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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Methyltetrazine-NHS ester

Methyltetrazine-Ph-NHS ester is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1644644-96-1
  • MF: C15H13N5O4
  • MW: 327.29
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-NH-PEG15-CH2CH2COOH

Fmoc-NH-PEG15-CH2CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2378590-46-4
  • MF: C48H77NO19
  • MW: 972.12
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

E3 ligase Ligand-Linker Conjugates 30

E3 ligase Ligand-Linker Conjugates 30 incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase, and a PROTAC linker. E3 ligase Ligand-Linker Conjugates 30 can be used to design PROTAC MDM2 degrader[1].

  • CAS Number: 2093416-31-8
  • MF: C21H28N4O7
  • MW: 448.47
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

22-(tert-Butoxy)-22-oxodocosanoic acid

22-(tert-Butoxy)-22-oxodocosanoic acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). 22-(tert-Butoxy)-22-oxodocosanoic acid is also a alkyl chain-based PROTAC linker that can be used in t

  • CAS Number: 1642333-05-8
  • MF: C26H50O4
  • MW: 426.673
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC ER Degrader-3

PROTAC ER Degrader-3 is an intermediate for synthesis of PAC. PAC comprises an antibody conjugated via a linker to a PROTAC. PAC extracts from patent WO2017201449A1, compound LP2. PAC is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).

  • CAS Number: 2158322-29-1
  • MF: C71H77N7O12
  • MW: 1220.41
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

dTAGV-1 TFA

dTAGV-1 TFA is a potent and selective degrader of mutant FKBP12F36V fusion proteins. dTAGV-1 TFA can induce degradation of FKBP12F36V-Nluc in vivo[1].

  • CAS Number: 2624313-15-9
  • MF: C70H91F3N6O16S
  • MW: 1361.56
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Acid-apeg6-acid n-boc

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

  • CAS Number: 2055023-35-1
  • MF: C23H43NO12
  • MW: 525.59
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-(Propargyl-PEG4-carbonyl)-N-bis(PEG1-methyl ester)

N-(Propargyl-PEG4-carbonyl)-N-bis(PEG1-methyl ester) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2112732-01-9
  • MF: C24H41NO11
  • MW: 519.58
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SLF-amido-C2-COOH

Target Protein-binding moiety 13 is a synthetic ligand for FKBP (SLF), which is used in the synthesis of PROTACs.

  • CAS Number: 1092369-24-8
  • MF: C34H44N2O9
  • MW: 624.72
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-Benzyl-N-bis(PEG1-OH)

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

  • CAS Number: 119580-47-1
  • MF: C15H25NO4
  • MW: 283.36
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5-[Boc(methyl)amino]pentanal

5-[Boc(methyl)amino]pentanal is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1620280-47-8
  • MF: C11H21NO3
  • MW: 215.29
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-NH-CBP/p300 ligand 2

Thalidomide-NH-CBP/p300 ligand 2 (P-007) is a PROTAC-based CBP and p300 degrader (extracted from patent WO2020173440)[1].

  • CAS Number: 2484739-21-9
  • MF: C48H57F2N11O6
  • MW: 922.03
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Benzyl-PEG4-amine

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

  • CAS Number: 86770-76-5
  • MF: C15H25NO4
  • MW: 283.36300
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: 390.4±32.0°C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: N/A

Benzyl-PEG5-amine

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

  • CAS Number: 86770-77-6
  • MF: C17H29NO5
  • MW: 327.416
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 429.7±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 210.7±21.0 °C

PROTAC CDK9 degrader-4

PROTAC CDK9 degrader-4 is a highly potent and efficacious CDK9 degrader for targeting transcription regulation.

  • CAS Number: 2411021-01-5
  • MF: C43H56N10O5
  • MW: 792.97
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG9-azide

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

  • CAS Number: 1171122-72-7
  • MF: C20H40N6O9
  • MW: 508.57
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

sulfo-NHS-acetate

Sulfo-NHS-Acetate is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 152305-87-8
  • MF: C6H7NO7S
  • MW: 237.18700
  • Catalog: PROTAC Linker
  • Density: 1.8g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Boc-NH-PEG5-CH2CH2COOH

Boc-NH-PEG5-CH2CH2COOH is a PEG-based PROTAC linker can be used in the synthesis of PROTAC[1].

  • CAS Number: 1347750-78-0
  • MF: C18H35NO9
  • MW: 409.472
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 536.9±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 278.5±30.1 °C

Bromo-PEG1-C2-azide

Bromo-PEG1-C2-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1144106-65-9
  • MF: C4H8BrN3O
  • MW: 194.03
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MS-PEG12-THP

MS-PEG12-THP is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 552886-58-5
  • MF: C30H60O16S
  • MW: 708.85
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC MDM2 Degrader-1

PROTAC MDM2 Degrader-1 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-1 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase[1].

  • CAS Number: 2249944-98-5
  • MF: C74H84Cl4N10O13
  • MW: 1463.33
  • Catalog: MDM-2/p53
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-Boc-PEG-t-butyl ester

N-Boc-PEG-t-butyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 145119-18-2
  • MF: C14H27NO5
  • MW: 289.37
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azide-PEG4-Tos

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

  • CAS Number: 168640-82-2
  • MF: C15H23N3O6S
  • MW: 373.42500
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

FAK PROTAC B5

FAK PROTAC B5 (Compound B5) is a FAK PROTAC degrader with an IC50 value of 14.9 nM. FAK PROTAC B5 presents strong FAK degradation activity, antiproliferative activity, outstanding plasma stability and moderate membrane permeability. FAK PROTAC B5 inhibits cell migration and invasion[1].

  • CAS Number: 2471525-44-5
  • MF: C41H43ClN10O7
  • MW: 823.30
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

dTAG-47

dTAG-47, heterobifunctional dTAG molecule, targets mutant FKBP12 (FKBP12F36V). FKBP12F36V serves as a degradation tag (dTAG) and is fused to a protein of interest. dTAG-47 can be used for the research of basal-like breast cancers (BBC)[1].

  • CAS Number: 2265886-81-3
  • MF: C59H73N5O14
  • MW: 1076.24
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-(Azido-PEG2-amido)-1,3-propandiol

2-(Azido-PEG2-amido)-13-propandiol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1398044-52-4
  • MF: C10H20N4O5
  • MW: 276.290
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-Phthalimidehydroxy-acetic acid

2-Phthalimidehydroxy-acetic acid is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 134724-87-1
  • MF: C10H7NO5
  • MW: 221.16600
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Benzyl-PEG2-ethoxyethane-PEG2

Benzyl-PEG2-ethoxyethane-PEG2 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2115897-18-0
  • MF: C19H32O5
  • MW: 340.45
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Biotin-PFP ester

Biotin-PFP ester is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 120550-35-8
  • MF: C16H15F5N2O3S
  • MW: 410.359
  • Catalog: PROTAC Linker
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 555.3±50.0 °C at 760 mmHg
  • Melting Point: 190.0 to 194.0 °C
  • Flash Point: 289.6±30.1 °C

Azido-PEG10-amine

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

  • CAS Number: 912849-73-1
  • MF: C22H46N4O10
  • MW: 526.62100
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A