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Home >> Signaling Pathways >> PROTAC

PROTAC

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.

Targets for  PROTAC

Products for  PROTAC

  1. Cat.No. Product Name Information
  2. GC68352 (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine Chemical Structure
  3. GC60009 (S,R,S)-AHPC-PEG5-COOH

    VH032-PEG5-COOH; VHL Ligand-Linker Conjugates 16; E3 Ligase Ligand-Linker Conjugates 58

     (S,R,S)-AHPC-PEG5-COOH (VH032-PEG5-COOH) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 5-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-PEG5-COOH Chemical Structure
  4. GC50469 A 410099.1 amide-alkylC4-amine A 410099.1 amide-alkylC4-amine A 410099.1 amide-alkylC4-amine Chemical Structure
  5. GC50468 A 410099.1 amide-PEG2-amine A 410099.1 amide-PEG2-amine A 410099.1 amide-PEG2-amine Chemical Structure
  6. GC50467 A 410099.1 amide-PEG3-amine A 410099.1 amide-PEG3-amine A 410099.1 amide-PEG3-amine Chemical Structure
  7. GC50737 A 410099.1 amide-PEG4-amine A 410099.1 amide-PEG4-amine Chemical Structure
  8. GC50739 A 410099.1 amide-PEG5-amine A 410099.1 amide-PEG5-amine Chemical Structure
  9. GC33280 A1874 A1874 is a nutlin-based (MDM2 ligand) and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation. A1874 Chemical Structure
  10. GC35227 ACBI1 ACBI1 is a potent and cooperative SMARCA2, SMARCA4 and PBRM1 degrader with DC50s of 6, 11 and 32 nM, respectively. ACBI1 is a PROTAC degrader. ACBI1 shows anti-proliferative activity. ACBI1 induces apoptosis. ACBI1 Chemical Structure
  11. GC91040 AP-1

    A PROTAC that drives ALK degradation

     AP-1 Chemical Structure
  12. GC50744 ARCC 4 negative control ARCC 4 negative control Chemical Structure
  13. GC60594 ARCC-4 ARCC-4 is a low-nanomolar Androgen Receptor (AR) degrader based on PROTAC, with a DC50 of 5?nM. ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy. ARCC-4 Chemical Structure
  14. GC63492 ARD-2128 ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer. ARD-2128 Chemical Structure
  15. GC63704 ARD-2585 ARD-2585 is an exceptionally potent and orally active PROTAC degrader of androgen receptor. ARD-2585 Chemical Structure
  16. GC68696 ARV-766

    ARV-766 is an orally effective protein degradation agent of protein hydrolysis targeted chimeras (PROTACs). ARV-766 degrades wild-type androgen receptor AR, as well as related AR LBD mutants, including the most common pathogenic AR L702H, H875Y and T878A mutations.

     ARV-766 Chemical Structure
  17. GC32685 ARV-771 ARV-771 is a potent BET PROTAC based on E3 ligase von Hippel-Lindau with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively. ARV-771 Chemical Structure
  18. GC19038 ARV-825 ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 Chemical Structure
  19. GC33354 AT6 AT6 is a PROTAC AT1 analogue, which is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 with highly selectivity to bromodomain (Brd4). AT6 Chemical Structure
  20. GC50630 aTAG 2139 Degrader of MTH1 fusion proteins for use within the aTAG system aTAG 2139 Chemical Structure
  21. GC50631 aTAG 4531 Degrader of MTH1 fusion proteins for use within the aTAG system aTAG 4531 Chemical Structure
  22. GC65506 BETd-246 BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and BET, exhibiting superior selectivity, potency and antitumor activity. BETd-246 Chemical Structure
  23. GC32791 BETd-260 (ZBC 260)

