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
-
PROTACs Related Products (1398)
Related Products (1398)
-
Antibodies (1)
-
PROTACs Isoform Comparison
-
PROTAC BRD4 Degrader-17
0 ImagesCat. No.: HY-143328CAS No.: 2585561-49-3PROTAC BRD4 Degrader-17 (compound 13i) is a potent PROTAC BRD4 Degrader, with IC50 values of 29.54 nM (BRD4 (BD1)) and 3.82 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-17 significantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-17 significantly induces apoptosis in MV-4-11 cells.
-
PROTAC TTK degrader-2
0 ImagesCat. No.: HY-143905CAS No.: 2953426-48-5PROTAC TTK degrader-2 is a threonine tyrosine kinase (TTK) PROTAC degrader with a DC50 of 3.1 nM in COLO-205 cells. PROTAC TTK degrader-2 induces proteasome-mediated degradation of TTK. It inhibits the proliferation of colorectal cancer cells. In colorectal cancer xenograft mouse models, PROTAC TTK degrader-2 mediates target degradation and exerts anticancer activity. PROTAC TTK degrader-2 can be used in colorectal cancer-related research.
-
PROTAC CB1R Degrader-1
0 ImagesCat. No.: HY-178176PROTAC CB1R Degrader-1 is a potent and selective CB1R PROTAC degrader that exploits the ubiquitin-proteasome system (UPS) achieving a DC50 of 3.37 μM in MCF-7 cells and showing no impact on CB2R. PROTAC CB1R Degrader-1 reduces CB1R-associated downstream signaling (p-AKT, p-ERK, BCL2, and MCM5), thereby inhibiting breast cancer cell proliferation and inducing apoptosis. PROTAC CB1R Degrader-1 can be used for breast cancer research.
-
PROTAC HDAC8 Degrader-1
0 ImagesCat. No.: HY-163920CAS No.: 3057302-08-3
-
(Rac)-Vepdegestrant
0 ImagesCat. No.: HY-138642ACAS No.: 2229711-08-2Synonyms: (Rac)-ARV-471; (Rac)-PF-07850327(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 AR Degrader-10
0 ImagesCat. No.: HY-173372PROTAC AR Degrader-10 is a potent cereblon (CRBN)-recruited androgen receptor (AR) PROTAC degrader. PROTAC AR Degrader-10 exhibits high AR degradation activity and can be applied to research related to prostate cancer.
-
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).
-
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.
-
NCP07
0 ImagesCat. No.: HY-187225NCP07 is a PROTAC degrader targeting the coactivator-binding site (CBS) of ERα. NCP07 induces the formation of the ERα-NCP07-VHL ternary complex and promotes ERα degradation via the ubiquitin-proteasome system. NCP07 induces apoptosis and cell cycle arrest in endocrine therapy-resistant breast cancer cells. NCP07 inhibits the proliferation of wild-type and ESR1-mutant breast cancer cells. NCP07 is applicable to breast cancer-related 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.
