PROTACs or Proteolysis Targeting Chimeric Molecules are heterobifunctional nanomolecules that theoretically target any protein for ubiquitination and degradation. In terms of the structure, PROTACs consist of one moiety which is recognized by the E3 ligase. This moiety is then chemically and covalently linked to a small molecule or a protein that recognizes the target protein. The trimeric complex formation leads to the transfer of ubiquitins to the target protein.

By removing target proteins directly rather than merely blocking them, PROTACs can provide multiple advantages over small molecule inhibitors, which can require high systemic exposure to achieve sufficient inhibition, often resulting in toxic side effects and eventual drug resistance. PROTAC molecules possess good tissue distribution and the ability to target intracellular proteins, thus can be directly applied to cells or injected into animals without the use of vectors.

Targeted protein degradation using the PROTAC technology is emerging as a novel therapeutic method to address diseases, such as cancer, driven by the aberrant expression of a disease-causing protein. In addition to the use of PROTACs for the treatment of human disease, these molecules provide a chemical genetic approach to “knock down” proteins to study their function. Currently, there are several small molecule inhibitors that have been found to show good biological activity by specifically targeting BET, estrogen receptor (ER), androgen receptor, etc.

References:
[1] Sakamoto KM. Pediatr Res. 2010 May;67(5):505-8.
[2] Neklesa TK, et al. Pharmacol Ther. 2017 Jun;174:138-144.


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PROTAC IRAK4 degrader-5

PROTAC IRAK4 degrader-5 is a PROTAC-based IRAK4 degrader extracted from patent US20190192668A1, compound I-171[1].

  • CAS Number: 2360530-61-4
  • MF: C41H40F3N11O9
  • MW: 887.82
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(S,R,S)-AHPC-3-methylbutanyl acetate-methanesulfonothioate-Me-C10-NH2 TFA

(S,R,S)-AHPC-3-methylbutanyl acetate-methanesulfonothioate-Me-C10-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC ligand, it can be used in PROTAC technology[1].

  • CAS Number: 2417370-89-7
  • MF: C41H62F3N5O10S3
  • MW: 938.15
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tos-PEG9

Tos-PEG9 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 62573-11-9
  • MF: C25H44O12S
  • MW: 568.67500
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-amido-PEG4-TFP ester

Mal-amido-PEG4-TFP ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1807540-84-6
  • MF: C24H28F4N2O9
  • MW: 564.481
  • Catalog: PROTAC Linker
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 686.7±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 369.1±31.5 °C

Azido-PEG4-4-nitrophenyl carbonate

Azido-PEG4-4-nitrophenyl carbonate is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1422540-98-4
  • MF: C15H20N4O8
  • MW: 384.341
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG8-OH

Propargyl-PEG8-OH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].

  • CAS Number: 1351556-81-4
  • MF: C19H36O9
  • MW: 408.484
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 483.5±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 246.2±27.3 °C

Gefitinib-based PROTAC 3

Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively[1].

  • CAS Number: 2230821-27-7
  • MF: C47H57ClFN7O8S
  • MW: 934.51
  • Catalog: EGFR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG12-OH

m-PEG12-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. m-PEG12-OH is also a non-cleavable 12 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].

  • CAS Number: 2050595-03-2
  • MF: C25H52O13
  • MW: 560.67
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG7-alcohol

Propargyl-PEG7-alcohol is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].

  • CAS Number: 1422023-54-8
  • MF: C17H32O8
  • MW: 364.431
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 447.2±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 224.2±27.3 °C

m-PEG10-SH

m-PEG10-SH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 651042-85-2
  • MF: C21H44O10S
  • MW: 488.63300
  • Catalog: PROTAC Linker
  • Density: 1.079
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TLR4-IN-C34-C2-COOH

TLR4-IN-C34-C2-COO is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis[1].

  • CAS Number: 1159408-54-4
  • MF: C19H29NO11
  • MW: 447.43
  • Catalog: Toll-like Receptor (TLR)
  • Density: 1.29±0.1 g/cm3(Predicted)
  • Boiling Point: 634.1±55.0 °C(Predicted)
  • Melting Point: N/A
  • Flash Point: 337.3±31.5 °C

Thalidomide-amido-PEG2-NH2

Thalidomide-amido-PEG2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].

