Scientific Reviews
Product Guides
Blogs
Topics
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
35 Results for "
VHL E3 ubiquitin ligase complex
" in MedChemExpress (MCE) Product Catalog:
Products (35)
35 Results for "VHL E3 ubiquitin ligase complex" in MCE Product Catalog:
2
2 Cited Publications
Target:
Research Areas:
VZ185 is a BRD9 and BRD7 PROTAC degrader, with DC50 values of 1.76 nM and 4.5 nM, respectively, in RI-1 cells; and DC50 values of 4 nM and 34 nM, respectively, in HEK293 cells. VZ185 hijacks the CRL2 VHL E3 ubiquitin ligase complex to induce ubiquitination and subsequent proteasomal degradation of BRD9 and BRD7. VZ185 can be used in research related to acute myeloid eosinophilic leukemia and malignant rhabdoid tumors .
1
1 Cited Publications
Research Areas:
XL01126 is a blood-brain barrier-permeable, selective LRRK2 PROTAC degrader (DC50: 14 nM (G2019S LRRK2) and 32 nM (WT LRRK2)). XL01126 forms a positively cooperative ternary complex with VHL E3 ubiquitin ligase and LRRK2, mediating the polyubiquitination and proteasomal degradation of LRRK2. XL01126 induces Mitophagy. XL01126 is applicable to research related to Parkinson's disease .
1
1 Cited Publications
Homo-PROTAC pVHL30 degrader 1 is a Homo-PROTAC autodegraders targeting the von Hippel-Lindau E3 ubiquitin ligase (VHL), with Kd values of 11 nM and 25 nM for pVHL19-EloBC and pVHL30-EloBC, respectively. Homo-PROTAC pVHL30 degrader 1 induces Cullin2 depletion, promotes VHL dimerization to form a ternary complex, and drives proteasome-dependent and CRL2-VHL-like ubiquitination-dependent autodegradation. Homo-PROTAC pVHL30 degrader 1 does not trigger hypoxic responses, and only causes extremely mild stabilization of hypoxia-inducible factor α subunits. Homo-PROTAC pVHL30 degrader 1 can be used in studies related to cervical cancer and osteosarcoma .
Cat. No.: HY-160525
Target:
Research Areas:
NVS-VHL720 is a selective VHL-based cysteine dioxygenase (CDO1) molecular glue degrader. NVS-VHL720 recruits CDO1 to the VHL E3 ligase complex, driving ubiquitin-dependent proteasomal degradation of CDO1. NVS-VHL720 can be used for the research of cancer .
Cat. No.: HY-173011
Target:
Research Areas:
RJS308 is a selective Cyclophilin A (CypA) PROTAC degrader. RJS308 induces ubiquitin-dependent CypA degradation by recruiting the VHL E3 ligase complex, and forms a ternary complex with CypA and VHL/elongin C/elongin B. RJS308 exhibits anti-HIV-1 and anti-HCV activities. RJS308 can be used in studies related to viral infections .
Target:
Research Areas:
ARD-69 is a PROTAC degrader based on the E3 ubiquitin ligase VHL and targeting the androgen receptor, which can induce androgen receptor (AR) protein degradation in AR-positive prostate cancer cells. ARD-69 inhibits AR-regulated gene expression, binds to the AR ligand binding domain at one end and binds to VHL at the other end, prompting AR to be recruited to the E3 ubiquitin ligase complex, triggering proteasome degradation, thereby inhibiting AR signaling pathways and downstream gene expression (such as PSA, TMPRSS2). ARD-69 can be used to study of castration-resistant prostate cancer (mCRPC) .
Cat. No.: HY-173011A
Target:
Research Areas:
RJS308 TFA is a selective Cyclophilin A (CypA) PROTAC degrader. RJS308 TFA induces ubiquitin-dependent CypA degradation by recruiting the VHL E3 ligase complex, and forms a ternary complex with CypA and VHL/elongin C/elongin B. RJS308 TFA exhibits anti-HIV-1 and anti-HCV activities. RJS308 TFA can be used in studies related to viral infections .
Target:
Research Areas:
PROTAC_ERRα is a potent and selective ERRα PROTAC degrader (DC50: ~100 nM in MCF-7 cells). PROTAC_ERRα recruits the VHL E3 ubiquitin ligase to ERRα, inducing ERRα ubiquitination and proteasomal degradation in a VHL-dependent manner. PROTAC_ERRα can be used in breast cancer-related research .
Target:
Research Areas:
PROTAC Bcl-xL degrader-2 is a selective Bcl-xL PROTAC degrader with a DC50 of 4.8 nM against Bcl-xL. PROTAC Bcl-xL degrader-2 forms a ternary complex with VHL E3 ligase, thereby redirecting the ubiquitin-proteasome system to mediate the degradation of Bcl-xL. PROTAC Bcl-xL degrader-2 triggers Apoptosis. PROTAC Bcl-xL degrader-2 can be used in the research of solid tumors and hematologic malignancies .
CST626 is a PROTAC degrader targeting IAP, with DC50 values of 0.7 nM, 2.4 nM and 6.2 nM against XIAP, cIAP1 and cIAP2, respectively. This compound recruits the VHL E3 ubiquitin ligase to form a heterotrimeric complex, thereby inducing ubiquitination and proteasomal degradation of the target proteins. CST626 also exhibits certain degrading activity against VHL30 and VHL19. CST626 inhibits the proliferation and induces apoptosis of various hematologic tumor cell lines, and its anti-tumor effect is further enhanced when used in combination with TNF-α. CST626 can be used in research related to multiple myeloma, acute myeloid leukemia and diffuse large B-cell lymphoma .
