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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Azido-PEG7-azide

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

  • CAS Number: 225523-86-4
  • MF: C16H32N6O7
  • MW: 420.461
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Acid-PEG3-C2-Boc

Acid-PEG3-C2-Boc is a PEG- and Alkyl/ether-based PROTAC linker can be used in the synthesis of PROTACs for the degradation of EGFR and inhibition of mTOR[1][2].

  • CAS Number: 1807539-06-5
  • MF: C14H26O7
  • MW: 306.352
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 423.2±35.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 147.2±19.4 °C

TCO4-PEG3-Maleimide

TCO4-PEG3-Maleimide is a PROTAC linker and belongs to the PEG class. TCO4-PEG3-Maleimide contains TCO and Maleimide groups, which can undergo specific "click" reactions with tetrazine groups or thiol groups, or "mercapto-acrylamide" reactions.

  • CAS Number: 1914971-04-2
  • MF: C24H37N3O8
  • MW: 495.57
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 703.1±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 379 °C

H-Hyp-OMe hydrochloride

H-Hyp-OMe hydrochloride is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). H-Hyp-OMe hydrochloride is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1]<

  • CAS Number: 40216-83-9
  • MF: C6H12ClNO3
  • MW: 181.617
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: 247.2ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 103.3ºC

Aminooxy-PEG2-methane

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

  • CAS Number: 54149-49-4
  • MF: C5H13NO3
  • MW: 135.16
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HO-PEG8-CH2COOH

HO-PEG8-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 780006-30-6
  • MF: C18H36O11
  • MW: 428.47
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC BRD9 Degrader-1

PROTAC BRD9 Degrader-1 is a lead PROTAC BRD9 chemical degrader, which can be used as a selective probe useful for the study of BAF complex biology[1].

  • CAS Number: 2097971-01-0
  • MF: C42H45N7O12S2
  • MW: 903.98
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

1-Amino-3,6,9,12-tetraoxapentadecane-15-hydrazide

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

  • CAS Number: 1449390-65-1
  • MF: C12H26N2O6
  • MW: 294.34
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PEG5-bis-(ethyl phosphonate)

PEG5-bis-(Ethyl phosphonate) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1446282-28-5
  • MF: C20H44O11P2
  • MW: 522.5
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC ERα Degrader-4

PROTAC ERα Degrader-4 is a highly potent and selectivePROTAC ERα degrader (Ki: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER+ breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.

  • CAS Number: 2521299-80-7
  • MF: C55H62F3N5O10S2
  • MW: 1074.23
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG7-azide

m-PEG7-azide is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 208987-04-6
  • MF: C15H31N3O7
  • MW: 365.42300
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG1-methylamine

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

  • CAS Number: 1835759-88-0
  • MF: C5H12N4O
  • MW: 144.17
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG2-C2-Boc

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

  • CAS Number: 1271728-79-0
  • MF: C11H21N3O4
  • MW: 259.302
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-(m-PEG4)-N'-(hydroxy-PEG2)-Cy5

N-(m-PEG4)-N'-(hydroxy-PEG2)-Cy5 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2107273-12-9
  • MF: C40H57ClN2O7
  • MW: 713.34
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pomalidomide-PEG1-NH2-1 hydrochloride

Pomalidomide-PEG1-NH2 hydrochloride is a crosslinker-E3 ligase ligand conjugate, consisting of an E3 ligase ligand pomalidomide and a PEGylated crosslinker with terminal amine for reactivity with a carboxyl group on the target ligand[1].

  • CAS Number: 2380273-67-4
  • MF: C17H19ClN4O6
  • MW: 410.81
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

JH-XII-03-02

JH-XII-03-02 is a potent and selective LRRK2 PROTAC degrader. JH-XII-03-02 can be used for parkinson's Disease (PD)?research[1].

  • CAS Number: 2415900-86-4
  • MF: C43H51N9O10
  • MW: 853.92
  • Catalog: LRRK2
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-amido-PEG8-NHS ester

Mal-amido-PEG8-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 756525-93-6
  • MF: C30H47N3O15
  • MW: 689.70500
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG5-NHS ester

m-PEG5-NHS ester is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 874208-94-3
  • MF: C16H27NO9
  • MW: 377.38700
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-(Hydroxy-PEG3)-N-bis(PEG4-t-butyl ester)

N-(Hydroxy-PEG3)-N-bis(PEG4-Boc) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2112734-70-8
  • MF: C38H75NO16
  • MW: 802.00
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AD4

AD4 is an artemisinin derivative that is a proteolytic targeting chimera (PROTAC) targeting PCLAF. AD4 can effectively degrade PCLAF in RS4;11 cells (IC50: 0.6 nM), thereby activating the p21/Rb axis and exerting anti-tumor activity. AD4 also prolonged survival of RS4;11-transplanted NOD/SCID mice, with in vivo efficacy[1].

  • CAS Number: 2918262-09-4
  • MF: C55H78N4O15
  • MW: 1035.23
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-O-C6-COOH

Thalidomide-O-C6-COOH 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: 2169266-69-5
  • MF: C20H22N2O7
  • MW: 402.40
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Benzyl-PEG5-Ms

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

  • CAS Number: 1807539-07-6
  • MF: C18H30O8S
  • MW: 406.491
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 529.4±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 274.0±30.1 °C

Amino-PEG9-amine

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

  • CAS Number: 474082-35-4
  • MF: C20H44N2O9
  • MW: 456.571
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 527.4±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 263.9±22.4 °C

m-PEG4-hydrazide

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

  • CAS Number: 1449390-68-4
  • MF: C10H22N2O5
  • MW: 250.292
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 408.1±35.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 200.6±25.9 °C

N-Boc-Azido-tris(ethylenoxy)-L-alanine

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

  • CAS Number: 2054345-68-3
  • MF: C14H26N4O7
  • MW: 362.38
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG-acid

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

  • CAS Number: 125220-94-2
  • MF: (C2H4O)nC4H8O3
  • MW: 588.683
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 628.8±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 189.3±25.0 °C

Thalidomide-O-amido-PEG-C2-NH2 hydrochloride

Thalidomide-O-amido-PEG-C2-NH2 hydrochloride, a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs[1].

  • CAS Number: 2204226-02-6
  • MF: C19H23ClN4O7
  • MW: 454.86
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG4-Tos

m-PEG4-Tos is a derivative of silybin ethers, extracted from patent CN105037337A (compound III-b). m-PEG4-Tos is a PEG-based PROTAC linker can be used in the synthesis of Silymarin (HY-W043277)[1].

  • CAS Number: 62921-76-0
  • MF: C16H26O7S
  • MW: 380.45400
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-NH-Boc

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

  • CAS Number: 134272-63-2
  • MF: C11H16N2O4
  • MW: 240.25600
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 110-115 °C
  • Flash Point: N/A

Boc-NH-PEG4-azide

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

  • CAS Number: 940951-99-5
  • MF: C15H30N4O6
  • MW: 362.42
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A