  • CAS Number: 2380273-72-1
  • MF: C19H22N4O7
  • MW: 418.40
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG1-Boc

Propargyl-PEG1-Boc is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 488150-84-1
  • MF: C10H16O3
  • MW: 184.232
  • Catalog: PROTAC Linker
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 239.2±15.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 93.1±15.0 °C

N'-Boc-N-(Gly-Oleoyl)-Lys

N'-Boc-N-(Gly-Oleoyl)-Lys is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2353409-71-7
  • MF: C31H57N3O6
  • MW: 567.80
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

4-Boc-amino-2,2-dimethylbutyric acid

4-Boc-amino-22-dimethylbutyric acid is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 153039-17-9
  • MF: C11H21NO4
  • MW: 231.28900
  • Catalog: PROTAC Linker
  • Density: 1.065g/cm3
  • Boiling Point: 369.9ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 177.5ºC

Azetidin-3-ol hydrochloride

Azetidin-3-ol hydrochloride is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azetidin-3-ol hydrochloride is also a alkyl chain-based PROTAC linker that can be used in the synthes PROTAC.

  • CAS Number: 18621-18-6
  • MF: C3H8ClNO
  • MW: 109.555
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: 170.7ºC at 760 mmHg
  • Melting Point: 90-92°C
  • Flash Point: 120.4ºC

t-Boc-N-Amido-PEG7-propargyl

Boc-NH-PEG7-propargyl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2112737-90-1
  • MF: C22H41NO9
  • MW: 463.56
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Biotin-PEG7-azide

Biotin-PEG7-azide is a PEG-based PROTAC linker can be used in the synthesis of PROTAC.

  • CAS Number: 1334172-75-6
  • MF: C26H48N6O9S
  • MW: 620.75900
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pomalidomide-amido-C1-Br

Pomalidomide-amido-C1-Br is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker. Pomalidomide-amido-C1-Br can be used to design a B-Raf PROTAC degrader PROTAC B-Raf degrader 1 (HY-111758). PROTAC B-Raf degrader 1 has anti-cancer activity[1].

  • CAS Number: 2351106-38-0
  • MF: C15H12BrN3O5
  • MW: 394.18
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Biotin-PEG3-NHS ester

Biotin-PEG3-NHS ester is a PEG-based PROTAC linker can be used in the synthesis of PROTAC.

  • CAS Number: 1253286-56-4
  • MF: C23H36N4O9S
  • MW: 544.618
  • Catalog: PROTAC Linker
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

α-Lipoic acid-NHS

α-Lipoic acid-NHS is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 40846-94-4
  • MF: C12H17NO4S2
  • MW: 303.39800
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 93.0-97.0°C
  • Flash Point: N/A

Fluorescein-PEG6- NHS ester

Fluorescein-PEG6-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1818294-35-7
  • MF: C40H45N3O15S
  • MW: 839.861
  • Catalog: PROTAC Linker
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 976.2±75.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 544.2±37.1 °C

Hydroxy-PEG1-(CH2)2-Boc

Hydroxy-PEG1-(CH2)2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 671802-00-9
  • MF: C9H18O4
  • MW: 190.23700
  • Catalog: PROTAC Linker
  • Density: 1.031±0.06 g/cm3(Predicted)
  • Boiling Point: 274.0±15.0℃at 760 mmHg
  • Melting Point: N/A
  • Flash Point: N/A

THP-PEG8-Tos

THP-PEG8-Tos is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 669556-37-0
  • MF: C24H40O10S
  • MW: 520.63300
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HO-PEG24-OH

HO-PEG24-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2243942-52-9
  • MF: C48H98O25
  • MW: 1075.28
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-(2,6-dioxopiperidin-3-yl)-5-nitroisoindoline-1,3-dione

CRBN ligand-9 (Compound 4d) is a CRBN ligand (Ki: 8.9 μM). CRBN ligand-9 can be used for synthesis of PROTACs[1][2].

  • CAS Number: 55003-81-1
  • MF: C13H9N3O6
  • MW: 303.23
  • Catalog: Ligand for E3 Ligase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bromoacetamido-PEG5-azide

Bromoacetamido-PEG5-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1415800-37-1
  • MF: C14H27BrN4O6
  • MW: 427.29
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AT6

AT6 is a PROTAC AT1 analogue, which is a highly selective bromodomain (Brd4) degrader.

  • CAS Number: 2098836-50-9
  • MF: C48H58ClN9O7S3
  • MW: 1004.68
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-amido-PEG2-NH2 hydrochloride

Thalidomide-amido-PEG2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].

  • CAS Number: 2380273-73-2
  • MF: C19H23ClN4O7
  • MW: 454.86
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

t-Boc-Aminooxy-PEG7-bromide

t-Boc-Aminooxy-PEG7-bromide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2353410-15-6
  • MF: C21H42BrNO10
  • MW: 548.46
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A