A PROTAC that drives CRBN degradation
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TD-165

Item No. 44837

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2S,4R)-1-((2S)-2-(11-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)undecanamido)-3,3-dimethyl-butanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
CAS Number
2305936-56-3
Molecular Formula
C46H59N7O8S
Formula Weight
870.1
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C([C@@H](NC(CCCCCCCCCCNC1=C(C(C(N2C3C(NC(CC3)=O)=O)=O)=CC=C1)C2=O)=O)C(C)(C)C)N4[C@H](C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)C[C@H](C4)O
InChi Code
InChI=1S/C46H59N7O8S/c1-28-39(62-27-49-28)30-19-17-29(18-20-30)25-48-41(57)35-24-31(54)26-52(35)45(61)40(46(2,3)4)50-36(55)16-11-9-7-5-6-8-10-12-23-47-33-15-13-14-32-38(33)44(60)53(43(32)59)34-21-22-37(56)51-42(34)58/h13-15,17-20,27,31,34-35,40,47,54H,5-12,16,21-26H2,1-4H3,(H,48,57)(H,50,55)(H,51,56,58)/t31-,34?,35+,40-/m1/s1
InChi Key
KSXVXTSIDVRZBR-IINAPWRYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $56

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    5 mg

    $252

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    10 mg

    $448

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    Product Description

    TD-165 is a proteolysis-targeting chimera (PROTAC) that contains VH 032 (Item No. 39982) conjugated to the cereblon (CRBN) inhibitor pomalidomide (Item No. 19877).1 It induces degradation of CRBN in HEK293T cells with a half-maximal degradation concentration (DC50) value of 20.4 nM. TD-165 (0.5 µM) increases L-type voltage-gated calcium channel 1.2α (Cav1.2α) levels in AC16 ventricular cardiomyocytes.2 It increases left ventricle pressure and heart rate in mice. Intra-articular administration of TD-165 (1.5 µg/joint) decreases disease severity and subchondral bone plate thickness in a mouse model of osteoarthritis induced by destabilization of the medial meniscus.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kim, K., Lee, D.H., Park, S., et al. Disordered region of cereblon is required for efficient degradation by proteolysis-targeting chimera. Sci. Rep. 9(1), (2019).

    2. Park, N., Marquez, J., Pham, T.K., et al. Cereblon contributes to cardiac dysfunction by degrading Cav1.2α. Eur. Heart J. 43(20), 1973-1989 (2022).

    3. Lee, Y., Kim, H.-E., Kwak, J.-S., et al. The cereblon-AMPK (AMP-activated protein kinase) axis in chondrocytes regulates the pathogenesis of osteoarthritis. Osteoarthritis Cartilage 32(12), 1579-1590 (2024).