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-114229
    PROTAC BET degrader-3 3031993-61-7 98.77%
    PROTAC BET Degrader-3 is a PROTAC connected by ligands for von Hippel-Lindau and BET.
    PROTAC BET degrader-3
  • HY-175751
    LRK-4189 3063346-83-5
    LRK-4189 (Compound 319) is an orally active and selective PIP4K2C PROTAC degrader with a DC50 < 500 nM for PIP4K2C in MOLT-4 cells. LRK-4189 has an antitumor activity and induces intrinsic cell death and activates interferon signaling, therefore triggering immune-mediated tumor killing in immune-inert microsatellite stable (MSS) CRC cells. LRK-4189 can be used for cancers like MSS colorectal carcinoma research.
    LRK-4189
  • HY-162259
    QC-182 3032646-96-8
    QC-182 is a potent PROTAC degrader of p300/CBP. QC-182 reduces p300 protein in the SK-HEP-1 cells (DC50 = 93nM). QC-182 potently and effectively inhibits cell growth in the SK-HEP-1 and JHH7 cell lines with IC50 values of 0.733 and 0.477 μM, respectively. QC-182 can be used for the research of hepatocellular carcinoma (HCC).
    QC-182
  • HY-139707
    Thalidomide-NH-CBP/p300 ligand 2 2484739-21-9 98.55%
    Thalidomide-NH-CBP/p300 ligand 2 (P-007) is a PROTAC-based CBP and p300 degrader (extracted from patent WO2020173440).
    Thalidomide-NH-CBP/p300 ligand 2
  • HY-168221
    YD54 2951015-30-6
    YD54 is a PROTAC based SMARCA2 degrader with a DC50 of 3.5 nM (Red: SMARCA2 degrader (HY-44012B), black: linker, Blue: E3 ligase ligand).
    YD54
  • HY-157579
    MS154N 2675490-97-6 99.30%
    MS154N (compound 28) is the negative control of MS39 (HY-157581). MS154N is composed of PROTAC target protein ligand EGFR ligand-11 (HY-168305) (red part), E3 ligase ligand 4-Hydroxy-2-(1-methyl-2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione (HY-W441376) (blue part) and PROTAC Linker 8-Iodooctan-1-amine (HY-168306) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is Me-Thalidomide-O-C8-NH2 (HY-168307).
    MS154N
  • HY-170669
    PROTAC XPO1 degrader-1
    PROTAC XPO1 degrader-1 (Compound 2c) is an XPO1 degrader. PROTAC XPO1 degrader-1 exhibits anti-proliferative effects, can induce cell apoptosis, inhibit NF-κB activity, and cause cell cycle arrest in the G1 phase. PROTAC XPO1 degrader-1 can be used in research on hematological malignancies (Pink: Target Protein Ligand (HY-170672); Black: Linker (HY-W010525); Blue: E3 Ligase Ligand (HY-170671); E3 Ligase Ligand-Linker Conjugate (HY-170673)).
    PROTAC XPO1 degrader-1
  • HY-160142
    UBX-382 2884554-45-2
    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-168574
    SZU-B6 3059333-98-8 98.78%
    SZU-B6 is a PROTAC degrader for SIRT6 with DC50 of 45 nM and 154 nM in cell SK-HEP-1 and Huh-7. SZU-B6 inhibits the proliferation of cell SK-HEP-1 with an IC50 of 1.51 μM, inhibits the colony formation of SK-HEP-1 and Huh-7, induces apoptosis and arrests the cell cycle at G2/M phase in SK-HEP-1. SZU-B6 exhibits antitumor efficacy in mouse model. (Pink: ligand for target protein (HY-16605); Black: linker (HY-W012935); BLue: ligand for E3 ligase (HY-W453548)
    SZU-B6
  • HY-114324A
    rel-PROTAC PARP1 degrader 98.99%
    rel-PROTAC PARP1 degrader is the relative configuration of ROTAC PARP1 degrader (HY-114324). ROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.
    rel-PROTAC PARP1 degrader
  • HY-137340
    WH-10417-099 2769753-42-4 98.14%
    WH-10417-099 is a CRBN-type PROTAC multi-kinase degrader that can jointly induce the degradation of the largest number of unique kinases (more than 125 unique kinases). WH-10417-099 induces protein degradation through the ubiquitin biotinylation (E-STUB) pathway and consists of the target protein ligand (red part) PI3Kγ ligand 1 (HY-168319), the E3 ubiquitin ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547) and the PROTAC linker (black part) Amino-PEG5-C2-acid (HY-115384). The E3 ligase ligand and linker can form a conjugate Pomalidomide 4'-PEG5-acid (HY-131647).
