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 (1334)
Related Products (1334)
-
Antibodies (1)
-
PROTACs Isoform Comparison
-
PROTAC CYP1B1 degrader-2
0 ImagesCat. No.: HY-158429CAS No.: 2836297-26-6PROTAC CYP1B1 degrader-2 is a CYP1B1 PROTAC degrader with a DC50 of approximately 0.1 nM. PROTAC CYP1B1 degrader-2 induces ubiquitination and proteasomal degradation of CYP1B1, and forms a ternary complex with VHL ubiquitin ligase and CYP1B1. PROTAC CYP1B1 degrader-2 inhibits P-gp. PROTAC CYP1B1 degrader-2 inhibits FAK/SRC. PROTAC CYP1B1 degrader-2 exhibits anticancer activity against paclitaxel (HY-B0015)-resistant non-small cell lung cancer. PROTAC CYP1B1 degrader-2 can be used in studies related to non-small cell lung cancer.
-
PROTAC PDIA1 degrader 1
0 ImagesCat. No.: HY-178118CAS No.: 3024292-21-2PROTAC PDIA1 degrader 1 (Compound H4) is a PDIA1 PROTAC degrader with a DC50 of 29.71 μM. PROTAC PDIA1 degrader 1 has potent anticancer activity and significantly inhibits cancer cell proliferation. Pink: PDIA1 ligand (HY-100433); Blue: CRBN ligase ligand (HY-10984); Black: linker (HY-W015088)
-
PROTAC SMARCA2/4 degrader-1
0 ImagesCat. No.: HY-159452CAS No.: 2568273-68-5SMARCA2/4-degrader-1 (compound I-430) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC50s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment.
-
PROTAC SOS1 degrader-1
0 ImagesCat. No.: HY-145737CAS No.: 2913185-35-8PROTAC SOS1 degrader-1 is a degrader of SOS1 PROTAC, with a DC50 of 98.4 nM and a Kd value of 44 nM. PROTAC SOS1 degrader-1 induces the formation of a ternary complex with SOS1 and the VCB E3 ubiquitin ligase complex, thereby promoting the ubiquitination and proteasomal degradation of SOS1. PROTAC SOS1 degrader-1 reduces KRAS-GTP levels, inhibits the phosphorylation of ERK in the RAS-RAF-MEK-ERK pathway, and suppresses the proliferation of cancer cells carrying KRAS mutations. PROTAC SOS1 degrader-1 inhibits tumor growth in mouse xenograft models. PROTAC SOS1 degrader-1 can be used for the research of KRAS-driven cancers.
-
PROTAC PXR degrader-1
0 ImagesCat. No.: HY-169279PROTAC PXR degrader-1 is a PROTAC degrader targeting PXR, with a DC50 value of 49.8 nM in SNU-C4 3xFLAG-PXR KI cells. PROTAC PXR degrader-1 exhibits selectivity towards CAR, VDR, FXR, LXRα and LXRβ. PROTAC PXR degrader-1 induces the formation of a ternary complex with PXR and VHL, triggering proteasomal degradation of PXR. PROTAC PXR degrader-1 reduces both agonist-induced and basal PXR-mediated CYP3A4 promoter activation, and decreases the expression of endogenous CYP3A4 gene in cancer cells. PROTAC PXR degrader-1 enhances the cytotoxic effect of paclitaxel on cancer cells. PROTAC PXR degrader-1 can be used for the research of colorectal cancer.
-
XM-U-14
0 ImagesCat. No.: HY-159175CAS No.: 3098519-83-3XM-U-14 is a selective PROTAC USP7 Degrader (DC50: 0.74 nM in inducing USP7 degradation in RS4;11 cell line). XM-U-14 upregulates the levels of p53 and p21. XM-U-14 also significantly inhibits acute lymphoblastic leukemia (ALL) cell growth (IC50: 0.5 nM and 8.3 nM for RS4;11 cells and Reh cells respectively). XM-U-14 induces apoptosis and cycle arrest. XM-U-14 inhibits tumor growth. (Blue: VHL ligand (HY-159465), Black: linker (HY-W539783); Pink: USP7 inhibitor (HY-159464)).
