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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
23 Results for "
AURKA PROTAC degrader
" in MedChemExpress (MCE) Product Catalog:
Products (23)
23 Results for "AURKA PROTAC degrader" in MCE Product Catalog:
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2 Cited Publications
Synonyms: IPI 1040 sodium; TBC11251 sodium
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Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC50 of 1.4 nM and a Ki of 0.43 nM. Sitaxsentan sodium exhibits an IC50 for the ETB receptor of as high as 9800 nM. Sitaxsentan sodium is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan sodium can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension .
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1 Cited Publications
TL12-186 is a multi-kinase PROTAC degrader. TL12-186 recruits the CRBN E3 ubiquitin ligase to target and degrade a variety of distinct kinases, including FLT3, BTK, AURKA, PTK2B, and multiple cyclin-dependent kinases (CDKs). TL12-186 can be used in leukemia-related research .
Cat. No.: HY-171767
CAS No.: 3038446-94-2
Synonyms: JB325
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SK2188 (JB325) is a selective AURKA PROTAC degrader with a DC50 of 3.9 nM. SK2188 recruits CRBN E3 ubiquitin ligase to target and degrade AURKA, abrogating both its catalytic and non-kinase functions, which leads to the destabilization and degradation of the oncogenic protein MYCN, ultimately inducing replication stress, DNA damage and apoptosis. SK2188 is applicable to research related to neuroblastoma .
Cat. No.: HY-168543
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PROTAC AURKA degrader 3 is a selective AURKA PROTAC degrader, with DC50 values of 2.05, 157.85 and 43.05 nM against AURKA, AURKB and TTK, respectively. PROTAC AURKA degrader 3 exhibits cytotoxicity against acute myeloid leukemia cells. PROTAC AURKA degrader 3 can be used for research related to acute myeloid leukemia .
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Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
FMF-06-098-1 is a multi-target kinase PROTAC degrader. FMF-06-098-1 can be used to target degradation kinases which degrades AAK1, AΒL2, AURKA, AURKB, BUBIB, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDk6, CDK7, CDK9, CHEK1, CSNKID, EPHA1, PER, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, S1K2, STK35, TNK2, UHMK1, ULK1, and WEE1 .
Cat. No.: HY-137344A
Purity: 99.44%
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dAURK-4 hydrochloride is a selective AURKA PROTAC degrader. dAURK-4 hydrochloride promotes ubiquitination and degradation of AURKA . dAURK-4 hydrochloride can be used in the research of glioblastoma and multiple myeloma .
Cat. No.: HY-171768
CAS No.: 3038446-91-9
Synonyms: JB301
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SK2187 (JB301) is a selective AURKA PROTAC degrader. SK2187 induces targeted degradation of AURKA by recruiting the CRBN E3 ubiquitin ligase. SK2187 is applicable to research related to neuroblastoma .
Cat. No.: HY-168540
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PROTAC MPS1 degrader 1 is a selective monopolar spindle 1 (Mps1/TTK) PROTAC degrader, with DC50 values of 17.7, 108.67 and 570.25 nM against TTK, AURKA and AURKB, respectively. PROTAC MPS1 degrader 1 exhibits cytotoxicity against acute myeloid leukemia cells. PROTAC MPS1 degrader 1 can be used in research related to acute myeloid leukemia .
Cat. No.: HY-175830
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PROTAC AURKA degrader 1 is a AURKA PROTAC degrader . PROTAC AURKA degrader 1 forms a ternary complex with AURKA and CRBN E3 ligase, labels AURKA to induce its ubiquitination, and promotes its degradation via the ubiquitin-proteasome system. PROTAC AURKA degrader 1 is applicable to leukemia-related research .
Cat. No.: HY-137344
CAS No.: 2705844-81-9
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dAURK-4 is a selective AURKA PROTAC degrader. dAURK-4 promotes ubiquitination and degradation of AURKA . dAURK-4 can be used in the research of glioblastoma and multiple myeloma .
