PROTAC AR Degrader-13
PROTAC AR Degrader-13 is a proteolysis-targeting chimera (PROTACs) that targets the androgen receptor (AR). PROTAC AR Degrader-13 has a DC50 of 0.90 nM in LNCaP cells and a DC50 of 0.23 nM in hDPC cells. PROTAC AR Degrader-13 induces AR degradation, downregulates TGF-β1 expression, upregulates β-catenin levels, and restores the Wnt/β-catenin pro-proliferation signaling in hair follicles. In a testosterone-induced androgenetic alopecia mouse model, PROTAC AR Degrader-13 accelerates hair regeneration rate, increases hair density and hair diameter. PROTAC AR Degrader-13 can be used for the research of androgenetic alopecia.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C39H44ClF3N10O6
- 分子量:841.28
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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Cereblon |
PROTAC AR Degrader-13 (dAR-6-1) potently degrades androgen receptor in LNCaP cells with a DC50 of 0.90 nM and a Dmax of 91%[1].
PROTAC AR Degrader-13 (0.1-1000 nM; 0.5-36 h) potently degrades androgen receptor in hDPC cells with a DC50 of 0.23 nM and a Dmax of 90% via a CRBN-, ubiquitin-proteasome system-, and ternary complex-dependent mechanism[1].
PROTAC AR Degrader-13 (0.1-500 μM; 72 h) does not significantly inhibit hDPC cell viability, with an IC50 > 500 μM after 72 h of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human dermal papilla (hDPC) cells
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Concentration:0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM (6 h incubation)
10 nM (time-course incubations)
1, 10, 100 nM (4 h incubation with siRNA pretreatment)
1, 10, 100 nM (4 h incubation with inhibitor/ligand pretreatment) -
Incubation Time:6 h (0.1-1000 nM)
0.5, 1, 2, 3, 4, 6, 9, 12, 24, 36 h (10 nM)
4 h -
Result:Induced rapid, sustained AR degradation, detectable within 2 h and maintained for over 36 h at 10 nM.
Exhibited dose-dependent degradation across 0.1-1000 nM without a hook effect, with a DC50 of 0.23 nM and a Dmax of 90%.
Abrogated degradation occurred with CRBN knockdown, while pretreatment with MG-132 (HY-13259), Pevonedistat (HY-70062), lenalidomide (HY-A0003), or enzalutamide (HY-70002) blocked degradation.
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Cell Line:hDPC cells
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Concentration:0.01, 0.1, 1, 10, 100, 1000 μM
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Incubation Time:72 h
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Result:Did not induce significant growth inhibition, with cell viability remaining above ~90% at concentrations up to 100 μM, ~80% at 100−500 μM, and an IC50 > 500 μM.
| Species | Dose | Route | CL | T1/2 | Tmax | Cmax | C0 | AUClast | AUC0-∞ | MRTINF_obs | Vz |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 2 mg/kg | i.v. | 10.1 mL/min/kg | 1.79 h | 0.083 h | 1019 ng/mL | 1208 ng/mL | 3465 ng·h/mL | 3487 ng·h/mL | 3.96 h | 1.39 L/kg |
PROTAC AR Degrader-13 (1-100 mg/mL; topical) in C57BL/6 mice results in concentration-dependent skin retention[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 6 weeks old, depilated on dorsal skin, treated daily with 0.5% testosterone solution to induce follicular miniaturization)[1]
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Dosage:100 mg/mL
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Administration:topical; once daily or once every 3 days; 28 days
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Result:Triggered prominent hair coverage on day 10-11, showing superior hair coverage versus minoxidil at day 12, 14 and 16.
Achieved hair density equivalent to minoxidil, with both groups exhibiting higher hair density and distinctly enlarged hair diameter compared to the AGA model after daily topical use for 28 days.
Delivered hair regrowth potency comparable to minoxidil, with notably raised hair density and thickened hair diameter against the AGA model under triweekly administration.
Evoked no observable cutaneous irritation or histopathological lesions.
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Animal Model:C57BL/6 (male, 6 weeks old)[1]
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Dosage:1 mg/mL; 10 mg/mL; 100 mg/mL
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Administration:topical
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Result:Exhibited concentration-dependent skin retention, with 1 mg/mL formulation showing minimal retention, 10 mg/mL formulation presenting moderate retention, and 100 mg/mL formulation reaching the peak retention of 2900 ng/cm2.
化学情報
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分子量 841.28
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分子式 C39H44ClF3N10O6
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SMILES
ClC1=CC(O[C@H]2CC[C@@H](CC2)NC(C3=CC=C(N=N3)N4CCC(CC4)C[NH+]5CCN(C6=CC=C(N=N6)C7C(NC(CC7)=O)=O)CC5)=O)=CC=C1C#N.FC(C([O-])=O)(F)F
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
PROTAC AR Degrader-13 関連分類
HY-184195 関連分類
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