    ZBC 260

     BETd-260 (ZBC 260) (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line. BETd-260 (ZBC 260) potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells. BETd-260 (ZBC 260) Chemical Structure
  24. GC65457 BI-3663 BI-3663 is a highly selective PTK2/FAK PROTAC (DC50=30 nM), with Cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC50 of 18 nM. BI-3663 is a PROTAC that composes of BI-4464 linked to Pomalidomide with a linker. Anti-cancer activity. BI-3663 Chemical Structure
  25. GC33017 BRD4 degrader AT1 BRD4 degrader AT1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 as a highly selective Brd4 degrader, with a Kd of 44 nM for Brd4BD2 in cells. BRD4 degrader AT1 Chemical Structure
  26. GC65128 BSJ-03-123 BSJ-03-123 is a PROTAC connected by ligands for Cereblon and CDK as a potent and novel CDK6-selective small-molecule degrader. BSJ-03-123 Chemical Structure
  27. GC50615 BSJ-03-204 Selective Cdk4/6 degrader BSJ-03-204 Chemical Structure
  28. GC50614 BSJ-04-132 Selective Cdk4 degrader BSJ-04-132 Chemical Structure
  29. GC50610 BSJ-Bump Negative control for BSJ-03-123 BSJ-Bump Chemical Structure
  30. GC67861 CCT367766 formic CCT367766 formic Chemical Structure
  31. GC35635 CDK9 Antagonist-1 CDK9 Antagonist-1 Chemical Structure
  32. GC50363 cis MZ 1 Negative Control for MZ 1 cis MZ 1 Chemical Structure
  33. GC50629 cis VH 032, amine dihydrochloride Negative control for VH 032, amine cis VH 032, amine dihydrochloride Chemical Structure
  34. GC50616 cis-VZ 185 Negative control for VZ 185 cis-VZ 185 Chemical Structure
  35. GC35739 CP-10 CP-10 is a PROTAC connected by ligands for Cereblon and CDK, with highly selective, specific, and remarkable CDK6 degradation (DC50=2.1 nM). It inhibits proliferation of several haematopoietic cancer cells with impressive potency including multiple myeloma, and can still degrades mutated and overexpressed CDK6. CP-10 Chemical Structure
  36. GC50619 CRBN-6-5-5-VHL Potent and selective cereblon degrader; cell-permeable CRBN-6-5-5-VHL Chemical Structure
  37. GC66361 DB-0646 DB-0646, a PROTAC, is a multi-kinase degrader. DB-0646 Chemical Structure
  38. GC68942 DB1113

    DB1113 (Example 24) is a bifunctional compound that targets protein kinase degradation. DB1113 can degrade ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1 , MAP4K2，MAP4K3，MAP4K5，MAPK14，MAPK7，MAP K8，MAP K9，MAP KAP K2，MAP KAP K3，NL K ，PDI K1L ，PT K2B ，RIP K1 ，RPS6KA1 ，RPS6KA3 ，SIk2、SIk3、ST k35、TN k2 and UL k1. DB1113 can be used to study diseases or disorders mediated by abnormal kinase activity.

     DB1113 Chemical Structure
  39. GC19119 dBET1 dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM. dBET1 Chemical Structure
  40. GC63445 dBET23 dBET23 is a highly effective and selective PROTAC BRD4 degrader with a DC50/5h of ~ 50 nM for BRD4BD1 protein. dBET23 Chemical Structure
  41. GC35815 dBET57 dBET57 is a potent and selective degrader of BRD4BD1 based on the PROTAC technology. dBET57 mediates recruitment to the CRL4Cereblon E3 ubiquitin ligase, with a DC50/5h of 500 nM for BRD4BD1, and is inactive on BRD4BD2. dBET57 Chemical Structure
  42. GC32719 dBET6

    dBET6 is a highly potent, selective and cell-permeable PROTAC connected by ligands for Cereblon and BET, with an IC50 of 14 nM, and has antitumor activity.

     dBET6 Chemical Structure
  43. GC50518 dBRD9 Potent and selective BRD9 degrading PROTAC dBRD9 Chemical Structure
  44. GC50736 dBRD9-A dBRD9-A Chemical Structure
  45. GC50749 DD 03-171 DD 03-171 Chemical Structure
  46. GC35882 dMCL1-2 dMCL1-2 is a potent and selective PROTAC of myeloid cell leukemia 1 (MCL1) (Bcl-2 family member) based on Cereblon, which binds to MCL1 with a KD of 30 nM. dMCL1-2 activats the cellular apoptosis machinery by degradation of MCL1. dMCL1-2 Chemical Structure
  47. GC69004 Dovitinib-RIBOTAC

    Dovitinib RIBOTAC is a targeted RNA degrading agent that can efficiently and selectively cleave pre-miR-21.

