PROTAC
Read More about this categoryShow Less
The PROTAC molecule itself contains three distinct portions: a ligand for binding to the target protein, a ligand for binding to an E3 ligase, and a linker joining these two ligands.
PROTACs (proteolysis-targeting chimaeras) are bifunctional molecules that bring a target protein into spatial proximity with an E3 ubiquitin ligase to trigger target ubiquitination and subsequent proteasomal degradation. Effective redirection of ligase poly-ubiquitination activity toward a new substrate protein requires formation of a ligase:PROTAC:target ternary complex, an intermediate species that is crucial to the cellular activity of degrader molecules. A characteristic feature of PROTACs mode of action is their sub-stoichiometric catalytic activity that alleviates the requirement for target engagement and occupancy of traditional inhibitors. New PROTAC molecules designed guided by the crystal structure show exquisite selectivity for inducing cellular depletion of Brd4 over its BET family members Brd2 and Brd3.
Products Related to PROTAC(273)
- GC73223PROTAC GPX4 degrader-1CAS: 2916433-81-1Purity: >99.00%
PROTAC GPX4 degrader-1 (DC-2) is a PROTAC-based GPX4 degrader, with a DC50 of 0.03 μM in HT1080 cells.
- GC73377SIAIS100 TFAPurity: >99.00%
SIAIS100 TFA is a potent BCR-ABL PROTAC degrader with an DC50 value of 2.7 nM.
- GC73385HDAC6 degrader-3CAS: 2785404-83-1Purity: >98.00%
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.
- GC73389Nampt degrader-2CAS: 3035008-40-0Purity: >99.00%
Nampt degrader-2 is a fluorescent PROTAC, which efficiently degrades NAMPT with an IC50 of 41.9 nM.
- GC73444PROTAC BCR-ABL Degrader-1Purity: >98.00%
PROTAC BCR-ABL Degrader-1 (compound PROTAC 1) is a PROTAC with a 2-oxoetl linker.
- GC73448PROTAC BRD4 Degrader-19CAS: 2684292-71-3Purity: >98.00%
PROTAC BRD4 Degrader-19 (compound 176) is a PROTAC that targets BRD4 protein for degradation.
- GC73466PROTAC BRD9 Degrader-6CAS: 2676211-62-2Purity: >98.00%
PROTAC BRD9 Degrader-6 is a potent degrader of BRD9 (IC50=0.13 nM), can be used for research of BAF complex-related disorders.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC73159 | KTX-582 | 2573298-13-0 | >98.00% | |
KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM and 5 nM for IRAK4 and Ikaros, respectively. | ||||
| GC73161 | KTX-951 | 2573298-36-7 | >98.00% | |
KTX-951 is a PROTAC targeting IRAK4 degradation (DC50=18 nM). | ||||
| GC73166 | U7D-1 | - | >99.00% | |
U7D-1 is a first-in-class potent and selective USP7 (ubiquitin-specific protease 7) PROTAC degrader, with a DC50 of 33 nM in RS4;11 cells. | ||||
| GC73203 | AK-2292 | 2984506-77-4 | >99.00% | |
AK-2292 is a potent and selective STAT5 PROTAC degrader, with a DC50 of 0.10 μM. | ||||
| GC73223 | PROTAC GPX4 degrader-1 | 2916433-81-1 | >99.00% | |
PROTAC GPX4 degrader-1 (DC-2) is a PROTAC-based GPX4 degrader, with a DC50 of 0.03 μM in HT1080 cells. | ||||
| GC73230 | SP27 | 3034805-75-6 | >99.00% | |
SP27 is a PROTAC that can selective degrades PLK4, with a DC50 of 19.5 nM. | ||||
| GC73236 | AD4 | 2918262-09-4 | >98.00% | |
AD4 is an artemisinin derivative that is a proteolytic targeting chimera (PROTAC) targeting PCLAF. | ||||
| GC73276 | LC-MB12 | 2828438-38-4 | >99.00% | |
LC-MB12 is an orally active PROTAC compound targets FGFR2 degradation with a DC50 of 11.8 nM. | ||||
| GC73277 | ARD-2051 | 2632305-17-8 | >98.00% | |
ARD-2051 is a potent and orally active androgen receptor (AR) proteolysis-targeting chimera degrader. | ||||
| GC73299 | MDEG-541 | - | >98.00% | |
MDEG-541 is a potent MYC-MAX degrader. | ||||
| GC73306 | XF067-68 | 2407452-79-1 | >99.00% | |
XF067-68 is a PROTAC for targeted degradation of WD40 repeat domain protein 5 (WDR5) (extracted from patent WO2019246570A1). | ||||
| GC73356 | dBRD4-BD1 | 2839318-19-1 | >98.00% | |
dBRD4-BD1 is a selective and durable BRD4 degrader with an DC50 value of 280 nM (Dmax=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1. | ||||
| GC73358 | MS15 TFA | - | >99.00% | |
MS15 TFA is a potent and selective AKT PROTAC degrader. | ||||
| GC73359 | ACBI2 | 2913161-19-8 | >99.00% | |
ACBI2 is a highly potent and orally active VHL PROTAC SMARCA2 degrader (EC50: 7 nM), which selectively degrades SMARCA2 with a DC50 value of 1 nM in RKO cells. | ||||
| GC73369 | SJ988497 | 2595365-41-4 | >98.00% | |
SJ988497 is a PROTAC JAK2 degrader. | ||||
| GC73374 | TD1092 | - | >99.00% | |
TD1092 is a pan-IAP degrader, degrades cIAP1, cIAP2, and XIAP. | ||||
| GC73377 | SIAIS100 TFA | - | >99.00% | |
SIAIS100 TFA is a potent BCR-ABL PROTAC degrader with an DC50 value of 2.7 nM. | ||||
| GC73385 | HDAC6 degrader-3 | 2785404-83-1 | >98.00% | |
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. | ||||
| GC73389 | Nampt degrader-2 | 3035008-40-0 | >99.00% | |
Nampt degrader-2 is a fluorescent PROTAC, which efficiently degrades NAMPT with an IC50 of 41.9 nM. | ||||
| GC73432 | CFT1946 | 2882165-79-7 | >99.00% | |
CFT1946 is an orally active, CRBN-based and mutant-selective bifunctional degradation activating compound (BiDAC™) degrader of BRAFV600E with a DC50 of 14 nM in A375 cells. | ||||
| GC73437 | YD23 | 2951015-29-3 | >98.00% | |
YD23 is a SMARCA2 PROTAC. | ||||
| GC73444 | PROTAC BCR-ABL Degrader-1 | - | >98.00% | |
PROTAC BCR-ABL Degrader-1 (compound PROTAC 1) is a PROTAC with a 2-oxoetl linker. | ||||
| GC73448 | PROTAC BRD4 Degrader-19 | 2684292-71-3 | >98.00% | |
PROTAC BRD4 Degrader-19 (compound 176) is a PROTAC that targets BRD4 protein for degradation. | ||||
| GC73466 | PROTAC BRD9 Degrader-6 | 2676211-62-2 | >98.00% | |
PROTAC BRD9 Degrader-6 is a potent degrader of BRD9 (IC50=0.13 nM), can be used for research of BAF complex-related disorders. | ||||