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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Hydroxy-PEG3-MS

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

  • CAS Number: 139115-89-2
  • MF: C7H16O6S
  • MW: 228.26300
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-Boc-serinol

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

  • CAS Number: 125414-41-7
  • MF: C8H17NO4
  • MW: 191.225
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 363.0±32.0 °C at 760 mmHg
  • Melting Point: 85-89ºC
  • Flash Point: 173.4±25.1 °C

Fmoc-N-PEG20-acid

Fmoc-N-amido-PEG20-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1952360-93-8
  • MF: C58H97NO24
  • MW: 1192.383
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 1033.9±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 579.1±34.3 °C

PROTAC GPX4 degrader-1

PROTAC GPX4 degrader-1 (DC-2) is a PROTAC-based GPX4 degrader, with a DC50 of 0.03 μM in HT1080 cells[1].

  • CAS Number: 2916433-81-1
  • MF: C50H57ClN10O10
  • MW: 993.50
  • Catalog: Ferroptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-PEG3-N'-(azide-PEG3)-Cy5

N-PEG3-N'-(azide-PEG3)-Cy5 (chloride) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2226235-96-5
  • MF: C39H54ClN5O6
  • MW: 724.33
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Biotin-PEG4-amino-t-Bu-DADPS-C3-alykne

Biotin-PEG4-amino-t-Bu-DADPS-C3-alykne is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2241685-22-1
  • MF: C42H62N4O9SSi
  • MW: 827.11
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG6-NH2

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

  • CAS Number: 1198080-04-4
  • MF: C15H29NO6
  • MW: 319.394
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 401.8±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 190.0±21.0 °C

PEG21

HO-PEG20-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 351342-08-0
  • MF: C40H82O21
  • MW: 899.07
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Biotin alkyne

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

  • CAS Number: 773888-45-2
  • MF: C13H19N3O2S
  • MW: 281.37400
  • Catalog: PROTAC Linker
  • Density: 1.185±0.06 g/cm3(Predicted)
  • Boiling Point: 614.8±50.0 °C(Predicted)
  • Melting Point: 169-170 °C
  • Flash Point: N/A

KRAS G12D inhibitor 17

KRAS G12D inhibitor 17 (example 8) is a quinazoline-linked (4R)-4-hydroxy-L-prolinamide compound, inducing degradation of G12D-mutation KRAS protein[1].

  • CAS Number: 2821793-99-9
  • MF: C60H65FN12O7S
  • MW: 1117.30
  • Catalog: Ras
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Phenol-amido-C1-PEG3-N3

PROTAC Linker 21 is a PROTAC linker, which refers to the alkyl/ether composition. PROTAC Linker 21 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: 1096439-18-7
  • MF: C14H20N4O5
  • MW: 324.33
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG6-CH2CH2COOH

m-PEG6-CH2CH2COOH is a PEG-based based PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 874208-91-0
  • MF: C16H32O9
  • MW: 368.42000
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-O-amido-C11-COOH

Thalidomide-O-amido-C11-COOH (compound IMiD acid 1) is an E3 ligase ligand and linker CRBN (Cereblon) conjugate. Thalidomide-O-amido-C11-COOH can be used to synthesize PROTAC that target the degradation of DOT1L[1].

  • CAS Number: 2473270-96-9
  • MF: C27H35N3O8
  • MW: 529.58
  • Catalog: PROTAC-linker Conjugate for PAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-NH-C9-NH2 hydrochloride

Thalidomide-NH-C9-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-NH-C9-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs[1].

  • CAS Number: 2305936-77-8
  • MF: C22H31ClN4O4
  • MW: 450.96
  • Catalog: Ligand for E3 Ligase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bis-PEG3-acid

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

  • CAS Number: 96517-92-9
  • MF: C10H18O7
  • MW: 250.24600
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-NH-PEG2-C2-NH2 hydrochloride

Thalidomide-O-amido-PEG3-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology[1].

  • CAS Number: 2245697-87-2
  • MF: C19H25ClN4O6
  • MW: 440.88
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TCO-PEG4-TCO

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

  • CAS Number: 2243569-23-3
  • MF: C28H48N2O8
  • MW: 540.69
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Diazo Biotin-PEG3-alkyne

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

  • CAS Number: 1884349-58-9
  • MF: C39H53N7O9S
  • MW: 795.94
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

t-Boc-Aminooxy-PEG4-t-butyl ester

t-Boc-Aminooxy-PEG4-t-butyl ester is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 1872433-64-1
  • MF: C20H39NO9
  • MW: 437.52
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-5-O-C4-NH2 hydrochloride

Thalidomide-5-O-C4-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C4-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs[1].

  • CAS Number: 2694727-93-8
  • MF: C17H20ClN3O5
  • MW: 381.81
  • Catalog: Ligand for E3 Ligase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HO-PEG7-CH2COOH

HO-PEG7-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2250056-27-8
  • MF: C16H32O10
  • MW: 384.42
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

EGNHS

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

  • CAS Number: 70539-42-3
  • MF: C18H20N2O12
  • MW: 456.35800
  • Catalog: PROTAC Linker
  • Density: 1.52g/cm3
  • Boiling Point: 603.4ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 318.7ºC

m-PEG5-phosphonic acid

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

  • CAS Number: 1807512-39-5
  • MF: C11H25O8P
  • MW: 316.29
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

t-Boc-N-Amido-PEG3-propargyl

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

  • CAS Number: 1333880-60-6
  • MF: C14H25NO5
  • MW: 287.35
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azide-PEG7-Tos

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

  • CAS Number: 1418561-41-7
  • MF: C21H35N3O9S
  • MW: 505.58
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Benzyl-PEG10-alcohol

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

  • CAS Number: 908258-44-6
  • MF: C27H48O11
  • MW: 548.66300
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG4-tetra-Ac-beta-D-galactose

Propargyl-PEG4-tetra-Ac-beta-D-galactose is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1397682-61-9
  • MF: C25H38O14
  • MW: 562.559999999999
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG4-hydrazide HCl

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

  • CAS Number: 2170240-96-5
  • MF: C11H23N5O5
  • MW: 305.33
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Di(N-succinimidyl)adipate

Di(N-succinimidyl)adipate is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 59156-70-6
  • MF: C14H16N2O8
  • MW: 340.28500
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Br-PEG6-C2-acid

Br-PEG6-C2-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 309916-91-4
  • MF: C15H29BrO8
  • MW: 417.29
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A