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.
PROTACs Isoform Specific Products
All Product Categories
-
PROTACs Related Products (1323)
Related Products (1323)
-
Antibodies (1)
-
PROTACs Isoform Comparison
-
(Rac)-Vepdegestrant
0 ImagesCat. No.: HY-138642ACAS No.: 2229711-08-2Synonyms: (Rac)-ARV-471(Rac)-Vepdegestrant is the isomer of Vepdegestrant (HY-138642). Vepdegestrant is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM.
-
PROTAC BRD3 degrader-1
0 ImagesCat. No.: HY-180889CAS No.: 2257497-15-5PROTAC BRD3 degrader-1 (compound D072) is a potent and selective PROTAC BRD3 degrader. PROTAC BRD3 degrader-1 selectively degrades BRD3 in mice, leading to the downregulation of H3K18ac without affecting BRD2 or BRD4. PROTAC BRD3 degrader-1 reduces intraocular inflammation in the experimental autoimmune uveitis (EAU) mouse mode and inhibits proinflammatory microglia in both uveitis retina and LPS (HY-D1056) treated mouse microglia cell line BV2. PROTAC BRD3 degrader-1 can be used for uveitis research.
-
PROTAC PI3Kα/δ degrader-1
0 ImagesCat. No.: HY-182083PROTAC PI3Kα/δ degrader-1 is an orally active PI3Kα/δ PROTAC degrader, with an IC50 of 0.34 nM for PI3Kα and 1.85 nM for PI3Kδ. PROTAC PI3Kα/δ degrader-1 inhibits the proliferation and migration of cancer cells, induces G1-phase cell cycle arrest and PI3Kα degradation. PROTAC PI3Kα/δ degrader-1 suppresses tumor growth in breast cancer xenograft mouse models. PROTAC PI3Kα/δ degrader-1 can be used for the research of breast cancer.
-
PROTAC GPX4 degrader-3
0 ImagesCat. No.: HY-161930PROTAC GPX4 degrader-3 is a glutathione peroxidase 4 (GPX4) PROTAC degrader with a DC50 of 0.019 μM in HT1080 cells. PROTAC GPX4 degrader-3 degrades GPX4 primarily via the ubiquitin-proteasome system (UPS) in a dose- and time-dependent manner. PROTAC GPX4 degrader-3 induces lipid peroxidation (LPO) and ROS accumulation, thereby triggering ferroptosis (ferroptosis). PROTAC GPX4 degrader-3 exhibits in vitro anti-tumor activity against cancer cells. PROTAC GPX4 degrader-3 can be used in the research of fibrosarcoma, triple-negative breast cancer, and renal cell carcinoma.
-
TKP-5
0 ImagesCat. No.: HY-182370CAS No.: 3076612-97-7TKP-5 is a PROTAC protein degrader targeting BRD4. TKP-5 can binds to BRD2, BRD3, BRD4 and BRDT, with Kd values of 150 nM, 100 nM and 150 nM for the first three proteins respectively. TKP-5 inhibits the production of thymic stromal lymphopoietin and suppresses the expression of IL-33 mRNA. TKP-5 is applicable to studies related to tape-stripping induced skin injury.
-
Leu-PEG1-Dasa
0 ImagesCat. No.: HY-180925CAS No.: 3037776-72-7Leu-PEG1-Dasa is a potent BCR-ABL PROTAC degrader with a DC50 of 0.48 nM. Leu-PEG1-Dasa uses a single amino acid as the E3 ligand and belongs to a mini-PROTAC, functioning through the N-terminal canonical pathway. Leu-PEG1-Dasa exhibits potent anti-proliferative activity against K562 cells. Leu-PEG1-Dasa can be used for the study of chronic myeloid leukemia (CML).
-
FDU73
0 ImagesCat. No.: HY-173125FDU73 is a highly effective and selective BTK PROTAC degrader with a DC50 of 2.9 nM (in JeKo-1 cells). FDU73 can inhibit the proliferation of tumor cells and exhibits anti-tumor activity. (Pink: BTK ligand-14 (HY-173126); Black: Linker (HY-168297); Blue: E3 ligase ligand 59 (HY-173378); E3 ligase ligand+Linker (HY-173127))
-
PROTAC BRD9 Degrader-2
0 ImagesCat. No.: HY-145395CAS No.: 2633631-78-2
-
PROTAC ERα Degrader-13
0 ImagesCat. No.: HY-178961PROTAC ERα Degrader-13 is an orally active PROTAC molecule that efficiently and selectively degrades ERα (DC50 = 3.78 nM). PROTAC ERα Degrader-13 has the characteristics of strong anti proliferation (IC50 = 0.6 nM), induction of apoptosis, and overcoming drug resistance in MCF-7 cells. PROTAC ERα Degrader-13 has good safety and no significant organ toxicity. PROTAC ERα Degrader-13 can be used for cancer research.
