degrader based on PROTAC, consists of two ligands of von Hippel-Lindau.
    Homo-PROTAC pVHL30 degrader 1
  • HY-149480
    ERD-3111 2832865-25-3 98.72%
    ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer.
    ERD-3111
  • HY-129966
    PROTAC IRAK4 degrader-1 2360533-90-8 99.77%
    PROTAC IRAK4 degrader-1 (compound I-210) is a Cereblon-based IRAK4 PROTAC degrader.
    PROTAC IRAK4 degrader-1
  • HY-112718
    PROTAC BET Degrader-10 1957234-97-7 99.39%
    PROTAC BET Degrader-10 (dBET37) is a potent BET protein BRD4 degrader, connected by ligands for Cereblon and BRD4, with a DC50 of 49 nM.
    PROTAC BET Degrader-10
  • HY-151613A
    MS15 TFA 99.82%
    MS15 TFA is a potent and selective AKT PROTAC degrader. MS15 TFA inhibits the AKT1, -2, and -3 activities, with IC50 values of 798 nM, 90 nM, and 544 nM, respectively.
    MS15 TFA
  • HY-112156
    MS4077 2230077-10-6 99.66%
    MS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 37 nM for binding affinity to ALK.
    MS4077
  • HY-122653A
    CCT367766 formic 98.10%
    CCT367766 formic is a potent and the third generation heterobifunctional and Cereblon-based pirin targeting protein degradation probe (PDP, or PROTAC), depletes pirin protein expression at low concentration. CCT367766 formic exhibits a moderate affinity for the CRBN-DDB1 complex with an IC50 value of 490 nM. CCT367766 formic reveals a good affinity for the recombinant pirin and CRBN with Kd values of 55 nM and 120 nM, respectively. CCT367766 formic provides a potential chemical tool to study a largely unexplored protein.
    CCT367766 formic
  • HY-137346
    DD-03-156 2769753-69-5 99.90%
    DD-03-156 is a potent and selective degrader of CDK17 and LIMK2. DD-03-156 is exquisite and makes an advanced starting point for the development of a chemical probe for the degradation of CDK17.
    DD-03-156
  • HY-158684
    YX-02-030 3049076-98-1 99.86%
    YX-02-030 is a VHL-dependent MDM2 PROTAC degrader with a Kd of 35 nM. YX-02-030 recruits the VHL E3 ligase to form a ternary complex, leading to ubiquitination and proteasome-mediated degradation of MDM2. YX-02-030 inhibits MDM2-p53 and VHL-HIF1α binding with IC50 values of 63 and 1350 nM. YX-02-030 activates TAp73, upregulates p53 family target genes and induces apoptosis. YX-02-030 demonstrates on-target efficacy in TNBC xenograft-bearing mice, extending survival without normal cell toxicity.
    YX-02-030
  • HY-170859
    AH078 3110370-06-1 99.73%
    AH078 is a PROTAC-based CK1δ/ε degrader (DC50=0.55 μM, Dmax=70%) that lacks subtype selectivity between CK1δ and CK1ε. AH078 induces target protein degradation either by recruiting the CUL4-CRBN E3 ligase complex and proteasome, or via the VHL- and ubiquitin-dependent pathway. AH078 also exhibits selectivity for CK1α, and is widely applicable to research related to colon cancer, pancreatic cancer, breast cancer, ovarian cancer, chronic lymphocytic leukemia, acute myeloid leukemia, glioma, and metastatic breast adenocarcinoma.
    AH078
  • HY-143275
    HL-8 2766352-64-9 99.17%
    HL-8 is a PI3Kα PROTAC degrader. HL-8 promotes the ubiquitination and degradation of PI3Kα. HL-8 reduces pAKT levels. HL-8 has anticancer activity against colon and cervical cancer (Pink: PI3Kα ligand (HY-143277); Blue: E3 ligase VHL ligand (HY-138678); Black: linker (HY-W002042)).
