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
32 Results for "
DCAF16
" in MedChemExpress (MCE) Product Catalog:
Products (32)
32 Results for "DCAF16" in MCE Product Catalog:
4
4 Cited Publications
Target:
Research Areas:
KB02-JQ1 is a potent and selective BRD4 PROTAC degrader. KB02-JQ1 degrades BRD4 via the ubiquitin-proteasome pathway by bridging DCAF16 E3 ubiquitin ligase and BRD4. KB02-JQ1 can be used for cancer research .
1
1 Cited Publications
Research Areas:
MMH2 is a novel BRD4 molecular glue degrader that functions by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4BD2) .
1
1 Cited Publications
Cat. No.: HY-163638
CAS No.: 3094209-54-5
Research Areas:
BRD4 degrader-1 (Compound mL 1-50) is a relatively selective, monovalent and covalent BRD4 Molecular glue degrader. BRD4 degrader-1 induces degradation of both long and short isoforms of BRD4 by targeting DCAF16 (an E3 ligase). BRD4 degrader-1 can be used in breast cancer research .
1
1 Cited Publications
Cat. No.: HY-160528
Research Areas:
IBG3 is a bivalent molecular glue degrader targeting BRD2 and BRD4, with DC50 values of 8.6 pM and 6.7 pM, respectively. IBG3 exhibits selectivity for BRD2 and BRD4 over BRD3. By recruiting the DCAF16 E3 ligase and binding in cis to the tandem bromodomains of BRD2 and BRD4, IBG3 enhances BRD-DCAF16 binding affinity and promotes ubiquitination and proteasomal degradation, without degrading isolated bromodomains. Although IBG3 lacks degradation selectivity between PSMA-positive and PSMA-negative prostate cancer cells and demonstrates lower in vivo antitumor potency compared to the PSMA-targeting conjugate IBG-P3, it serves as a useful tool for prostate cancer research .
Cat. No.: HY-163640
CAS No.: 3094209-58-9
Target:
Research Areas:
CDK4 degrader 1 is a selective CDK4 molecular glue degrader. CDK4 degrader 1 induces intracellular CDK4 degradation, and its activity is dependent on DCAF16. CDK4 degrader 1 targets the cysteine residue on DCAF16 through its vinylsulfonylpiperazine domain, thereby mediating the degradation of CDK4. CDK4 degrader 1 can be used in research related to cervical cancer .
Research Areas:
TMX1 is a covalent, selective BRD4 molecular glue degrader. TMX1 binds to the JQ1-binding site of BRD4BD2, forms covalent bonds with Cys58 of DCAF16 and Cys87 of GAK in a BRD4BD2-dependent template-assisted manner, stabilizes the BRD4-TMX1-DCAF16 ternary complex, and promotes the ubiquitination of BRD4 via the CRL4DCAF16 ubiquitin ligase complex. TMX1 induces selective degradation of BRD4, mild degradation of BRD2 and BRD3, as well as DCAF16-dependent cytotoxicity .
MMH1 is a novel BRD4 molecular glue degrader. MMH1 functions by recruiting the CUL4 DCAF16 ligase to the second bromodomain of BRD4 (BRD4 BD2). MMH1 binds to the JQ1-binding site of BRD4 BD2, acts as a template to covalently modify Cys58 of DCAF16, stabilizes the BRD4-DCAF16 ternary complex, and thereby promotes BRD4 degradation via the CRL4DCAF16 ubiquitin ligase pathway. Using BRD4 BD2 as a structural template, MMH1 covalently modifies Cys87 of GAK and induces the GAK-BRD4 BD2 interaction. Through its covalent mechanism, MMH1 exhibits sustained BRD4 degradation activity, and shows selective degradation activity for BRD4 BD2 over BRD4 BD1 .
Cat. No.: HY-172615
CAS No.: 3033019-04-1
Research Areas:
AMPTX-1 is a selective, orally active, covalent reversible BRD9 molecular glue degrader with a DC50 of 0.05 nM. AMPTX-1 selectively recruits BRD9 to the E3 ligase DCAF16. AMPTX-1 forms a ternary complex with BRD9 and a reversible covalent adduct with Cys58 on the surface of DCAF16. AMPTX-1 mediates BRD9 degradation via the proteasome and Cullin RING E3 ligase pathways. AMPTX-1 can be used in the research of solid tumors and hematological malignancies .
KB02-SLF is a nuclear FKBP12 covalent PROTAC degrader. KB02-SLF covalently modifies cysteine residues in DCAF16, forms a ternary complex with nuclear FKBP12, and mediates degradation via the CUL4-DDB1 E3 ubiquitin ligase pathway. KB02-SLF promotes polyubiquitination and proteasomal degradation of nucleus-localized FKBP12. KB02-SLF can be used in breast cancer research .