    WH-10417-099
  • HY-160966
    PROTAC BTK Degrader-10 2988804-46-0 99.24%
    PROTAC BTK Degrader-10 (Example 1P) is a PROTAC degrader for BTK. PROTAC BTK Degrader-10 can be used for research of chronic lymphocytic leukemia (CLL)(Pink: ligand for target protein (HY-170758); Black: linker (HY-W392857); Blue: ligand for E3 ligase Cereblon (HY-W733176))
    PROTAC BTK Degrader-10
  • HY-156568A
    SMD-3040 TFA 99.90%
    SMD-3040 TFA is a potent and selective SMARCA2 PROTAC degrader (DC50: 12 nM; Dmax: 91%). SMD-3040 TFA can inhibit tumor cell proliferation and exhibits antitumor activity. SMD-3040 TFA can be used in the study of tumors such as melanoma. (SMARCA2/4-ligand (HY-171765); HY-112078 VHL ligand (HY-112078))
    SMD-3040 TFA
  • HY-155356
    YN14
    YN14 is a KRASG12C proteolysis targeting chimera (PROTAC). YN14 is highly potent and selective KRASG12C degrader and induces a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). YN14 has antiproliferative effects and significantly inhibits KRASG12C-mutant cancer cell growth. YN14 leads to tumor regression with tumor growth inhibition (TGI%) rates more than 100 % in the MIA PaCa-2 xenograft model.
    YN14
  • HY-163938
    PROTAC erf3a Degrader-1 3033871-19-8 99.44%
    PROTAC erf3a Degrader-1 (Compound C63) is an orally active PROTAC erf3a Degrader. PROTAC erf3a Degrader-1 inhibits cancer cell proliferation (eg: 22Rv1). PROTAC erf3a Degrader-1 can be used for research of prostate cancer, ovarian cancer, liver cancer, cervical cancer, leukemia, breast cancer. (Red: erf3a ligand (HY-13778); Black: linker (HY-163960); Blue: CRBN ligand (HY-41547)).
    PROTAC erf3a Degrader-1
  • HY-146393
    PROTAC CYP1B1 degrader-1 2411389-67-6 98.09%
    PROTAC CYP1B1 degrader-1 (Compound 6C), a α-naphthoflavone chimera derivative, is able to eliminate cytochrome P450 (CYP)1B1-mediated agent resistance via targeted CYP1B1 degradation, with IC50s of 95.1 and 9838.6 nM for CYP1B1 and CYP1A2, respectively. PROTAC CYP1B1 degrader-1 can be used for the research of CYP1B1-overexpressing prostate cancer.
    PROTAC CYP1B1 degrader-1
  • HY-161410
    WH244 2941088-96-4 99.82%
    WH244 is a second generation BCL-2 and BCL-xL dual depressant (PROTAC). The primary activity of WH244 is the specific degradation of BCL-2 and BCL-xL proteins (BCL-xL: DC50=0.6 nM, BCL-2: DC50=7.4 nM). WH244 promotes their ubiquitination and subsequent proteasome degradation by targeting these proteins, thereby restoring the cell's apoptosis pathway. WH244 has good antitumor activity. (Pink: BCL-2/BCL-xL ligand (HY-161415); Blue: E3 ligase ligand (HY-112078); Black: linker).
    WH244
  • HY-171769
    dAurAB2
    dAurAB2 is a dual-degrading PROTAC that potently degrades Aurora-A and Aurora-B with DC50s of 59 nM and 39 nM, respectively. dAurAB2 reduces N-Myc levels in MYCN-amplified IMR32 neuroblastoma cells. dAurAB2 can be used for the study of neuroblastoma. (Pink, Aurora ligand (HY-10804); Blue, E3 ligand: (HY-103597); Black, linker (HY-W105740)).
    dAurAB2
  • HY-161615
    PROTAC ATR degrader-2 3010273-12-5 99.73%
    PROTAC ATR degrader-2 (Compound 8i) is a PROTAC degrader for ATR, through of . PROTAC ATR degrader-2 degrades ATR in acute myeloid leukemia (AML) cells MV-4-11 and MOLM-13, with DC50 of 22.9 and 34.5 nM. APROTAC ATR degrader-2 induces apoptosis, inhibits proliferations of AML cells. PROTAC ATR degrader-2 exhibits good pharmacokinetics charachers and antitumor efficacy against AML in mouse model. (Pink: ATR ligand (HY-161616); Blue:E3 ligase ligand Lenalidomide (HY-A0003); Black: linker)
    PROTAC ATR degrader-2
  • HY-162537
    LYP-8 99.89%
    LYP-8 is a potent and effective NAMPT degrader with maximum degradation of 97% at 0.5 μM in SKOV-3 cells. LYP-8 shows anti-cancer activity in vivo and in vitro(Sturcture Note:(Blue: Cereblon ligand (HY-112078), Black: linker (HY-128801);Pink: Nampt inhibitor Nampt-IN-11 (HY-158689)).
    LYP-8
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