PROTAC AR Degrader-13

Cat. No.: HY-184195: Data Sheet Handling Instructions
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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.

For research use only. We do not sell to patients.

PROTAC AR Degrader-13 Chemical Structure

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Cereblon

In Vitro

PROTAC AR Degrader-13 (dAR-6-1) potently degrades androgen receptor in LNCaP cells with a DC₅₀ of 0.90 nM and a D_max 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 D_max 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.

Western Blot Analysis^[1]

Cell Line:	human dermal papilla (hDPC) cells
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 (1, 10, 100 nM with siRNA pretreatment) 4 h (10, 100 nM with 2 h inhibitor/ligand pretreatment)
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 D_max 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.

Cell Viability Assay^[1]

Cell Line:	hDPC cells
Concentration:	0.01, 0.1, 1, 10, 100, 1000 μM
Incubation Time:	72 h
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.

Parmacokinetics

Species	Dose	Route	CL	T_1/2	T_max	C_max	C₀	AUC_last	AUC_0-∞	MRT_{INF_obs}	V_z
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

In Vivo

PROTAC AR Degrader-13 (dAR-6−1) (100 mg/mL; topical; once daily; 28 days) induces faster hair regeneration than Minoxidil (HY-B0112) in an androgenetic alopecia mouse model, with comparable hair density and greater hair diameter by day 28^[1].
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.

Animal Model:	C57BL/6 (male, 6 weeks old, depilated on dorsal skin, treated daily with 0.5% testosterone solution to induce follicular miniaturization)^[1]
Dosage:	100 mg/mL
Administration:	topical; once daily or once every 3 days; 28 days
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.

Animal Model:	C57BL/6 (male, 6 weeks old)^[1]
Dosage:	1 mg/mL; 10 mg/mL; 100 mg/mL
Administration:	topical
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.

Molecular Weight

841.28

Formula

C₃₉H₄₄ClF₃N₁₀O₆

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Wang X, et al. Discovery of an Androgen Receptor Degrader Featuring a Pyridazinyl Glutarimide CRBN-Binding Motif for Transdermal Treatment of Androgenetic Alopecia. J Med Chem. 2026 Jun 11;69(11):13028-13054. [Content Brief]