Cat. No.: HY-168545
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SF-1 is an AURKA ligand that can be used for the synthesis of PROTACs, such as PROTAC MPS1 degrader 2 (HY-168543). SF-1 can act as a free inhibitor and has the ability to pull down AURKA, AURKB, and TTK with DC50 values of 273.5, 933.5, and 1274 nM respectively. SF-1 has an anti-proliferative effect on acute myeloid leukemia .
Cat. No.: HY-175525
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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-175827
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MK-5108-NH-PEG2-alkyne is a Aurora kinase A (AURKA) inhibitor. MK-5108-NH-PEG2-alkyne can be used for synthesis of PROTAC AURKA degrader 1 (HY-175830) .
Cat. No.: HY-180132
CAS No.: 3093582-13-6
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PROTAC AURKA degrader 2 (compound D) is a potent and selective PROTAC AURKA degrader with an IC50 of 3.58 nM. PROTAC AURKA degrader 2 exhibits 21.6-fold selectivity for AURKA over AURKB (IC50 = 77.2 nM). PROTAC AURKA degrader 2 specifically depletes AURKA on the mitotic spindle .
Cat. No.: HY-187470
CAS No.: 3135155-78-8
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PROTAC AURKA degrader-4 is a AURKA PROTAC degrader with a DC50 of 25.62 nM (Jurkat cells). PROTAC AURKA degrader-4 recruits the CRBN E3 ubiquitin ligase via the ubiquitin-proteasome system. PROTAC AURKA degrader-4 disrupts both the catalytic and non-catalytic functions of AURKA, including its interactions with TPX2 and c-Myc. PROTAC AURKA degrader-4 induces G2/M phase arrest and apoptosis. PROTAC AURKA degrader-4 exhibits enhanced antiproliferative activity and in vivo antitumor efficacy in models with high CRBN and AURKA expression. PROTAC AURKA degrader-4 can be used for the research of acute lymphoblastic leukemia .
Cat. No.: HY-172144
CAS No.: 3038446-90-8
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JB300 is a PROTAC degrader that selectively targets and degrades AURORA-A by recruiting cereblon, with EC50 values of 373 nM and 193 nM in intact cells and permeabilized cells, respectively. JB300 can be used in studies related to acute myeloid leukemia and targeted protein degradation mechanisms .
Cat. No.: HY-179641
CAS No.: 3131860-12-0
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SK5527 is a selective AURKA PROTAC degrader degrading AURKA with DC50 = 2 nM. SK5527 bind to NanoLuc-AURKA with an IC50 of 20 nM. SK5527 effectively reduces MYCN levels in MYCN-amplified neuroblastoma cells and limited by MDR1-mediated efflux. SK5527 efficiently reduced AURKA levels in vivo. SK5527 can be used for neuroblasto2ma research .
Cat. No.: HY-187196
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ATR/AURKA-ligand 1 (Compound 8g) is a ATR/AURKA ligand. ATR/AURKA-ligand 1 serves as a target protein ligand for the synthesis of ATR/AURKA PROTAC degraders, such as Abd141 (HY-187195). ATR/AURKA-ligand 1 is applicable to the research of acute lymphoblastic leukemia .
Cat. No.: HY-179640
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SK4454 is a selective AURKA PROTAC degrader degrading AURKA with IC50 = 8 nM. MYCN levels in MYCN-amplified neuroblastoma cells and limited by MDR1-mediated efflux. SK4454 efficiently reduced AURKA levels in vivo. SK4454 can be used for neuroblastoma research .
Cat. No.: HY-181311
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CCT400028 is a PROTACs-class degrader that targets the Aurora A (AURKA) kinase. CCT400028 induces ubiquitination and proteasomal degradation of target proteins by recruiting the cereblon (CRBN) E3 ubiquitin ligase. The KD values of CCT400028 against the three subtypes of human AURKA are 71 nM, 2100 nM and >10000 nM, respectively, and its IC50 against human CRBN is 6300 nM. CCT400028 is applicable to relevant research on leukemia, neuroblastoma and glioma .
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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