-
CPP-13
0 ImagesCat. No.: HY-187176CPP-13 is a selective PARP1 PROTAC degrader with a DC50 of 0.48 nM. CPP-13 induces CRBN-dependent ubiquitination and proteasomal degradation of PARP1. CPP-13 induces DNA damage. CPP-13 inhibits the growth of BRCA-deficient breast cancer and pancreatic cancer. CPP-13 can be used in studies related to BRCA-deficient breast cancer and BRCA-deficient pancreatic cancer.
-
PROTAC BET Degrader-14
0 ImagesCat. No.: HY-179588PROTAC BET Degrader-14 is a highly efficient PROTAC targeting BET (bromodomain and extra-terminal domain). PROTAC BET Degrader-14 can degrade all BET (BRD2, BRD3, BRD4) family proteins. PROTAC BET Degrader-14 potently degrades BET proteins in U2OS osteosarcoma cell lines (BRD4 DC50 = 130 nM) and KYSE180 esophageal squamous cell carcinoma cell lines (DC50 = 40 nM). PROTAC BET Degrader-14’s dependence on the ubiquitin-proteasome system. PROTAC BET Degrader-14 decreases levels of BET-regulated gene products c-Myc, RUNX2, and KRT14. PROTAC BET Degrader-14 can be used for the study of osteosarcoma.
-
PROTAC FGFR2 degrader 2
0 ImagesCat. No.: HY-162626CAS No.: 3080487-43-7FGFR2 degrader 1 (compound 28E) is a selectively PROTACS degrader of FGFR2, with the DC50 of 0.645 nM. FGFR2 plays an important role in cancer research (Pink: ligand of target protein; (HY-13304) black: linker; blue: ligand of E3 ligase).
-
PROTAC PARP1 degrader-3
0 ImagesCat. No.: HY-168722PROTAC PARP1 degrader-3 is a PARP1 PROTAC degrader with a DC50 of 58.14 nM. PROTAC PARP1 degrader-3 promotes the ubiquitination and degradation of PARP1 via the ubiquitin-proteasome system. PROTAC PARP1 degrader-3 acts synergistically with SN-38 (HY-13704) to inhibit colorectal cancer. PROTAC PARP1 degrader-3 can be used in studies related to colorectal cancer.
-
PROTAC SMARCA2/4 degrader-2
0 ImagesCat. No.: HY-159453CAS No.: 2568277-76-7PROTAC SMARCA2/4 degrader-2 is a PROTAC degrader targeting SMARCA2 and SMARCA4, with a DC50 of < 100 nM for both proteins. PROTAC SMARCA2/4 degrader-2 induces ubiquitination and subsequent proteasome-mediated degradation of SMARCA2 and SMARCA4 proteins. PROTAC SMARCA2/4 degrader-2 can be used in cancer-related research.
-
SIAIS562055
0 ImagesCat. No.: HY-168637CAS No.: 3062106-15-1SIAIS562055 is a potent cereblon-based SOS1 PROTAC with a Kd of 95.9 nM. SIAIS562055 exhibits sustained degradation of SOS1 and inhibition of downstream ERK pathways. SIAIS562055 effectively blocked the binding of KRASG12C or KRASG12D to SOS1, with the IC50 values of 95.7 nM and 134.5 nM, respectively. SIAIS562055 exhibits potent anticancer activity.
-
PROTAC TG2 degrader-1
0 ImagesCat. No.: HY-155643CAS No.: 3033465-55-0PROTAC TG2 degrader-1 (compound 11) is a von Hippel-Lindau (VHL)-based PROTAC targeting tissue transglutaminase (TG2) with a KD of 68.9 μM. PROTAC TG2 degrader-1 reduces TG2 in ovarian cancer cells in a proteasome-dependent manner.
-
PROTAC ALK5 Degrader-1
0 ImagesCat. No.: HY-183785CAS No.: 3125240-35-6PROTAC ALK5 Degrader-1 is a selective ALK5 PROTAC degrader. PROTAC ALK5 Degrader-1 induces ALK5 degradation via ALK5 ATP-binding pocket engagement, CRBN recruitment, and the ubiquitin-proteasome system.PROTAC ALK5 Degrader-1 inhibits ALK5 downstream signaling. PROTAC ALK5 Degrader-1 can be used for the research of pulmonary fibrosis.
