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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t-Butyl acetate-PEG2-CH2COOH

t-Butyl acetate-PEG2-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 883564-93-0
  • MF: C12H22O7
  • MW: 278.30
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ERK-CLIPTAC

ERK-CLIPTAC is a PROTAC molecule that triggers the degradation of ERK[1].

  • CAS Number: 2087490-46-6
  • MF: C60H61ClN12O9
  • MW: 1129.65
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC EED degrader-1

PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit[1].

  • CAS Number: 2639882-72-5
  • MF: C55H60FN11O8S
  • MW: 1054.20
  • Catalog: Histone Methyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG3-Ms

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

  • CAS Number: 60696-83-5
  • MF: C6H14O5S
  • MW: 198.24
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-(Biotin-peg4)-n-bis(peg4-t-butyl ester)

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

  • CAS Number: 2112730-79-5
  • MF: C50H94N4O18S
  • MW: 1071.36
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Benzyl-PEG3-methyl ester

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

  • CAS Number: 127457-61-8
  • MF: C15H22O5
  • MW: 282.33
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG6-(CH2)8-phosphonic acid

m-PEG6-(CH2)6-Phosphonic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2028284-71-9
  • MF: C19H41O9P
  • MW: 444.50
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CC-885-CH2-PEG1-NH-CH3

CC-885-CH2-PEG1-NH-CH3 is a neoDegrader that can be used in the synthesis of Antibody neoDegrader Conjugate (AnDC)[1][2].

  • CAS Number: 2722698-03-3
  • MF: C26H30ClN5O5
  • MW: 528.00
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(SRS)-AHPC-PEG4-NH2 hydrochloride

E3 ligase Ligand-Linker Conjugates 7 is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.

  • CAS Number: 2064292-52-8
  • MF: C32H50ClN5O8S
  • MW: 700.29
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG3-maleimide

Azido-PEG3-maleimide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. Azido-PEG3-maleimide is also a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].

  • CAS Number: 1858264-36-4
  • MF: C15H23N5O6
  • MW: 369.373
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pomalidomide-C3-NH2

Pomalidomide-C3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology[1].

  • CAS Number: 2093388-20-4
  • MF: C16H19ClN4O4
  • MW: 366.80
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(S,R,S)-AHPC-C4-NH2 dihydrochloride

(S,R,S)-AHPC-C4-NH2 dihydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for EED-Targeted PROTAC[1].

  • CAS Number: 2341796-78-7
  • MF: C27H41Cl2N5O4S
  • MW: 602.62
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

I-PEG6-OH

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

  • CAS Number: 136399-07-0
  • MF: C12H25IO6
  • MW: 392.23
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Methylamino-PEG4-Boc

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

  • CAS Number: 1621616-14-5
  • MF: C16H33NO6
  • MW: 335.436
  • Catalog: PROTAC Linker
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 401.7±35.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 196.8±25.9 °C

HDAC6 degrader-3

HDAC6 degrader-3 is a potent and selective HDAC6 degrader via ternary complex formation and the ubiquitin-proteasome pathway with a DC50 value of 19.4 nM. HDAC6 degrader-3 has IC50s of 4.54 nM and 0.647 μM for HDAC6 and HDAC1, respectively. HDAC6 degrader-3 causes strong hyperacetylation of α-tubulin[1].

  • CAS Number: 2785404-83-1
  • MF: C41H41F4N7O11
  • MW: 883.80
  • Catalog: HDAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fluorescein-PEG6-bis-NHS ester

Fluorescein-PEG6-bis-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2055105-59-2
  • MF: C44H50N4O17S
  • MW: 938.95
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Hydroxy-PEG3-NHS

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

  • CAS Number: 1807518-71-3
  • MF: C13H21NO8
  • MW: 319.308
  • Catalog: PROTAC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 458.0±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 230.8±31.5 °C

S-Acetyl-PEG8-OH

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

  • CAS Number: 1334177-81-9
  • MF: C18H36O9S
  • MW: 428.538
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 512.3±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 263.6±30.1 °C

FmocNH-PEG4-t-butyl acetate

FmocNH-PEG4-t-butyl acetate is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 894427-95-3
  • MF: C29H39NO8
  • MW: 529.62200
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG4-(CH2)3-methyl ester

m-PEG4-CH2-methyl ester is a PEG- and Alkyl/ester-based PROTAC linker can be used in the synthesis of PROTACs[1].

  • CAS Number: 1920109-55-2
  • MF: C12H24O6
  • MW: 264.32
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dovitinib-RIBOTAC TFA

Dovitinib RIBOTAC TFA is a targeted RNA degrader that cleaves pre-miR-21 with enhanced potency and selectivity.

  • CAS Number: 2759351-69-2
  • MF: C53H57F4N9O12S
  • MW: 1120.13
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Amino-Tri-(carboxyethoxymethyl)-methane hydrochloride

Amino-Tri-(carboxyethoxymethyl)-methane hydrochloride is a cleavable PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Amino-Tri-(carboxyethoxymethyl)-methan hydrochloride is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1][2].

  • CAS Number: 1416771-72-6
  • MF: C13H24ClNO9
  • MW: 373.78
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG3-succinimidyl carbonate

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

  • CAS Number: 477775-77-2
  • MF: C12H19NO8
  • MW: 305.28100
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

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

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

  • CAS Number: 2353409-90-0
  • MF: C41H68N6O21
  • MW: 981.01
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC RIPK degrader-6

PROTAC RIPK degrader-6 (example 1) is a PROTAC targeting RIP Kinase degradation wherein the RIP2 kinase inhibitor is linked via a linker to a cereblon binder[1].

  • CAS Number: 2089205-64-9
  • MF: C43H48N6O11S2
  • MW: 889.00
  • Catalog: RIP kinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SPDP-PEG4-acid

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

  • CAS Number: 581065-97-6
  • MF: C19H30N2O7S2
  • MW: 462.581
  • Catalog: PROTAC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 677.3±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 363.4±31.5 °C

Lipoamido-PEG4-azide

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

  • CAS Number: 890016-39-4
  • MF: C16H30N4O4S2
  • MW: 406.564
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

dTRIM24

dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC.

  • CAS Number: 2170695-14-2
  • MF: C55H68N8O13S2
  • MW: 1113.3
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pyrene azide 3

Pyrene azide 3 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2252168-06-0
  • MF: C26H28N4O3
  • MW: 444.53
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG11-CH2COOH

Azido-PEG11-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2567584-97-6
  • MF: C24H47N3O13
  • MW: 585.64
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A