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Cat. No.: HY-184464

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PROTAC TSSK1 Degrader-2

PROTAC TSSK1 Degrader-2 is a cereblon-recruiting PROTAC degrader targeting TSSK1, with a DC₅₀ of 10.8 nM and an IC₅₀ of 56.8 nM against TSSK1. PROTAC TSSK1 Degrader-2 recruits the cereblon E3 ubiquitin ligase to induce proteasomal degradation of TSSK1. PROTAC TSSK1 Degrader-2 reduces the motility and in vitro fertilization capacity of mouse sperm. PROTAC TSSK1 Degrader-2 undergoes metabolic N-dealkylation and exhibits high efflux. PROTAC TSSK1 Degrader-2 can be used in studies related to male fertility.
(Pink: TSSK1 ligand (HY-184429); Blue: Cereblon ligand (HY-103596); Black: linker (HY-133052)).

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

Formula: C₄₅H₅₂ClN₉O₁₁S
Molecular Weight:962.47

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

PROTAC TSSK1 Degrader-2 Chemical Structure

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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Biological Activity

Description

PROTAC TSSK1 Degrader-2 is a cereblon-recruiting PROTAC degrader targeting TSSK1, with a DC₅₀ of 10.8 nM and an IC₅₀ of 56.8 nM against TSSK1. PROTAC TSSK1 Degrader-2 recruits the cereblon E3 ubiquitin ligase to induce proteasomal degradation of TSSK1. PROTAC TSSK1 Degrader-2 reduces the motility and in vitro fertilization capacity of mouse sperm. PROTAC TSSK1 Degrader-2 undergoes metabolic N-dealkylation and exhibits high efflux. PROTAC TSSK1 Degrader-2 can be used in studies related to male fertility^[1]. (Pink: TSSK1 ligand (HY-184429); Blue: Cereblon ligand (HY-103596); Black: linker (HY-133052)).

All PROTACs Isoforms :

In Vitro

PROTAC TSSK1 Degrader-2 (Compound 5.1) (24-48 h) potently degrades HiBiT-tagged TSSK1 in stable CHO-K1 (SC B1.1) cells, with a half-maximal degradation concentration (DC₅₀) of 10.8 nM and maximum degradation (D_max) of 68% after a 48 h incubation^[1].
PROTAC TSSK1 Degrader-2 (120 min pre-incubation, 60 min kinase reaction) directly engages and inhibits recombinant TSSK1 kinase activity with an IC₅₀ of 56.8 nM^[1].
PROTAC TSSK1 Degrader-2 (10 mM, 2 μM; 2 h, 0-60 min) has poor solubility (3.66 μM in FaSSIF) and moderate metabolic stability in mouse and human liver microsomes, with half-lives of 26.3 min and 14.8 min, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

Molecular Weight 962.47
Formula C₄₅H₅₂ClN₉O₁₁S
SMILES

O=S(C1=CC=CC=C1NC2=NC(NC3=CC=C(C4CCN(C(CCOCCOCCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)=O)CC4)C=C3OC)=NC=C2Cl)(NC)=O
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]. Holdaway JA, et al. Development of TSSK1 and TSSK2 Targeted Degraders Reveals Sperm Machinery for Protein Degradation and Potential for Nonhormonal Male Contraception. Journal of medicinal chemistry. 2026 Jun 25;69(12):14236-14254. [Content Brief]

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
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PROTAC TSSK1 Degrader-2

All PROTACs Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PROTAC TSSK1 Degrader-2 Related Classifications

HY-184464 Related Classifications