PROTAC
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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.
Research Areas
Products Related to PROTAC(285)
- GC80934PROTAC BRD4 Degrader-49CAS: 3115940-40-1Purity: >98%
BRD4 degrader-8 is a BRD4 -targeting degrader.
- GC80936PROTAC BLIMP-1 degrader-1Purity: >98.00%
PROTAC BLIMP-1 degrader-1 is an orally active BLIMP-1 PROTAC degrader with an EC 50 of 13.1 nM.
- GC80937PROTAC KAT6 Degrader-1Purity: >98%
PROTAC KAT6 Degrader-1 is a CRBN-dependented KAT6 PROTAC degrader.
- GC80943KT-474 hydrochlorideCAS: 2751703-31-6Purity: >98.00%
KT-474 (KYM-001; PROTAC IRAK4 degrader-7) hydrochloride is an orally active PROTAC IRAK4 degrader with anti-tumor effects.
- GC80944PROTAC BCL6 Degrader-3CAS: 3005272-58-9Purity: >99.50%
PROTAC BCL6 Degrader-3 (compound 92) is a BCL6 PROTAC degrader.
- GC80945APH02174 hemiformicPurity: >98.00%
APH02174 hemiformic is a highly selective and orally active IRAK4 PROTAC degrader with the DC 50 of 4.01 nM in THP-1 cells.
- GC80946PROTAC JAK1/2 degrader-1Purity: >99.00%
PROTAC JAK1/2 degrader-1 is an orally active JAK1 / JAK2 PROTAC degrader, with DC 50 values of 1.4 μM and 0.92 μM against JAK1 and JAK2, respectively.
- GC80949PROTAC STAT6 degrader-3CAS: 3077385-98-6Purity: >98.00%
PROTAC STAT6 degrader-3 is a potent STAT6 PROTAC degrader with a DC 50 of less than 1 nM.
- GC81024PROTAC RNF4 degrader-1Purity: >98.00%
PROTAC RNF4 degrader-1 is a RNF4 PROTAC degrader ( K d = 64.5 nM) that degrades RNF4 via the ubiquitin-proteasome system.
- GC81026PROTAC SKP2 Degrader-1CAS: 3120650-15-6Purity: >99.50%
PROTAC SKP2 Degrader-1 is a PROTAC degrader targeting SKP2, with a K d value of 6.28 μM.
- GC81027PROTAC HIF-1α degrader-2CAS: 3095636-64-6Purity: >98%
PROTAC HIF-1α degrader-2 is a highly efficient and selective PROTAC degrader targeting HIF-1α. PROTAC HIF-1α degrader-2 promotes HIF-1α degradation via the ubiquitin-proteasome pathway by facilitating the formation of a HIF-1α/VHL ternary complex.
- GC81036PROTAC AAK1 degrader-1CAS: 3113123-63-7Purity: >98.00%
PROTAC AAK1 degrader-1 (compound 14) is a selective PROTAC AAK1 degrader with a DC 50 of <10 nM.
- GC81038PROTAC mHTT Degrader-1CAS: 2919475-43-5Purity: >98%
PROTAC mHTT Degrader-1 is a blood-brain barrier-penetrant mutant huntingtin ( mHTT ) PROTAC degrader.
- GC81039PROTAC MALT1 Degrader-1CAS: 2975664-37-8Purity: >98.00%
PROTAC MALT1 Degrader-1 (Compound 176) is a MALT1 PROTAC degrader.
