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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m-PEG6-Br

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

  • CAS Number: 125562-29-0
  • MF: C13H27BrO6
  • MW: 359.254
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 385.1±37.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 158.2±25.0 °C

Azido-PEG4-Boc

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

  • CAS Number: 581066-04-8
  • MF: C15H29N3O6
  • MW: 347.407
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pomalidomide-C6-O-C5-O-C4-COOH

Pomalidomide-C6-O-C5-O-C4-COOH is a E3 ligase ligand-linker conjugate comprising a Pomalidomide (HY-10984)-based cereblon ligand and linker. Pomalidomide-C6-O-C5-O-C4-COOH can be used for the synthesis of PROTACs[1].

  • CAS Number: 2375774-54-0
  • MF: C29H41N3O8
  • MW: 559.65
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DB1113

DB1113 (Example 24) is a bifunctional compound targeted protein degradation of kinases. DB1113 degrades ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2, and ULK1. DB1113 can be used for research of disease or disorder mediated by aberrant kinase activity[1].

  • CAS Number: 2769753-53-7
  • MF: C59H68F3N13O6S
  • MW: 1144.31
  • Catalog: Ferroptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-Boc-1,5-diaminopentane

PROTAC Linker 23 is a PROTAC linker, which refers to the alkyl chain composition. PROTAC Linker 23 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: 51644-96-3
  • MF: C10H22N2O2
  • MW: 202.294
  • Catalog: PROTAC Linker
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 309.2±25.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 140.8±23.2 °C

Br-C10-methyl ester

Br-C10-methyl ester is a PROTAC linker, which refers to the alkyl/ether composition. Br-C10-methyl ester is used in the synthesis of a series of PROTACs (MS432).  PROTACs contain two different ligands connected by a linker; one is the VHL ligand portion and the other is for the target protein[1].

  • CAS Number: 6287-90-7
  • MF: C12H23BrO2
  • MW: 279.21400
  • Catalog: PROTAC Linker
  • Density: 1.157 g/mL at 25ºC(lit.)
  • Boiling Point: 115ºC0.04 mm Hg(lit.)
  • Melting Point: 13°C(lit.)
  • Flash Point: >230 °F

E3 ligase Ligand-Linker Conjugates 6 Free Base

E3 ligase Ligand-Linker Conjugates 6 Free Base is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.

  • CAS Number: 2010159-60-9
  • MF: C28H41N5O6S
  • MW: 575.72
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

VH032 analogue-1

VH032 analogue-1 is a VH032 (HY-120217) analog that acts as a ligand for VHL, recruiting von Hippel-Lindau (VHL) protein. VH032 analogue-1 will remove the protective group under acidic conditions and be directly used for PROTAC molecular synthesis. VH032 analogue-1 is a key intermediate in the synthesis of PROTACs based on VHL ligands.

  • CAS Number: 2111829-84-4
  • MF: C23H30N4O5S
  • MW: 474.57
  • Catalog: Ligand for E3 Ligase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-Tos-N-(t-butoxycarbonyl)-aminoxy-PEG4-Tos

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

  • CAS Number: 1817735-42-4
  • MF: C27H39NO11S2
  • MW: 617.73
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG4-NHS ester

m-PEG4-NHS ester is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 622405-78-1
  • MF: C14H23NO8
  • MW: 333.334
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 431.7±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 214.9±31.5 °C

Fmoc-Lys (biotin-PEG4)-OH

Fmoc-Lys (biotin-PEG4)-OH is a biotin-labeled, PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1334172-64-3
  • MF: C42H59N5O11S
  • MW: 842.01
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bromo-PEG3-bromide

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

  • CAS Number: 31255-26-2
  • MF: C8H16Br2O3
  • MW: 320.01900
  • Catalog: PROTAC Linker
  • Density: 1.57 g/cm3at 25°C (lit.)
  • Boiling Point: 146 °C at 0.06 Torr (lit.)
  • Melting Point: N/A
  • Flash Point: N/A

Biotin-PEG8-amine

Biotin-PEG8-amine is a biotin-labeled, PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2183447-27-8
  • MF: C28H54N4O10S
  • MW: 638.81
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dde Biotin-PEG4-alkyne

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

  • CAS Number: 1802908-00-4
  • MF: C32H50N4O8S
  • MW: 650.83
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PF-05231023

PF-05231023, a long-acting fibroblast growth factor 21 (FGF21) analog, is a FGF21-receptor agonist, suitable for development as a potential treatment for T2DM[1][5].

