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 MLLT1 Degrader-1
0 ImagesCat. No.: HY-181834CAS No.: 3111054-37-3PROTAC MLLT1 Degrader-1 is a PROTAC degrader targeting MLLT1. PROTAC MLLT1 Degrader-1 inhibits AML cell proliferation and viability, suppresses tumor growth in human AML xenograft models, and can block the oncogene transcriptional program. PROTAC MLLT1 Degrader-1 can be used for the research of MLL-rearranged acute myeloid leukemia (AML).
-
XYD129
0 ImagesCat. No.: HY-161710XYD129 is a CBP/p300 PROTAC degrader. XYD129 potently binds to CBP, p300 and CRBN proteins, with IC50 values of 0.021 μM, 0.03 μM and 0.18 μM, respectively. XYD129 forms a ternary CRBN-CBP/p300 complex and induces CBP/p300 degradation via the ubiquitin-proteasome system. XYD129 inhibits tumor growth and suppresses the proliferation of acute myeloid leukemia cells. XYD129 can be used in studies related to acute myeloid leukemia.
-
CW-10201
0 ImagesCat. No.: HY-189305CW-10201 is a KRASG12D and KRASG12V PROTAC degrader with DC50 values of 4.0 nM. CW-10201 induces ubiquitination and degradation of KRASG12D and KRASG12V. CW-10201 mildly inhibits pERK1/2. CW-10201 does not induce degradation of IKZF1 and GSPT1. CW-10201 exhibits anticancer activity against pancreatic cancer and colorectal cancer. CW-10201 can be used for research on pancreatic cancer and colorectal cancer.
-
PROTAC EGFR degrader 12
0 ImagesCat. No.: HY-171958CAS No.: 2654821-05-1PROTAC EGFR degrader 12 (example 1) is a PROTAC degrader targeting EGFR that can effectively degrade EGFR mutants, but has little effect on EGFR WT. PROTAC EGFR degrader 12 shows IC50s against EGFRL858R-T790M (NCI-H1975 cells), EGFRL858R (NCI-H3255 cells), and EGFRL858R-T790M-L797S (NCI-H1975+CS cells) of all <50 nM.
-
PROTAC SARS-CoV-2 Mpro degrader-4
0 ImagesCat. No.: HY-174233PROTAC SARS-CoV-2 Mpro degrader-4 is a SARS-CoV-2 MPro PROTAC degrader with antiviral activity, with a DC50 value of 4.7 μM. PROTAC SARS-CoV-2 Mpro degrader-4 induces MPro ubiquitination and proteasomal degradation, and inhibits SARS-CoV-2 replication. PROTAC SARS-CoV-2 Mpro degrader-4 can be used in the research of coronavirus infections.
-
PROTAC STAT3 degrader-2
0 ImagesCat. No.: HY-153023CAS No.: 2429877-78-9PROTAC STAT3 degrader-2 is a PROTAC degrader that targets STAT3, with a DC50 value of 3.54 μM. PROTAC STAT3 degrader-2 inhibits the growth of leukemia and lymphoma cells with high levels of phosphorylated STAT3. PROTAC STAT3 degrader-2 is used in the research of acute myeloid leukemia and anaplastic large cell lymphoma.
-
PROTAC AKR1C3 degrader-1
0 ImagesCat. No.: HY-163609PROTAC AKR1C3 degrader-1 is a PROTAC degrader targeting AKR1C3, with a DC50 of 52 nM. PROTAC AKR1C3 degrader-1 induces proteasome-dependent degradation of AKR1C3 and inhibits the enzymatic activities of AKR1C3, AKR1C1 and AKR1C2. PROTAC AKR1C3 degrader-1 degrades ARv7 by disrupting the stable AKR1C3/ARv7 complex. PROTAC AKR1C3 degrader-1 reduces the viability of prostate cancer cells expressing AKR1C3 and sensitizes Enzalutamide (HY-70002)-resistant prostate cancer cells. PROTAC AKR1C3 degrader-1 can be used in the research of prostate cancer.
-
PROTAC CDK9 degrader-12
0 ImagesCat. No.: HY-181231CAS No.: 3052648-82-2PROTAC CDK9 degrader-12 is a selective CDK9 PROTAC degrader with a DC50 of 23 nM. PROTAC CDK9 degrader-12 induces proteasome-dependent degradation of CDK9, blocks CDK9-mediated HIV-1 transcriptional elongation, and reduces HIV-1 RNA synthesis. PROTAC CDK9 degrader-12 is applicable to research related to HIV-1 infection.