- GC81297DFCI-002-06CAS: 3092208-36-8Purity: >98%
DFCI-002-06 is an orally active dual-target HCK/BTK PROTAC degrader with DC₅₀ values for HCK and BTK of 1.3 and 4.5 nM respectively.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC80928 | NP1192 | 2966791-41-1 | >99.00% | |
NP1192 is a potent, selective PROTAC NAT10 degrader. | ||||
| GC80934 | PROTAC BRD4 Degrader-49 | 3115940-40-1 | >98% | |
BRD4 degrader-8 is a BRD4 -targeting degrader. | ||||
| GC80935 | JQ1-JX5 | - | >98% | |
JQ1-JX5 is a DCAF16-based BRD4 PROTAC degrader. | ||||
| GC80936 | PROTAC BLIMP-1 degrader-1 | - | >98.00% | |
PROTAC BLIMP-1 degrader-1 is an orally active BLIMP-1 PROTAC degrader with an EC 50 of 13.1 nM. | ||||
| GC80937 | PROTAC KAT6 Degrader-1 | - | >98% | |
PROTAC KAT6 Degrader-1 is a CRBN-dependented KAT6 PROTAC degrader. | ||||
| GC80938 | DOT1L808 | - | >98.00% | |
DOT1L808 is a potent and highly selective DOT1L PROTAC degrader with a DC 50 value of 5 nM. | ||||
| GC80939 | MS115 TFA | 3109377-61-6 | >98.00% | |
MS115 TFA is a selective PRMT5/MEP50 PROTAC degrader, with DC 50 values of 17.4 nM and 11.3 nM for PRMT5 and MEP50, respectively. | ||||
| GC80940 | dIRF4-2 | 3136609-62-3 | >99.00% | |
dIRF4-2 is a selective IRF4 PROTAC degrader with a DC 50 value of 2.2 μM. | ||||
| GC80941 | RJS308 TFA | - | >98.00% | |
RJS308 TFA is a selective Cyclophilin A ( CypA) PROTAC degrader. | ||||
| GC80943 | KT-474 hydrochloride | 2751703-31-6 | >98.00% | |
KT-474 (KYM-001; PROTAC IRAK4 degrader-7) hydrochloride is an orally active PROTAC IRAK4 degrader with anti-tumor effects. | ||||
| GC80944 | PROTAC BCL6 Degrader-3 | 3005272-58-9 | >99.50% | |
PROTAC BCL6 Degrader-3 (compound 92) is a BCL6 PROTAC degrader. | ||||
| GC80945 | APH02174 hemiformic | - | >98.00% | |
APH02174 hemiformic is a highly selective and orally active IRAK4 PROTAC degrader with the DC 50 of 4.01 nM in THP-1 cells. | ||||
| GC80946 | PROTAC JAK1/2 degrader-1 | - | >99.00% | |
PROTAC JAK1/2 degrader-1 is an orally active JAK1 / JAK2 PROTAC degrader, with DC 50 values of 1.4 μM and 0.92 μM against JAK1 and JAK2, respectively. | ||||
| GC80949 | PROTAC STAT6 degrader-3 | 3077385-98-6 | >98.00% | |
PROTAC STAT6 degrader-3 is a potent STAT6 PROTAC degrader with a DC 50 of less than 1 nM. | ||||
| GC81024 | PROTAC RNF4 degrader-1 | - | >98.00% | |
PROTAC RNF4 degrader-1 is a RNF4 PROTAC degrader ( K d = 64.5 nM) that degrades RNF4 via the ubiquitin-proteasome system. | ||||
| GC81025 | PSP-0119 | 3104855-98-0 | >98.50% | |
PSP-0119 is a highly efficient and effective PROTAC degrader targeting IRAK4 ( IC 50 = 2.83 nM). | ||||
| GC81026 | PROTAC SKP2 Degrader-1 | 3120650-15-6 | >99.50% | |
PROTAC SKP2 Degrader-1 is a PROTAC degrader targeting SKP2, with a K d value of 6.28 μM. | ||||
| GC81027 | PROTAC HIF-1α degrader-2 | 3095636-64-6 | >98% | |
PROTAC HIF-1α degrader-2 is a highly efficient and selective PROTAC degrader targeting HIF-1α. PROTAC HIF-1α degrader-2 promotes HIF-1α degradation via the ubiquitin-proteasome pathway by facilitating the formation of a HIF-1α/VHL ternary complex. | ||||
| GC81036 | PROTAC AAK1 degrader-1 | 3113123-63-7 | >98.00% | |
PROTAC AAK1 degrader-1 (compound 14) is a selective PROTAC AAK1 degrader with a DC 50 of <10 nM. | ||||
| GC81038 | PROTAC mHTT Degrader-1 | 2919475-43-5 | >98% | |
PROTAC mHTT Degrader-1 is a blood-brain barrier-penetrant mutant huntingtin ( mHTT ) PROTAC degrader. | ||||
| GC81039 | PROTAC MALT1 Degrader-1 | 2975664-37-8 | >98.00% | |
PROTAC MALT1 Degrader-1 (Compound 176) is a MALT1 PROTAC degrader. | ||||
| GC81041 | GP262 | 3107761-81-6 | >98.50% | |
GP262 is a PI3K/mTOR PROTAC degrader targeting PI3Kγ, PI3Kα and mTOR with DC 50 values of 42.23 nM, 227.4 nM and 45.4 nM, respectively in MDA-MB-231 cells. | ||||
| GC81296 | PRT3789 epimer | 3023568-80-8 | >98.50% | |
PRT3789 epimer is an epimer of PRT3789. | ||||
| GC81297 | DFCI-002-06 | 3092208-36-8 | >98% | |
DFCI-002-06 is an orally active dual-target HCK/BTK PROTAC degrader with DC₅₀ values for HCK and BTK of 1.3 and 4.5 nM respectively. | ||||