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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Protein degrader 1 hydrochloride

Protein degrader 1 hydrochloride is used in the synthesis of HaloPROTACs.

  • CAS Number: 1448189-80-7
  • MF: C22H31ClN4O3S
  • MW: 467.025
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Hexane-1,6-diyldiphosphonic acid

Hexane-1,6-diyldiphosphonic acid is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 4721-22-6
  • MF: C6H16O6P2
  • MW: 246.13500
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 206 °C
  • Flash Point: N/A

N-Ethylpropionamide-PEG1-Br

N-Ethylpropionamide-PEG1-Br is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1539080-27-7
  • MF: C7H14BrNO2
  • MW: 224.10
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cbz-NH-PEG1-CH2CH2COOH

Cbz-NH-PEG1-CH2CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1205751-19-4
  • MF: C13H17NO5
  • MW: 267.28
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

VH032-PEG2-NH-BOC

VH032-PEG2-NH-BOC is a Boc-modified VH032 (HY-120217) that serves as a ligand for VHL and recruits von Hippel-Lindau (VHL) proteins. VH032-PEG2-NH-BOC will remove the protecting group under acidic conditions and be directly used for PROTAC molecule synthesis. VH032-PEG2-NH-BOC is a key intermediate in the synthesis of PROTAC based on VHL ligand.

  • CAS Number: 2162120-75-2
  • MF: C33H49N5O8S
  • MW: 675.84
  • Catalog: Ligand for E3 Ligase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-BOC-2,2′-(ethylenedioxy)bis(ethylamine)

PROTAC Linker 13 is a PROTAC linker, which refers to the alkyl/ether composition. PROTAC Linker 13 can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

  • CAS Number: 153086-78-3
  • MF: C11H24N2O4
  • MW: 248.319
  • Catalog: PROTAC Linker
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 365.2±27.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 174.6±23.7 °C

Bis-PEG4-sulfonic acid

Bis-PEG4-sulfonic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1807539-08-7
  • MF: C10H22O10S2
  • MW: 366.406
  • Catalog: PROTAC Linker
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

1-Phenyl-2,5,8,11,14,17-hexaoxanonadecan-19-yl methanesulfonate

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

  • CAS Number: 1262681-32-2
  • MF: C20H34O9S
  • MW: 450.54
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-O-amido-C5-NH2

Thalidomide-O-amide-C5-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: 2360527-40-6
  • MF: C20H24N4O6
  • MW: 416.428
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 757.3±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 411.8±32.9 °C

Bromo-PEG7-azide

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

  • CAS Number: 1056969-61-9
  • MF: C16H32BrN3O7
  • MW: 458.35
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azide-PEG3-L-alanine-Fmoc

Azide-PEG3-L-alanine-Fmoc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2054345-69-4
  • MF: C24H28N4O7
  • MW: 484.50
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thiol-PEG5-acid

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

  • CAS Number: 1449390-67-3
  • MF: C13H26O7S
  • MW: 326.41
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(4R)-4-Hydroxy-D-proline hydrochloride (1:1)

cis-4-Hydroxy-D-proline hydrochloride is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). cis-4-Hydroxy-D-proline hydrochloride is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2].

  • CAS Number: 77449-94-6
  • MF: C5H10ClNO3
  • MW: 167.591
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: 368.6ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: N/A

Biotin-PEG4-Picolyl azide

Biotin-PEG4-Picolyl azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2222687-71-8
  • MF: C27H42N8O7S
  • MW: 622.74
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Acid-apeg4-acid n-boc

N-Boc-N-bis(PEG2-acid) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2054339-01-2
  • MF: C19H35NO10
  • MW: 437.48
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

diethyl 10-bromodecylphosphonate

Diethyl 10-bromodecylphosphonate is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 272785-01-0
  • MF: C14H30BrO3P
  • MW: 357.26
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MZP-55

MZP-55 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 8 nM for Brd4BD2.

  • CAS Number: 2010159-48-3
  • MF: C57H70ClN7O10S
  • MW: 1080.72
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-O-C7-NH2

Thalidomide-O-C7-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: 2093536-11-7
  • MF: C20H25N3O5
  • MW: 387.43
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bis-methacrylate-PEG5

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

  • CAS Number: 13497-24-0
  • MF: C18H30O8
  • MW: 374.42600
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-NH-PEG1-NH2 diTFA

Thalidomide-NH-PEG1-NH2 diTFA 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: 2768514-19-6
  • MF: C21H22F6N4O9
  • MW: 588.41
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Biotin-PEG2-azide

Biotin-PEG2-azide is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 1910803-72-3
  • MF: C16H28N6O4S
  • MW: 400.5
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-(t-Boc-Aminooxy-PEG2)-N-bis(PEG3-propargyl)

N-(t-Boc-Aminooxy-PEG2)-N-bis(PEG3-propargyl) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2112737-60-5
  • MF: C29H52N2O11
  • MW: 604.73
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bromo-PEG6-Boc

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

  • CAS Number: 1393330-41-0
  • MF: C19H37BrO8
  • MW: 473.396
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 489.9±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 250.1±27.3 °C

PROTAC BRD9-binding moiety 1

Target Protein-binding moiety 6 is a compound that binds to BRD9, and used for inhibiting BRD9 activity.

  • CAS Number: 2097512-23-5
  • MF: C23H25N3O7S2
  • MW: 519.59
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BC-1215

BC-1215 is an inhibitor of F-box protein 3 (FBXO3, a ubiquitin E3 ligase component, IC50=0.9 μg/mL for IL-1β release). BC-1215 decreases Fbxo3-Fbxl2 interaction and prevents SCFFbxo3 catalyzed Fbxl2 ubiquitination. BC-1215 inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1–TRAF6. BC-1215, interacts with ApaG to profoundly inhibit secretion of a broad spectrum of TH1 panel cytokines from human PBMC[1].

  • CAS Number: 1507370-20-8
  • MF: C26H26N4
  • MW: 394.511
  • Catalog: Ligand for E3 Ligase
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 589.9±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 310.6±30.1 °C

Bromoacetamido-C2-PEG2-NH-Boc

Bromoacetamido-C2-PEG2-NH-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 182244-33-3
  • MF: C13H25BrN2O5
  • MW: 369.252
  • Catalog: PROTAC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 506.5±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 260.1±30.1 °C

DBCO-Biotin

DBCO-Biotin is a Click Chemistry intermidate used for antibody-drug conjugates.

  • CAS Number: 1418217-95-4
  • MF: C28H30N4O3S
  • MW: 502.628
  • Catalog: PROTAC Linker
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 905.9±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 501.6±34.3 °C

Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc

Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc is a synthesized E3 ligase ligand-linker conjugate. Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc incorporates the Thalidomide based cereblon ligand and a linker. Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc can be used for the synthesis of PROTAC BET degrader[1]. (From patent WO2017180417A1 compound s7).

  • CAS Number: 1799711-31-1
  • MF: C30H42N4O11
  • MW: 634.67
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pomalidomide-PEG3-C2-NH2 hydrochloride

Pomalidomide-PEG3-C2-NH2 (Cereblon Ligand-Linker Conjugates 5) hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology[1].

  • CAS Number: 2446474-09-3
  • MF: C21H29ClN4O7
  • MW: 484.93
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide fluoride

E3 ligase Ligand 4 is a ligand of E3 ligase, used in PROTAC technology.

  • CAS Number: 835616-60-9
  • MF: C13H9FN2O4
  • MW: 276.22000
  • Catalog: Ligand for E3 Ligase
  • Density: 1.570±0.06 g/cm3(Predicted)
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A