  • CAS Number: 1037589-69-7
  • MF: C26H32N4O8
  • MW: 528.55
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG4-C2-acid

Azido-PEG4-C2-acid a PEG-based PROTAC linker can be used in the synthesis of vRucaparib-TP4. Azido-PEG4-C2-acid is also a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

  • CAS Number: 1257063-35-6
  • MF: C11H21N3O6
  • MW: 291.30100
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tri(carboxyethyloxyethyl)amine

Tri-(PEG1-C2-acid) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1381861-95-5
  • MF: C15H27NO9
  • MW: 365.38
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Chloroacetamido-PEG4-NHS ester

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

  • CAS Number: 1353011-95-6
  • MF: C17H27ClN2O9
  • MW: 438.857
  • Catalog: PROTAC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-PEG4-Propargyl

Thalidomide-PEG4-Propargyl 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: 2098799-77-8
  • MF: C24H28N2O9
  • MW: 488.49
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ANB-NOS

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

  • CAS Number: 60117-35-3
  • MF: C11H7N5O6
  • MW: 305.203
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 131-133ºC
  • Flash Point: N/A

Bis(2-bromoethyl) ether

Bis2-bromoethyl ether is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 5414-19-7
  • MF: C4H8Br2O
  • MW: 231.914
  • Catalog: PROTAC Linker
  • Density: 1.8±0.1 g/cm3
  • Boiling Point: 216.3±0.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 85.0±0.0 °C

TCO-PEG3-amine

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

  • CAS Number: 1800507-93-0
  • MF: C17H32N2O5
  • MW: 344.45
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Biotin-PEG9-amine

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

  • CAS Number: 960132-48-3
  • MF: C30H58N4O11S
  • MW: 682.86700
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

A 410099.1 amide-PEG3-amine

A 410099.1 amide-PEG3-amine-Boc is a functionalized IAP ligand for PROTACs that incorporates an IAP ligand and an amide-PEG3 linker with terminal amine. A 410099.1 amide-PEG3-amine-Boc can conjugates with target protein ligands.

  • CAS Number: 2415256-19-6
  • MF: C40H64N6O9
  • MW: 772.97
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG4-O-NHS ester

m-PEG4-O-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 147912-03-6
  • MF: C14H23NO9
  • MW: 349.33400
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG7-Boc

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

  • CAS Number: 1818294-29-9
  • MF: C22H40O9
  • MW: 448.548
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 494.3±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 207.8±27.4 °C

Aminooxy-PEG8-methane HCl

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

  • CAS Number: 2055024-52-5
  • MF: C17H37NO9
  • MW: 399.48
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PEG4-sulfonic acid

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

  • CAS Number: 173459-90-0
  • MF: C8H18O7S
  • MW: 258.289
  • Catalog: PROTAC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-(Azido-PEG3-amido)-1,3-bis(NHS ester)

2-(Azido-PEG3-amido)-1,3-bis(NHS ester) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2320560-36-7
  • MF: C26H38N6O14
  • MW: 658.61
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Lenalidomide-PEG1-azide

Lenalidomide-PEG1-azide is a E3 ligase lgand-linker conjugate. Lenalidomide-PEG1-azide incorporates the Lenalidomide based cereblon ligand and a linker. Lenalidomide-PEG1-azide can be used to design a PROTAC BRD4 Degrader-2 (HY-133136)[1].

  • CAS Number: 2185795-67-7
  • MF: C17H18N6O5
  • MW: 386.36
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A