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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2,5-Dioxopyrrolidin-1-yl 1-(9H-fluoren-9-yl)-3-oxo-2,7,10,13,16,19,22,25,28,31,34,37,40-tridecaoxa-4-azatritetracontan-43-oate

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

  • CAS Number: 2227246-92-4
  • MF: C46H68N2O18
  • MW: 937.03
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Biotin-PEG3-CH2COOH

Biotin-PEG3-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1189560-96-0
  • MF: C18H31N3O7S
  • MW: 433.520
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 769.1±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 419.0±32.9 °C

11-Maleimidoundecanoic acid

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

  • CAS Number: 57079-01-3
  • MF: C15H23NO4
  • MW: 281.347
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 452.8±18.0 °C at 760 mmHg
  • Melting Point: 89-90ºC
  • Flash Point: 227.6±21.2 °C

Bromoacetamido-PEG3-acid

Bromoacetamido-PEG3-C2-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1807534-79-7
  • MF: C11H20BrNO6
  • MW: 342.18
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

S-Acetyl-peg2-t-butyl ester

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

  • CAS Number: 1820641-93-7
  • MF: C13H24O5S
  • MW: 292.39
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NH2-PEG6-C1-Boc

NH2-PEG6-C1-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 297162-50-6
  • MF: C18H37NO8
  • MW: 395.49
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Zxh-1-161

ZXH-1-161 is a potent cereblon (CRBN) modulator with an IC50 value of 39 nM in MM1.S wild type cells. ZXH-1-161 has selective degradation activity towards GSPT1. ZXH-1-161 can be used for researching multiple myeloma[1].

  • CAS Number: 2407654-51-5
  • MF: C26H24N6O3
  • MW: 468.51
  • Catalog: Ligand for E3 Ligase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

E3 ligase Ligand-Linker Conjugates 3

E3 ligase Ligand-Linker Conjugates 3 is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.

  • CAS Number: 2101200-09-1
  • MF: C26H35N7O5S
  • MW: 557.67
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Carboxy-PEG2-sulfonic acid

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

  • CAS Number: 1817735-45-7
  • MF: C7H14O7S
  • MW: 242.25
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-Desthiobiotin-N-bis(PEG4-NHS ester)

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

  • CAS Number: 2353409-61-5
  • MF: C40H65N5O18
  • MW: 903.97
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ms-PEG6-THP

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

  • CAS Number: 42607-89-6
  • MF: C18H36O10S
  • MW: 444.54
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

S-acetyl-PEG3-Boc

S-acetyl-PEG3-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1818294-27-7
  • MF: C15H28O6S
  • MW: 336.444
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 413.9±35.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 188.4±14.0 °C

2,2'-((Oxybis(ethane-2,1-diyl))bis(oxy))diethanol

PROTAC Linker 18 is a PROTAC linker, which refers to the alkyl/ether composition. PROTAC Linker 18 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: 112-60-7
  • MF: C8H18O5
  • MW: 194.225
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 328.0±0.0 °C at 760 mmHg
  • Melting Point: -5.6 °C(lit.)
  • Flash Point: 176.7±0.0 °C

cis-MZ 1

cis-MZ 1 is a negative control of MZ 1 (HY-107425). cis-MZ 1 is a PROTAC targeting to BRD4[1].

  • CAS Number: 1797406-72-4
  • MF: C49H60ClN9O8S2
  • MW: 1002.64
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KTX-951

KTX-951 is an IRAK4 degrader (DC50=18 nM). KTX-951 (10 mg/kg) shows the oral bioavailability (F%) of 22% in a rat model. KTX-951 has good anticancer potential[1].

  • CAS Number: 2573298-36-7
  • MF: C46H52F2N8O6
  • MW: 850.95
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

1,14-Diazido-3,6,9,12-tetraoxatetradecane

Azido-PEG4-azide is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 182760-73-2
  • MF: C10H20N6O4
  • MW: 288.30400
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MS5033

MS5033 is a potent PROTAC-based AKT (protein kinase B) degrader, with a DC50 of 430 nM in PC3 cells[1].

  • CAS Number: 2376137-29-8
  • MF: C51H66ClN11O11
  • MW: 1044.59
  • Catalog: Akt
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

1,1,1-Trifluoroethyl-PEG2-azide

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

  • CAS Number: 1835759-68-6
  • MF: C6H10F3N3O2
  • MW: 213.16
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Acid-PEG5-mono-methyl ester

Acid-PEG5-mono-methyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1309460-30-7
  • MF: C15H28O9
  • MW: 352.377
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 469.4±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 161.3±22.2 °C

tans-4-Hydroxy-D-proline methyl ester hydrochloride

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

  • CAS Number: 481704-21-6
  • MF: C6H12ClNO3
  • MW: 181.617
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tetraethylene glycol monomethyl ether

Tetraethylene glycol monomethyl ether is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 23783-42-8
  • MF: C9H20O5
  • MW: 208.252
  • Catalog: PROTAC Linker
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 285.4±25.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 126.4±23.2 °C

CRBN-6-5-5-VHL

CRBN-6-5-5-VHL is a potent and selective cereblon (CRBN) degrader with a DC50 value of 1.5 nM. CRBN-6-5-5-VHL has almost no effect on the degradation of the neo-substrates IKZF1 and IKZF3[1].

  • CAS Number: 2362575-45-7
  • MF: C51H69N7O10S
  • MW: 972.20
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG3-OH

m-PEG3-alcohol is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 112-35-6
  • MF: C7H16O4
  • MW: 164.199
  • Catalog: PROTAC Linker
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 233.9±20.0 °C at 760 mmHg
  • Melting Point: -44ºC
  • Flash Point: 95.3±21.8 °C

(S,R,S)-AHPC-Boc-trans-3-aminocyclobutanol-Pip-CH2COOH

(S,R,S)-AHPC-Boc-trans-3-aminocyclobutanol-Pip-CH2COOH (VH032-Boc-trans-3-aminocyclobutanol-Pip-CH2COOH) is a E3 ligase ligand-linker conjugate that contains on one end a VHL ligand. (S,R,S)-AHPC-Boc-trans-3-aminocyclobutanol-Pip-CH2COOH is used in PROTAC technology[1].

  • CAS Number: 2086301-47-3
  • MF: C39H58N6O7S
  • MW: 754.98
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG5-S-methyl ethanethioate

Azido-PEG5-S-methyl ethanethioate is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1352221-64-7
  • MF: C14H27N3O6S
  • MW: 365.45
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SIAIS178

SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC50 of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity[1].

  • CAS Number: 2376047-73-1
  • MF: C50H62ClN11O6S2
  • MW: 1012.68
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NH2-C2-amido-C2-Boc

NH2-C2-amido-C2-Boc is a PROTAC linker, which refers to the alkyl/ether composition. NH2-C5-NH-Boc can be used in the synthesis of a series of PROTACs, such as the PROTAC CDK2/9 Degrader-1 (HY-130709)[1].

  • CAS Number: 1692613-62-9
  • MF: C10H20N2O3
  • MW: 216.28
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Hydroxy-PEG5-C2-methyl ester

Hydroxy-PEG5-C2-methyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2100306-80-5
  • MF: C14H28O8
  • MW: 440.53
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Aminooxy-PEG8-acid

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

  • CAS Number: 2055013-68-6
  • MF: C19H39NO11
  • MW: 457.51
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propanol-PEG3-CH2OH

Propanol-PEG3-CH2OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 112935-57-6
  • MF: C10H22O5
  • MW: 222.28
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A