    HL-8
  • HY-173333
    PROTAC SMARCA2/4 degrader-38 3081688-77-6 99.46%
    PROTAC SMARCA2/4 degrader-38 is a degrader SMARCA2/4 PROTAC (DC50: 3.0 nM and 4.0 nM respectively). PROTAC SMARCA2/4 degrader-38 promotes the ubiquitination and degradation of SMARCA2/4. PROTAC SMARCA2/4 degrader-38 blocks the G0/G1 cell cycle and induces apoptosis. PROTAC SMARCA2/4 degrader-38 can be used in acute myeloid leukemia (AML) research. (Pink: SMARCA2/4 ligand; Blue: VHL ligand (HY-112078); Black: linker; Target Protein Ligand-Linker Conjugates (HY-173343)).
    PROTAC SMARCA2/4 degrader-38
  • HY-153796
    PROTAC Her3 Degrader-8 2103331-95-7 99.60%
    PROTAC Her3 Degrader-8 (Compound PP2) is a Her3 PROTAC degrader. PROTAC Her3 Degrader-8 promotes the ubiquitination and degradation of Her3. PROTAC Her3 Degrader-8 can be used in the study of lung adenocarcinoma and ovarian cancer.
    PROTAC Her3 Degrader-8
  • HY-149295
    PROTAC ERα Degrader-4 2521299-80-7 99.06%
    PROTAC ERα Degrader-4 (Compound ZD12) is a highly potent and selectivePROTAC ERα degrader (Ki: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER+ breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.
    PROTAC ERα Degrader-4
  • HY-147330B
    SJ1008030 formic 98.91%
    SJ1008030 (compound 8) formic is a JAK2 PROTAC which selectively degrades JAK2. SJ1008030 formic inhibits MHH–CALL-4 cell growth with an IC50 of 5.4 nM. SJ1008030 formic can be used for the research of leukemia.
    SJ1008030 formic
  • HY-144304
    PROTAC EGFR degrader 2 3031336-58-7
    PROTAC EGFR degrader 2 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 2 exhibits excellent antiproliferative activity with IC50 of 4.0 nM and good EGFR degradation activity with DC50 of 36.51 nM. PROTAC EGFR degrader 2 can be used for the synthesis of nitroreductase (NTR)-responsive PROTAC.
    PROTAC EGFR degrader 2
  • HY-137342
    SB1-G-187 2769753-18-4 98.70%
    SB1-G-187 is a multi-target kinase PROTAC degrader with activity against various kinases including GCK, YES1, IRAK1 and LYN. SB1-G-187 induces degradation of target kinases via a p97-dependent pathway, and forms ternary complexes with CRBN and specific functional kinases. SB1-G-187 can be used in tumor-related research.
    SB1-G-187
  • HY-148290
    KTX-951 2573298-36-7 99.60%
    KTX-951 is an orally active IRAK4 and IMiD (Ikaros/Aiolos) substrates PROTAC degrader (Kd = 3.5 nM). KTX-951 has DC50s of 13 nM, 14 nM and 13 nM for IRAK4, Ikaros and Aiolos, respectively. KTX-951 has IC50 of 35 nM for OCl-Ly10 CTG. KTX-951 has antitumor activity.
    KTX-951
  • HY-176428
    PROTAC MNK1 degrader-1 3120743-91-8 98.93%
    PROTAC MNK1 degrader-1 is a selective MNK1 PROTAC degrader with a DC50 of 11.92 nM, and a Dmax > 96% in MV4-11 cells. PROTAC MNK1 degrader-1 significantly reduces p-eIF4E (IC50: 22.07 nM), induces apoptosis, and arrests the cell cycle at the G1 phase. PROTAC MNK1 degrader-1 has potent antitumor activity. PROTAC MNK1 degrader-1 has robust antileukemic efficacy in MV4-11 xenograft mice model with acceptable drug safety. Pink: MNK1 ligand (HY-176429); Blue: CRBN ligase ligand (HY-A0003); Black: linker (HY-Y1139); CRBN + linker: HY-176430
    PROTAC MNK1 degrader-1
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