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
16 Results for "
HiBiT
" in MedChemExpress (MCE) Product Catalog:
Products (16)
16 Results for "HiBiT" in MCE Product Catalog:
Synonyms: PROTAC BRD4 Degrader-5
Target:
Research Areas:
GAL-02-221 is a BRD4 PROTAC degrader with blood-brain barrier permeability, with a DC50 of 0.009 μM (Jurkat BRD4-HiBiT). GAL-02-221 induces proteasome-catalyzed BRD4 degradation, binds to VHL to trigger BRD4 ubiquitination, and recruits the VHL E3 ligase complex to participate in protein degradation. GAL-02-221 degrades BRD4 in breast cancer cells as well as mouse liver and brain tissues. GAL-02-221 is applicable to research related to breast cancer .
Cat. No.: HY-173066
CAS No.: 3048196-52-4
Research Areas:
NU227326 is a blood-brain barrier penetrant IDO1 PROTAC degrader, with a DC50 of 4.5 nM in HiBiT degradation assays. NU227326 degrades IDO1 in U87 and GBM43 cells, with DC50 values of 7.1 nM and 11.8 nM, respectively (WB assays). NU227326 is applicable to research related to glioblastoma, prostate cancer, triple-negative breast cancer, pancreatic cancer, and ovarian cancer .
Cat. No.: HY-169370
CAS No.: 2767166-30-1
Target:
Research Areas:
STAT3 HiBiT degrader 1 is a STAT3 HiBiT degrader with a DC50 of less than 0.05 μM in A549 cells .
Cat. No.: HY-178322
Target:
Research Areas:
UNC10415667 is a non-competitive, non-prodrug NSD2 degrader with a DC50 of 460 nM in U2OS NSD2 HiBiT cells. UNC10415667 forms a reversible covalent hemithioacetal bond with Cys326 of FBXO22, promoting the formation of a ternary complex with FBXO22 and NSD2, which in turn triggers the polyubiquitination and degradation of NSD2 via the ubiquitin-proteasome system. UNC10415667 can form complexes with FBXO22, NSD2 and BACH1 simultaneously, driving the synchronized degradation of NSD2 and BACH1 without competition. UNC10415667 can be used in research related to multiple myeloma, acute lymphoblastic leukemia, and prostate cancer .
Cat. No.: HY-W1128213
CAS No.: 2983841-00-3
Target:
Research Areas:
IKZF2-degrader 2 is a selective and orally active IKZF2 molecular glue degrader with DC50 values of 0.5 nM and 1.8 nM in HiBit and FACS. The IKZF2-degrader 2 mediates the ubiquitination and degradation of target proteins by recruiting the CRL4-CRBN E3 ubiquitin ligase. IKZF2-degrader 2 displays moderate degradation against SALL4 with a DC50 of 9 nM but does not induce any significant degradation towards IKZF1, IKZF3, CK1α and GSPT1. IKZF2-degrader 2 can be used for the study of cancer immunology .
Cat. No.: HY-168236
CAS No.: 2641510-88-3
Target:
Research Areas:
PROTAC SMARCA2 degrader-28 (Compound 158) is a PROTAC degrader for SMARCA2, that degrades SMARCA2 with a DC50 of 3 nM in HiBiT A549 cells .
Cat. No.: HY-168586
CAS No.: 2919995-09-6
Target:
Research Areas:
PROTAC IRAK4 degrader-12 is an orally active IRAK4 PROTAC degrader with a DC50 of 4.87 nM in K562 IRAK4-HiBiT cells. PROTAC IRAK4 degrader-12 induces protein degradation of IRAK4, IKZF1 and IKZF3. It inhibits the proliferation of diffuse large B-cell lymphoma cells. It suppresses tumor growth in mouse xenograft models of lymphoma cells. PROTAC IRAK4 degrader-12 can be used for the research of B-cell lymphoma and diffuse large B-cell lymphoma .
Target:
Research Areas:
Azacosterol (SC-12937) dihydrochloride is a chemosterilant which in-hibits reproduction in the pigeon. Azacosterol (SC-12937) dihydrochloride exerts its inhibitory effect through the blocking of the synthesis of cholesterol, thought to be a vital component in the formation of egg yolks .