-
PF15
0 ImagesCat. No.: HY-143286CAS No.: 2892631-70-6PF15 is an orally active FLT3-ITD PROTAC degrader with a DC50 of 76.7 nM and an IC50 of 36 nM against FLT3-ITD. PF15 induces FLT3-ITD protein degradation, thereby downregulating its phosphorylation level. PF15 inhibits the proliferation of FLT3-ITD-positive cells and reduces the phosphorylation level of STAT5, a downstream molecule of FLT3-ITD. PF15 exhibits efficacy in in vivo xenograft models of acute myeloid leukemia and prolongs survival. PF15 can be used for the research of acute myeloid leukemia.
-
PROTAC EGFR degrader 13
0 ImagesCat. No.: HY-158313CAS No.: 2861227-35-0PROTAC EGFR degrader 13 (compound 106) is an EGFR PROTAC degrader with a DC50 of <0.1 μM. PROTAC EGFR degrader 13 has proliferation inhibitory activity on cell Ba/F3-TEL-EGFR-T790M-L858R-C797S with an IC50 of 15.6 nM. PROTAC EGFR degrader 13 can be used for the study of EGFR-related diseases such as cancer.
-
PROTAC NSD2 degrader-1
0 ImagesCat. No.: HY-184968CAS No.: 3108071-48-0PROTAC NSD2 degrader-1 is a PROTAC degrader that selectively targets NSD2, with a DC50 of 0.37 μM. PROTAC NSD2 degrader-1 induces selective degradation of long and short isoforms of NSD2 containing the PWWP1 domain by forming a ternary complex with FBXO22. NSD2 degradation mediated by PROTAC NSD2 degrader-1 depends on the ubiquitin-proteasome system and the neddylation pathway. PROTAC NSD2 degrader-1 can be used in cancer-related research such as non-small cell lung cancer, multiple myeloma and prostate cancer.
-
ZSH-2117
0 ImagesCat. No.: HY-174415ZSH-2117 is a covalent and selective EGFR PROTAC degrader with a DC50 of 45 nM in Ba/F3-EGFRL858R/T790M/C797S cells. ZSH-2117 significantly inhibits cell proliferation and reduces the downstream EGFR signaling proteins level of AKT and ERK. ZSH-2117 effectively inhibits tumor growth in Ba/F3-EGFRL858R/T790M/C797S xenograft mice model.
-
P1D-34
0 ImagesCat. No.: HY-171334AP1D-34 is a Pin1 PROTAC degrader with a DC50 value of 177 nM. P1D-34 also down-regulates Pin1 client proteins such as Cyclin D1, Rb, Mcl-1, Akt, and c-Myc. P1D-34 shows anti-proliferative activities in a panel of acute myeloid leukemia (AML) cell lines. P1D-34 induces cell DNA damage and apoptosis by releasing ROS generation. Pink: PIN1 ligand (HY-171442A), Blue: CRBN ligand (HY-14658), Black: Linker (HY-W014883).
-
PROTAC SMARCA2 degrader-21
0 ImagesCat. No.: HY-169272CAS No.: 2891464-61-0
-
PROTAC IKKβ/NR4A1 degrader-1
0 ImagesCat. No.: HY-179112CAS No.: 2826215-20-5PROTAC IKKβ/NR4A1 degrader-1 is a highly efficient and effective dual-PROTAC degrader targeting IKKβ and NR4A1. PROTAC IKKβ/NR4A1 degrader-1 can increase the levels of caspase 3 and cleaved caspase 3 proteins, while the necroptosis marker RIP kinase remained unchanged, indicating that it can induce apoptosis. PROTAC IKKβ/NR4A1 degrader-1 can be used for the study of Acute myeloid leukemia (AML). Red: IKKβ/NR4A1 ligand (HY-13067); Blue: E3 ligase CRBN ligand (HY-14658); Black: Linker (HY-79577).
-
PROTAC SMARCA2 degrader-17
0 ImagesCat. No.: HY-162747CAS No.: 2568276-43-5
-
PROTAC HSP70 Degrader-1
0 ImagesCat. No.: HY-181147PROTAC HSP70 Degrader-1 (compound C4) is a cytosolic HSP70 PROTAC degrader that can engage CRBN to form a ternary complex. PROTAC HSP70 Degrader-1 mediates ubiquitination and proteasomal degradation of cytosolic HSP70. PROTAC HSP70 Degrader-1 exhibits cytotoxic activity against cancer cells, suppressing tumor cell proliferation and inducing apoptosis in combination with DTHIB. PROTAC HSP70 Degrader-1 can be used for the research of colon cancer and leukemia.