Cat. No.: HY-175756
CAS No.: 2901804-87-1
Target:
Research Areas:
SMARCA2/4 degrader-1 is a SMARCA2/4 molecular glue degrader with a DCAF16 EC50 of 110 nM. SMARCA2/4 degrader-1 covalently adducts at cysteine to form a ternary complex with SMARCA2/4 and recruits CUL4 DCAF16 and CRL1 FBXO22 E3 ligase complexes. SMARCA2/4 degrader-1 induces ubiquitination and proteasomal degradation of SMARCA2/4. SMARCA2/4 degrader-1 can be used for research of SMARCA4-deficient malignancies, non-small cell lung cancer (NSCLC), and colorectal cancer .
Cat. No.: HY-RS03562
Target:
Research Areas:
DCAF16 Human Pre-designed siRNA Set A contains three designed siRNAs for DCAF16 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-163641
Research Areas:
AR Degrader-1 is a molecular glue degrader targeting the androgen receptor (AR). AR Degrader-1 induces androgen receptor degradation by recruiting the DCAF16 E3 ligase substrate receptor, thereby triggering ubiquitination and proteasomal degradation. AR Degrader-1 exhibits relatively selective degradation of the androgen receptor in prostate cancer cells, reducing the levels of only a small number of other proteins. AR Degrader-1 can be used in studies related to prostate cancer .
Cat. No.: HY-178345
Synonyms: ZZ7
Research Areas:
ZZ7-23-022 (ZZ7) is a selective BRD9 molecule glue degrader. ZZ7-23-022 promotes the selective degradation of BRD9 through the ubiquitin-proteasome pathway, induces BRD9-DCAF16 interaction, and forms a ternary complex by covalently binding to the Cys178 site of DCAF16. ZZ7-23-022 induces the selective degradation of BRD9 in synovial sarcoma cells but does not affect human induced pluripotent stem cell (iPSC)-derived cardiomyocytes, while exerting antiproliferative effects on synovial sarcoma cells. ZZ7-23-022 can be used for research related to synovial sarcoma .
Cat. No.: HY-RS23600
Target:
Research Areas:
Dcaf16 Rat Pre-designed siRNA Set A contains three designed siRNAs for Dcaf16 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-170983
MC-25B is a DCAF16-recruiting FKBP12 PROTAC degrader with a DC50 of 0.35 μM. MC-25B promotes the formation of a ternary complex with DCAF16 and nuclear-localized FKBP12_NLS, thereby mediating DCAF16-dependent degradation of FKBP12_NLS via the proteasome and Cullin-RING ligase pathway .
Cat. No.: HY-157592
Purity: 98.72%
Research Areas:
MMH2-NR a negtive control of MMH2. MMH2 is a CUL4-associated factor (DCAF16)-based bromodomain protein 4 (BRD4) degrader .
Cat. No.: HY-176070
Target:
Research Areas:
HRG038 is a covalent CUL4 DCAF16-base PROTAC-liked BRD4 degrader. HRG038 induces proteasome- and Cullin E3 ligase-dependent degradation, covalently targets cysteine residue C173 on DCAF16 to mediate BRD4 degradation, and induces reduction in BRD3 levels. HRG038 shows selective loss of the short BRD4 isoform over the long isoform in non-cancer cells, degrades both BRD4 isoforms in breast cancer cells, and does not impair cell viability in non-cancer cells. HRG038 can be used for the research of breast cancer .
Cat. No.: HY-176067
Target:
Research Areas:
LO-4-25 is a CUL4 DCAF16 based covalent PROTAC-like degrader. LO-4-25 induces degradation of the androgen receptor (AR) and androgen receptor truncation variant AR-V7. LO-4-25 covalently targets cysteine residues on CUL4DCAF16 to mediate degradation of neo-substrates. LO-4-25 triggers proteasome-dependent degradation of target proteins via CUL4DCAF16-mediated ubiquitination. LO-4-25 can be used for the research of androgen-independent prostate cancer .
Cat. No.: HY-175186
Target:
Research Areas:
LO-3-62 is a SMARCA2/4 degrader. LO-3-62 incorporates a truncated fumaramide linker and conjugates it to a SMARCA2/4 inhibitor. LO-3-62 binds covalently to the CUL4 DCAF16 E3 ubiquitin ligase, inducing proteasome-dependent degradation of SMARCA2/4. LO-3-62 can be used in studies of monocytic leukemia .
- 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