Cat. No.: HY-156526
CAS No.: 2924182-31-8
Target:
Research Areas:
PHD-IN-1 (compound 80) is a potent inhibitor of PHD2，with an IC50 value of ≤5 nM. PHD-IN-1 shows EC50s of 2.5 μM in EPO Elisa assay both in Caco2-HIFla-HiBiT-clone-1 cells and Hep3B cells，respectively .
Cat. No.: HY-169264
Target:
Research Areas:
SJYHJ-026 is a PROTAC degrader targeting PXR, with a DC50 of 86.6 nM in SNU-C4 HiBiT-PXR KI cells. SJYHJ-026 shows higher selectivity for PXR over CAR, VDR, FXR, LXRα and LXRβ, and can bind to VHL to form a PXR-SJYHJ-026-VHL complex, inducing proteasomal degradation of PXR. SJYHJ-026 blocks agonist-induced PXR-mediated gene expression (including CYP3A4) and reduces basal PXR activity at the CYP3A4 promoter. SJYHJ-026 can be used for the research of colorectal cancer .
Cat. No.: HY-190203
CAS No.: 2930694-64-5
Research Areas:
GSPT1 degrader-20 is a cereblon (CRBN)-recruiting molecular glue degrader (with a
DC50 < 1 nM against GSPT1 HiBiT) that promotes the ubiquitination and proteasomal degradation of GSPT1 and/or IKZF1. GSPT1 degrader-20 can be used in research on hematological malignancies such as acute lymphoblastic leukemia .
DC50 < 1 nM against GSPT1 HiBiT) that promotes the ubiquitination and proteasomal degradation of GSPT1 and/or IKZF1. GSPT1 degrader-20 can be used in research on hematological malignancies such as acute lymphoblastic leukemia .
Cat. No.: HY-190223
CAS No.: 2915586-03-5
Target:
Research Areas:
IKZF1 degrader-5 is a CRBN-recruiting molecular glue degrader that selectively degrades IKZF1 in HiBiT-tagged HT-1080 cells (DC50 = 0.065 nM, Dmax = 88.3%). IKZF1/SALL4-IN-1 can be used for tumor-related research .
Cat. No.: HY-189442
ISM-PR44 is an orally active PROTAC degrader targeting BTK, with a DC50 of 0.05 nM in BTK-HiBiT Ramos cells. ISM-PR44 recruits CRBN E3 ligase to induce ubiquitination and proteasomal degradation of BTK. ISM-PR44 exhibits antiproliferative and cytotoxic activities in B-cell lymphoma cells. ISM-PR44 can be used for research on B-cell lymphoma .
Cat. No.: HY-190204
CAS No.: 2930694-65-6
Research Areas:
GSPT1 degrader-21 (compound 12) is a cereblon (CRBN)-recruiting GSPT1 molecular glue degrader. GSPT1 degrader-21 promotes the ubiquitination and proteasomal degradation of GSPT1 and/or IKZF1. GSPT1 degrader-21 has a GSPT1 HiBiT DC50 of < 1 nM. GSPT1 degrader-21 can be used for research on hematological tumors such as B-cell acute lymphoblastic leukemia and monocytic leukemia .
Cat. No.: HY-184335
CAS No.: 3097564-20-7
Research Areas:
PROTAC BET Degrader-18 is a PROTAC targeting BET, with a DC50 of 0.676 nM in HEK293-BRD4-HiBiT-KI cells. PROTAC BET Degrader-18 mainly targets and degrades BRD4 (EC50 = 59.91 nM), and exhibits weak degradation activity against BRD2. PROTAC BET Degrader-18 inhibits the expression of downstream oncoprotein c-Myc, thereby inducing cell cycle arrest and apoptosis. PROTAC BET Degrader-18 shows antiproliferative activity against acute myeloid leukemia cells and triple-negative breast cancer cells. PROTAC BET Degrader-18 demonstrates antitumor efficacy in xenograft mouse models. PROTAC BET Degrader-18 can be used for the research of acute myeloid leukemia and triple-negative breast cancer .
- 1
-
-
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
