VHL Ligand 1 (hydrochloride) Synthesis Route

VHL Ligand 1 (hydrochloride) Synthesis

VHL Ligand 1 (hydrochloride) (Synonyms: (2S,4R)-1-((S)-2-amino-3,3-dimethylbutanoyl)-4-hydroxy-n-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide)

VHL ligand 1 is a building block in the synthesis of proteolysis-targeting chimera technologies (PROTACs).1 It is the von Hippel-Lindau (VHL) E3 ligase binding portion of some VHL-based PROTACs, including BET PROTAC MZ1 (Item No. 21622).

VHL Ligand 1 (hydrochloride)

A PROTAC building block

Item No. AW52602
CAS No. 1448297-52-6
Purity: 95%

100mg

＄13.00

250mg

＄19.00

＄50.00

＄166.00

10g

＄297.00

25g

＄666.00

Quantity

Add to Cart

Buy Now

VHL Ligand 1 (hydrochloride) Synthetic Route

AB44890

CAS: 3959-07-7

AC64158

CAS: 68819-84-1

BA08222

CAS: 2308507-34-6

AV99903

CAS: 1448189-30-7

Al54018

CAS: 62965-35-9

AB79875

CAS: 40216-83-9

BF10349

CAS: 630421-45-3

A168087

CAS: 630421-46-4

AV99903

CAS: 1448189-30-7

AY06994

CAS: 1448189-98-7

AW52602

CAS: 1448297-52-6

1: sodium hydroxide / methanol / 5 h / 0 - 20 °C
2: potassium acetate; palladium diacetate / N,N-dimethyl acetamide / 10 h / 150 °C / Inert atmosphere
3: hydrogenchloride / methanol
4: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide / 20 °C
5: lithium hydroxide / water; tetrahydrofuran / 20 °C
6: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide / 20 °C
7: trifluoroacetic acid / dichloromethane / 20 °C

Order VHL Ligand 1 (hydrochloride) Intermediates

{{item['cas']}} | {{item['name']}}

MF:{{item['mf']}} MW:{{item['mw']}}

Download SDS

Catalog No.

Pack Size

Purity

Availability

Price

${{getUSMoneyFormat(sku['price'])}}

Add to Cart

Buy Now

References

1.J.Med. Chem. 2019, 62, 941−964. 

2.Raina, K., Lu, J., Qian, Y., et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proc. Natl. Acad. Sci. USA 113(26), 7124-7129 (2016).

3.Zengerle, M., Chan, K.-H., and Ciulli, A. Selective small molecule induced degradation of the BET bromodomain protein BRD4. ACS Chem. Biol. 10(8), 1770-1777 (2015).