Cat. No.: HY-175252
PROTAC EGFR degrader 14 is a EGFR PROTAC degrader, with a DC50 of 2.9 nM against EGFR L858R/T790M/C797S. PROTAC EGFR degrader 14 forms a stable ternary complex by bridging the ATP-binding pocket of the target protein EGFR with VHL E3 ubiquitin ligase, induces efficient and specific degradation of EGFR mutants via the ubiquitin-proteasome system, and ultimately induces cell cycle arrest and apoptosis. PROTAC EGFR degrader 14 can be used in studies related to non-small cell lung cancer carrying the EGFR C797S drug-resistant mutation .
Cat. No.: HY-170859
CAS No.: 3110370-06-1
Target:
Research Areas:
AH078 is a PROTAC-based CK1δ/ε degrader (DC50=0.55 μM, Dmax=70%) that lacks subtype selectivity between CK1δ and CK1ε. AH078 induces target protein degradation either by recruiting the CUL4-CRBN E3 ligase complex and proteasome, or via the VHL- and ubiquitin-dependent pathway. AH078 also exhibits selectivity for CK1α, and is widely applicable to research related to colon cancer, pancreatic cancer, breast cancer, ovarian cancer, chronic lymphocytic leukemia, acute myeloid leukemia, glioma, and metastatic breast adenocarcinoma .
Cat. No.: HY-156152A
Purity: 99.44%
Target:
Research Areas:
PROTAC CARM1 degrader-1 hydrochloride is a highly selective CARM1 PROTAC degrader, with a DC50 of 8.1 nM in MCF‑7 cells. PROTAC CARM1 degrader-1 hydrochloride recruits the VHL E3 ubiquitin ligase complex to act on CARM1, inducing a proteasome-dependent degradation process. PROTAC CARM1 degrader-1 hydrochloride downregulates the methylation level of CARM1 substrates in breast cancer cells, inhibits breast cancer cell migration, and exhibits no significant inhibitory effect on cell proliferation. PROTAC CARM1 degrader-1 hydrochloride is applicable for related research on breast cancer .
Cat. No.: HY-175370
Target:
Research Areas:
PROTAC RIPK1 Degrader-1 is a selective RIPK1 PROTAC degrader. PROTAC RIPK1 Degrader-1 induces complete degradation of RIPK1 through the ubiquitin-proteasome system by bridging the target protein RIPK1 and VHL E3 ubiquitin ligase. PROTAC RIPK1 Degrader-1 is applicable to melanoma-related research .
Cat. No.: HY-172798
Target:
Research Areas:
XZ338 is a highly potent and selective BCL-XL PROTAC degrader derived from A-1331852 (HY-19741), with a DC50 of 0.43 nM in MOLT‑4 cells. XZ338 induces the formation of a ternary complex with BCL-XL and VHL E3 ligase, mediates target protein degradation via the ubiquitin-proteasome system, and exhibits significantly weaker degradation activity in platelets than in tumor cells. XZ338 possesses anti-cancer activity. XZ338 can be used in the research of T-cell acute lymphoblastic leukemia (T-ALL) .
Cat. No.: HY-175678
Target:
Research Areas:
PROTAC BRD2 BD1 Degrader-1 is a potent and selective BRD2 BD1 PROTAC degrader, with a DC50 of 65 nM, an EC50 of 423 nM, and a Kd of 69 nM against BRD2 BD1. PROTAC BRD2 BD1 Degrader-1 induces the formation of a ternary complex between the BET bromodomain and the VHL E3 ubiquitin ligase complex, triggering VCB-dependent degradation of the target bromodomain. PROTAC BRD2 BD1 Degrader-1 can be used in cancer research .
Cat. No.: HY-169093
CAS No.: 2768610-97-3
Target:
Research Areas:
MS41 is a ENL PROTAC degrader with a DC50 of 3.50 nM. MS41 recruits the VHL E3 ubiquitin ligase, triggers ENL degradation via the ubiquitin-proteasome system, and simultaneously induces AF9 degradation. MS41 reduces the chromatin occupancy of ENL-associated transcription elongation complexes, suppresses oncogene expression, and activates differentiation gene expression. MS41 inhibits leukemia cell growth and induces cell cycle arrest and apoptosis. MS41 inhibits leukemia progression in xenograft mouse models. MS41 can be used for research on mixed lineage leukemia-rearranged leukemia and nephroblastoma .
Cat. No.: HY-156152
CAS No.: 3032785-00-2
Target:
Research Areas:
PROTAC CARM1 degrader-1 is a highly selective CARM1 PROTAC degrader, with a DC50 of 8.1 nM in MCF‑7 cells. PROTAC CARM1 degrader-1 recruits the VHL E3 ubiquitin ligase complex to act on CARM1, inducing a proteasome-dependent degradation process. PROTAC CARM1 degrader-1 downregulates the methylation level of CARM1 substrates in breast cancer cells, inhibits breast cancer cell migration, and exhibits no significant inhibitory effect on cell proliferation. PROTAC CARM1 degrader-1 is applicable for related research on breast cancer .
Cat. No.: HY-175525
Target:
Research Areas:
MS44 is a potent and selective AURKB PROTAC degrader with a DC50 of 103 nM. MS44 recruits the VHL E3 ligase to form a ternary complex, mediating the specific degradation of AURKB via the ubiquitin-proteasome system, and exhibits no activity against related kinases such as AURKA/C. MS44 can be used for research on AURKB-dependent tumors .
Cat. No.: HY-114405
CAS No.: 2254609-23-7
SJFδ is a p38δ PROTAC degrader with a DC50 of 46.17 nM. SJFδ selectively induces ubiquitin-proteasome-dependent degradation of p38δ by forming a ternary complex with p38δ and the VHL E3 ligase, with no effect on other p38 isoforms or members of the MAPK family. SJFδ can be used for breast cancer research .
- 1
- 2
-
-
Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
