A PROTAC that drives the degradation of Halo-tagged proteins
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HaloPROTAC-E

Item No. 46000

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2S,4R)-N-(2-(2-(2-(2-((6-chlorohexyl)oxy)ethoxy)ethoxy)ethoxy)-4-(4-methylthiazol-5-yl)benzyl)-1-((S)-2-(1-cyanocyclopropane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxypyrrolidine-2-carboxamide
CAS Number
2365478-58-4
Molecular Formula
C39H56ClN5O8S
Formula Weight
790.4
Purity
≥95%
Formulation (Request formulation change)
A solid
SMILES
O=C(N1[C@@H](C[C@H](C1)O)C(NCC2=C(C=C(C3=C(N=CS3)C)C=C2)OCCOCCOCCOCCCCCCCl)=O)[C@H](C(C)(C)C)NC(C4(CC4)C#N)=O
InChi Code
InChI=1S/C39H56ClN5O8S/c1-27-33(54-26-43-27)28-9-10-29(32(21-28)53-20-19-52-18-17-51-16-15-50-14-8-6-5-7-13-40)23-42-35(47)31-22-30(46)24-45(31)36(48)34(38(2,3)4)44-37(49)39(25-41)11-12-39/h9-10,21,26,30-31,34,46H,5-8,11-20,22-24H2,1-4H3,(H,42,47)(H,44,49)/t30-,31+,34-/m1/s1
InChi Key
NJCGXLMTZGCSRS-JSWXEYCZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $99

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    5 mg

    $347

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    10 mg

    $644

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    25 mg

    $1,238

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    Product Description

    HaloPROTAC-E is a proteolysis-targeting chimera (PROTAC) composed of the von Hippel-Lindau inhibitor VH 298 (Item No. 21133) conjugated to a chloroalkane moiety, which forms a covalent bond with the engineered bacterial dehalogenase HaloTag7 on fusion proteins.1 It induces the degradation of Halo-tagged serum/glucocorticoid-regulated kinase 3 (SGK3) and vacuolar protein sorting 34 (VPS34) with half-maximal degradation concentration (DC50) values between 3-10 nM for both. In HEK293 cells expressing Halo-tagged VPS34, HaloPROTAC-E is selective for VPS34 over 9,782 proteins but does induce the degradation of the VPS34 regulatory subunits VPS15, beclin 1, autophagy-related 14 (ATG14), and UV radiation resistance-associated gene protein (UVRAG) at 300 nM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tovell, H., Testa, A., Maniaci, C., et al. Rapid and reversible knockdown of endogenously tagged endosomal proteins via an optimized HaloPROTAC degrader. ACS Chem Biol. 14(5), 882-892 (2019).