-
PROTAC KSP degrader 1
0 ImagesCat. No.: HY-168725CAS No.: 3099825-86-9PROTAC KSP degrader 1 is a KSP PROTAC degrader with a DC50 of 114.8 nM. PROTAC KSP degrader 1 induces ubiquitination and degradation of KSP protein. PROTAC KSP degrader 1 induces G2/M phase arrest of the cell cycle. PROTAC KSP degrader 1 triggers Apoptosis. PROTAC KSP degrader 1 exhibits anticancer activity against colon cancer. PROTAC KSP degrader 1 can be used for the research of colon cancer, lung cancer and breast cancer.
-
JHK-02-102-1
0 ImagesCat. No.: HY-184913JHK-02-102-1 is a selective CDK5 degrader derived from the regorafenib kinase inhibitor scaffold. JHK-02-102-1 recruits CRL4CRBN E3 ubiquitin ligase to induce ternary complex formation between CDK5 and CRBN, triggering ubiquitin-proteasome system-dependent degradation. JHK-02-102-1 achieves selectivity redirection from CDK6 to CDK5 via subtle PROTAC architecture modifications.
-
PROTAC AR Degrader-13
0 ImagesCat. No.: HY-184195PROTAC AR Degrader-13 is a proteolysis-targeting chimera (PROTACs) that targets the androgen receptor (AR). PROTAC AR Degrader-13 has a DC50 of 0.90 nM in LNCaP cells and a DC50 of 0.23 nM in hDPC cells. PROTAC AR Degrader-13 induces AR degradation, downregulates TGF-β1 expression, upregulates β-catenin levels, and restores the Wnt/β-catenin pro-proliferation signaling in hair follicles. In a testosterone-induced androgenetic alopecia mouse model, PROTAC AR Degrader-13 accelerates hair regeneration rate, increases hair density and hair diameter. PROTAC AR Degrader-13 can be used for the research of androgenetic alopecia.
-
PROTAC HMGCR Degrader-2
0 ImagesCat. No.: HY-181134CAS No.: 2715104-46-2PROTAC HMGCR Degrader-2 is a HMGCR PROTAC degrader with an IC50 value of 0.25 μM. PROTAC degrades HMGCR-2 in Insig-silenced HepG2 cells with a DC50 of 0.12 μM. PROTAC HMGCR Degrader-2 takes PROTAC HMGCR Degrader-1 (HY-171823) as the oral prodrug. PROTAC HMGCR Degrader-2 degrades HMGCR by the VHL-dependent ubiquitin-proteasome system and reduces cellular cholesterol in HepG2 cells. PROTAC CDK2/4/6 Degrader-2 can be used for hyperlipidemia research.
-
M9101
0 ImagesCat. No.: HY-184193M9101 is a selective Aurora A PROTAC degrader with a DC50 of 2.3 nM. M9101 induces G2/M arrest in triple-negative breast cancer cells and potently inhibits the proliferation of multiple tumor cell lines. M9101 can be used in the research of various cancers including triple-negative breast cancer.
-
WB156
0 ImagesCat. No.: HY-174266CAS No.: 2368944-44-7WB156 is a dual MDM2 and GSPT1 PROTAC degrader with a DC50 of 23 nM against MDM2. WB156 induces the degradation of MDM2 and GSPT1 via the ubiquitin-proteasome system. WB156 upregulates the levels of p53 and p21, and triggers Apoptosis through the cleavage of PARP and Caspase-3. WB156 can be used in leukemia-related research.
-
NUCC-0227579
0 ImagesCat. No.: HY-184969NUCC-0227579 is a VHL-recruiting PROTAC degrader targeting CD73, with a DC50 of 0.32 μM. NUCC-0227579 synergistically mediates CD73 degradation through the ubiquitin-proteasome pathway and the lysosomal pathway. NUCC-0227579 inhibits the conversion of AMP to adenosine, abrogates adenosine-mediated immunosuppression, upregulates the activities of the NF-κB and NFAT pathways, and enhances the secretion, activation and proliferation levels of IFN-γ and TNF-α. NUCC-0227579 downregulates NAD+ synthesis in tumor cells, and inhibits the proliferation, migration and adhesion abilities of tumor cells under glutamine-deficient conditions. NUCC-0227579 significantly suppresses tumor growth in a humanized NSG mouse model of triple-negative breast cancer.
