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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Biotin-PEG12-acid

Biotin-PEG12-acid is a biotin-labeled, PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1621423-14-0
  • MF: C37H69N3O16S
  • MW: 844.019
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 932.7±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 517.9±34.3 °C

Acid-PEG5-TEMPO

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

  • CAS Number: 2055040-79-2
  • MF: C23H44N2O9
  • MW: 492.60
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Hydroxy-PEG4-CH2COOH

Hydroxy-PEG4-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 70678-95-4
  • MF: C10H20O7
  • MW: 252.26200
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Methylamino-PEG3-azide

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

  • CAS Number: 1355197-57-7
  • MF: C9H20N4O3
  • MW: 232.280
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(S,R,S)-AHPC-amido-C7-acid

(S,R,S)-AHPC-amido-C7-acid incorporates a VHL ligand for the E3 ubiquitin ligase and a PROTAC linker. (S,R,S)-AHPC-amido-C5-acid can be used to design PROTACs[1].

  • CAS Number: 2172819-76-8
  • MF: C31H44N4O6S
  • MW: 600.77
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-(2,6-Dioxopiperidin-3-yl)phthalimidine-C5-Br

2-(2,6-Dioxopiperidin-3-yl)phthalimidine-C5-Br is a E3 ligase ligand-linker conjugate for PROTAC.

  • CAS Number: 2411022-24-5
  • MF: C18H21BrN2O3
  • MW: 393.27
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

t-Boc-N-amido-PEG5-NHS ester

Boc-N-PEG5-C2-NHS ester is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].

  • CAS Number: 2055040-78-1
  • MF: C22H38N2O11
  • MW: 506.54
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bis-(N,N'-NHS-PEG4)-Cy5

Bis-(N,N'-PEG4-NHS ester)-Cy5 is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2107273-48-1
  • MF: C55H73ClN4O16
  • MW: 1081.64
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

JQAD1

JQAD1 is a CRBN-dependent PROTAC that selectively targets EP300 for degradation. JQAD1 suppresses EP300 expression and the H3K27ac modification. JQAD1 induces apoptosis. JQAD1 can be used in research of cancer[1].

  • CAS Number: 2417097-18-6
  • MF: C48H52F4N6O9
  • MW: 932.95
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG8-hydrazide

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

  • CAS Number: 2353410-11-2
  • MF: C19H39N5O9
  • MW: 481.54
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(+)-Biotin-PEG2-azide

Biotin-PEG2-CH2CH2N3 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 945633-30-7
  • MF: C16H28N6O4S
  • MW: 400.49600
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bis-PEG5-acid

Bis-PEG4-acid is a PEG PROTAC linker.

  • CAS Number: 31127-85-2
  • MF: C12H22O8
  • MW: 294.30
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HO-PEG13-OH

HO-PEG13-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 17598-96-8
  • MF: C26H54O14
  • MW: 590.69900
  • Catalog: PROTAC Linker
  • Density: 1.116g/cm3
  • Boiling Point: 631.6ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-NH-PEG8-NHS ester

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

  • CAS Number: 1334170-03-4
  • MF: C38H52N2O14
  • MW: 760.825
  • Catalog: PROTAC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-PEG4-acid

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

  • CAS Number: 518044-41-2
  • MF: C15H23NO8
  • MW: 345.34500
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cl-C6-PEG4-C3-COOH

Cl-C6-PEG4-C3-COOH is a PROTAC linker can be used in the synthesis of chloroalkane-containing PROTACs (HaloPROTACs)[1].

  • CAS Number: 2127391-58-4
  • MF: C18H35ClO6
  • MW: 382.92
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tetraethyl octane-1,8-diylbis(phosphonate)

Tetraethyl octane-1,8-diylbis(phosphonate) is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 5943-61-3
  • MF: C16H36O6P2
  • MW: 386.40100
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bis-(m-PEG4)-amidohexanoic acid

Bis-(m-PEG4)-amidohexanoic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2353409-74-0
  • MF: C26H50N2O12
  • MW: 582.68
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

endo-BCN-PEG4-Boc

endo-BCN-PEG4-Boc is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 1807501-83-2
  • MF: C26H43NO8
  • MW: 497.621
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 594.3±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 313.2±28.7 °C

endo-BCN-PEG8-acid

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

  • CAS Number: 2126805-02-3
  • MF: C30H51NO12
  • MW: 617.73
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

S-acetyl-PEG5-alcohol

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

  • CAS Number: 1000415-61-1
  • MF: C12H24O6S
  • MW: 296.38
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-NH-C4-NH2 TFA

Thalidomide-NH-C4-NH2 TFA (compound 29c) is an E3 ligase ligand-linker conjugate, and incorporates the Thalidomide based cereblon ligand and a linker. Thalidomide-NH-C4-NH2 TFA is used in PROTAC BRD2/BRD4 degrader-1 (HY-130612). PROTAC BRD2/BRD4 degrader-1 is a potent and selective BET protein BRD4 and BRD2 degrader[1].

  • CAS Number: 2093387-50-7
  • MF: C19H21F3N4O6
  • MW: 458.39
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Lenalidomide-d5

Lenalidomide-d5 is deuterium labeled Lenalidomide. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells[1][2].

  • CAS Number: 1227162-34-6
  • MF: C13H8D5N3O3
  • MW: 264.29
  • Catalog: Apoptosis
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 614.0±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 325.1±31.5 °C

TCO4-PEG2-Maleimide

TCO4-PEG2-Maleimide is a PROTAC linker and belongs to the PEG class. TCO4-PEG2-Maleimide contains TCO and Maleimide groups, which can undergo specific "click" reactions with tetrazine groups or thiol groups, or "mercapto-acrylamide" reactions.

  • CAS Number: 2141981-85-1
  • MF: C22H33N3O7
  • MW: 451.51
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BSJ-03-204

BSJ-03-204 is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 does not induce IKZF1/3 degradation and has anti-cancer activity[1].

  • CAS Number: 2349356-09-6
  • MF: C43H48N10O8
  • MW: 832.90
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bromo-PEG5-azide

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

  • CAS Number: 1402411-90-8
  • MF: C12H24BrN3O5
  • MW: 370.24
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Amino-PEG9-alcohol

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

  • CAS Number: 15332-95-3
  • MF: C18H39NO9
  • MW: 413.50
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

t-Boc-Aminooxy-PEG3-alcohol

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

  • CAS Number: 252378-66-8
  • MF: C11H23NO6
  • MW: 265.303
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC FLT-3 degrader 1

PROTAC FLT-3 degrader 1 is an FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM. Anti-proliferative activity; apoptosis induction[1].

  • CAS Number: 2230826-81-8
  • MF: C52H61N9O9S2
  • MW: 1020.23
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azide-PEG5-Boc

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

  • CAS Number: 1415800-41-7
  • MF: C17H33N3O7
  • MW: 391.460
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A