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 (1355)
Related Products (1355)
-
Antibodies (1)
-
PROTACs Isoform Comparison
-
PROTAC sEH degrader-1
0 ImagesCat. No.: HY-159494PROTAC sEH degrader-1 is a PROTAC degrader targeting soluble epoxide hydrolase (sEH) with a DC50 of 0.5 nM, and it also possesses sEH inhibitory activity. PROTAC sEH degrader-1 has an IC50 of 3.8 nM against human sEH and an IC50 of 210 nM against mouse sEH. PROTAC sEH degrader-1 relies on the ubiquitin-proteasome system to achieve target protein degradation, and it selectively degrades cytoplasmic sEH. PROTAC sEH degrader-1 rapidly reduces endoplasmic reticulum stress in cells, downregulates the phosphorylation levels of IRE1α, PERK and eIF2α, enhances cell viability, and alleviates Thapsigargin (HY-13433)-induced apoptosis. PROTAC sEH degrader-1 effectively degrades sEH in mouse liver and brown adipose tissue. PROTAC sEH degrader-1 can be used in studies related to metabolic disorders and inflammation.
-
PROTAC IRAK4 degrader-14
0 ImagesCat. No.: HY-181708CAS No.: 3113890-51-7
-
BI01826025
0 ImagesCat. No.: HY-153574Synonyms: pArg-JQ1BI01826025 (pArg-JQ1) is a BacPROTAC-type bifunctional degrader that induces the degradation of BRDTBD1-containing substrates by recruiting the ClpC1P1P2 protease system. BI01826025 binds to the BRDTBD1 substrate via its JQ1 moiety and to ClpC1 via its pArg moiety; it delivers the substrate to ClpC1, where the substrate undergoes ClpC1-mediated unfolding followed by proteolysis by ClpP1P2. BI01826025 can be used to study ClpC1P1P2-mediated targeted protein degradation and ClpC2-regulated bacterial protein homeostasis.
-
PROTAC SMARCA2/4 degrader-3
0 ImagesCat. No.: HY-159454CAS No.: 2568507-10-6
-
EC21
0 ImagesCat. No.: HY-184678EC21 is a PROTAC degrader that binds to CDK6, thereby targeting EYA2 for degradation. EC21 enhances the interaction between CDK6 and EYA2, thereby driving ubiquitin-proteasome-dependent degradation of EYA2. EC21 reduces EYA2 protein levels in tumor tissues without obvious toxicity. EC21 disrupts the DNA damage repair pathway and inhibits cancer cell proliferation. EC21 can be used in breast cancer-related research.
-
PROTAC SMARCA2 degrader-5
0 ImagesCat. No.: HY-159449CAS No.: 2568277-68-7PROTAC SMARCA2 degrader-5 (Compound I-425) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2. PROTAC SMARCA2 degrader-5 degrades SMARCA2 in MV411 and in A549 with DC50 <100 nM, degrades SMARCA4 with DC50 of 100-500 nM. (Pink: Ligand for target protein (HY-159531); Black: Linker (HY-159538); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
-
JQ1-JX5
0 ImagesCat. No.: HY-183575JQ1-JX5 is a DCAF16-based BRD4 PROTAC degrader. JQ1-JX5 covalently modifies Cys58 of DCAF16, promotes ternary complex formation with BRD4, enables BRD4 ubiquitination and proteasomal degradation. JQ1-JX5 induces time-dependent degradation of BRD4 long and short isoforms in AGS cells with DC50 of 43.97 and 16.77 nM. JQ1-JX5 can be used for the research of cancer, such as acute myeloid leukemia.
-
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)).
