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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
110 Results for "
DCAF
" in MedChemExpress (MCE) Product Catalog:
Products (110)
110 Results for "DCAF" in MCE Product Catalog:
15
15 Publications Verification
Synonyms: E 7070
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Indisulam (E 7070) is a carbonic anhydrase inhibitor with anticancer activity. Indisulam (E 7070) is a sulfonamide agent that targets the G1 phase of the cell cycle. Indisulam (E 7070) causes a blockade in the G1/S transition through inhibition of the activation of both CDK2 and cyclin E. Indisulam (E 7070) targets splicing by inducing RBM39 degradation via recruitment to DCAF15 .
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E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a molecular glue that induces the targeted degradation of splicing factor RBM39 by recruiting the E3 ubiquitin ligase CUL4-RBX1-DDB1-DCAF15 (CRL4 DCAF15). E7820 is an angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. E7820 can be used for the study of acute myeloid leukemia (AML) .
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4 Cited Publications
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KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1 .
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1 Cited Publications
Cat. No.: HY-160528
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IBG3 is a Molecular glue degrader targeting BRD2 and BRD4, with DC50 values of 8.6 pM and 6.7 pM, respectively. IBG3 binds simultaneously to the tandem bromodomains of BRD2/BRD4, induces intramolecular conformational changes, enhances the affinity of BRD2/BRD4 for DCAF16, and promotes ubiquitination and degradation. IBG3 is applicable to the research of chronic myeloid leukemia .
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Cat. No.: HY-161779
CAS No.: 2851986-76-8
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PLX-3618 is a molecular glue, that degrades BRD4 with DC50 of 12.2 nM. PLX-3618 promotes polyubiquitination and subsequent proteasomal degradation of BRD4 by recruiting of the E3 ligase substrate receptor, DCAF11. PLX-3618 inhibits the proliferation of various cancer cells, induces apoptosis in AML cells. PLX-3618 exhibits antitumor activity against AML in mouse models .
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MMH2 is a novel BRD4 molecular glue degrader that functions by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4BD2) .
Cat. No.: HY-163638
CAS No.: 3094209-54-5
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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 .
Cat. No.: HY-W037495
CAS No.: 2098346-67-7
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DCAF15 ligand-1 (compound 9) is a ligand for the E3 ligase DCAF15. DCAF15 ligand-1 can be used in the synthesis of IBG1 (HY-153459) .
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DCAF1 binder 1 is a selective for the CRL4 DCAF1 E3 ligase complex. DCAF1 binder 1 is a ligands for E3 Ligase, involving in targeted protein degradation (TPD) .
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OICR-8268 is a reversible DCAF1 ligand that binds to the DCAF1 WDR domain with a Kd of 38 nM. OICR-8268 can enable the development of DCAF1-based PROTACs .
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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 .
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MMH1 is a novel BRD4 molecular glue degrader that functions by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4BD2) .
Cat. No.: HY-172615
CAS No.: 3033019-04-1
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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 .
Cat. No.: HY-W133627
CAS No.: 118719-16-7
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dCeMM1 is a RBM39 glue degrader. dCeMM1 shows functions by re-directing the activity of the CRL4 DCAF15 ligase. dCeMM1 decreases the expression of RBM39 levels in WT KBM7 cells .
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IBG1 is a molecular glue degrader targeting BRD2 and BRD4 (DC50: 0.15 nM). IBG1 has no significant degradation effect on its paralogue BRD3. IBG1 can inhibit the growth of cancer cells and can be used in tumor research. (Pink: BRD2/BRD4 Ligand (HY-111139); Black: Linker; Blue: DCAF15 ligand-1 (HY-W037495)) .
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PROTAC BET Degrader-12 (Compound 8b) is a PROTAC degrader for bromodomain and extra-terminal domain (BET)-containing proteins, which degrades the BRD3 and BRD4 in a DCAF11-dependent manner. PROTAC BET Degrader-12 inhibits cell viability of KBM7 with a DC50 of 305.2 nM
Cat. No.: HY-156744
Purity: 98.87%
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DBr-1 is a potent BRD9 PROTAC degrader (KD: 13 nM). DBr-1 can overcome intrinsic resistance to VHL-degrader. Blue: DCAF1 binder (HY-149934), Black: linker, Pink: BRD9/BRD7 bromodomains inhibitor (HY-100352) .
Cat. No.: HY-175756
CAS No.: 2901804-87-1
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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-175343
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OICR-41103 is an effective, selective, cell-active DCAF1 small molecule chemical probe that targets the DCAF1 WDR domain and replaces the viral Vpr protein. The binding Ki value of OICR-41103 and DCAF1 is less than 2 nM .
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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