     Dovitinib-RIBOTAC Chemical Structure
  48. GC69005 Dovitinib-RIBOTAC TFA

    Dovitinib RIBOTAC TFA is a targeted RNA degrading agent that can efficiently and selectively cleave precursor miR-21.

     Dovitinib-RIBOTAC TFA Chemical Structure
  49. GC62942 DP-C-4 DP-C-4 is a Cereblon-based dual PROTAC for simultaneous degradation of EGFR and PARP. DP-C-4 Chemical Structure
  50. GC50754 dTAG-13-NEG dTAG-13-NEG Chemical Structure
  51. GC69027 dTAG-47

    dTAG-47 is a bifunctional dTAG molecule that targets the mutant form of FKBP12 (FKBP12F36V). FKBP12F36V can be used as a degradation tag (dTAG) and fused with target proteins. dTAG-47 can be used for research on basal-like breast cancer (BBC).

     dTAG-47 Chemical Structure
  52. GC50757 dTAGV-1 hydrochloride dTAGV-1 hydrochloride Chemical Structure
  53. GC50756 dTAGV-1 TFA dTAGV-1 TFA Chemical Structure
  54. GC50755 dTAGV-1-NEG dTAGV-1-NEG is a diastereomer and as a heterobifunctional negative control of dTAGV-1. dTAGV-1 is an FKBP12F36V-selective degrader. dTAGV-1-NEG Chemical Structure
  55. GC35904 dTRIM24 dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC, consists of ligands for von Hippel-Lindau and TRIM24. dTRIM24 Chemical Structure
  56. GC32902 E3 ligase Ligand-Linker Conjugates 10

    VH032-PEG2-C4-Cl; VHL Ligand-Linker Conjugates 7; E3 ligase Ligand-Linker Conjugates 10

     E3 ligase Ligand-Linker Conjugates 10 (VH032-PEG2-C4-Cl) is a conjugate of ligands for E3 and 13-atom-length linker. The connector of linker is Halogen group. E3 ligase Ligand-Linker Conjugates 10 incorporates the (S,R,S)-AHPC based VHL ligand and an alkyl/ether-based linker. E3 ligase Ligand-Linker Conjugates 10 is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays. E3 ligase Ligand-Linker Conjugates 10 Chemical Structure
  57. GC32987 E3 ligase Ligand-Linker Conjugates 8

    VH032-C6-PEG3-C4-Cl; VHL Ligand-Linker Conjugates 12; E3 ligase Ligand-Linker Conjugates 8

     E3 ligase Ligand-Linker Conjugates 8 (VH032-C6-PEG3-C4-Cl) is a conjugate of ligands for E3 and 20-atom-length linker. The connector of linker is Halogen group. E3 ligase Ligand-Linker Conjugates 8 incorporates the (S,R,S)-AHPC based VHL ligand and an alkyl/ether-based linker. E3 ligase Ligand-Linker Conjugates 8 is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays. E3 ligase Ligand-Linker Conjugates 8 Chemical Structure
  58. GC32976 E3 ligase Ligand-Linker Conjugates 9

    VH032-PEG6-C4-Cl; VHL Ligand-Linker Conjugates 10; E3 ligase Ligand-Linker Conjugates 9

     E3 ligase Ligand-Linker Conjugates 9 is a conjugate of ligands for E3 and 25-atom-length linker. The connector of linker is Halogen group. E3 ligase Ligand-Linker Conjugates 9 incorporates the (S,R,S)-AHPC based VHL ligand and 6-unit PEG linker. E3 ligase Ligand-Linker Conjugates 9 is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays. E3 ligase Ligand-Linker Conjugates 9 Chemical Structure
  59. GC36001 ERD-308 ERD-308 is a highly potent von Hippel-Lindau-based PROTAC degrader of estrogen receptor (ER) for ER positive breast cancer treatment. ERD-308 induces >95% of ER degradation at concentrations as low as 5 nM in both cell lines (DC50 (concentration causing 50% of protein degradation) of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells, respectively). ERD-308 Chemical Structure
  60. GC91060 Ferritin PROTAC DeFer-2

    A PROTAC that drives ferritin degradation

     Ferritin PROTAC DeFer-2 Chemical Structure
  61. GC39264 FKBP12 PROTAC dTAG-13

    dTAG-13

     FKBP12 PROTAC dTAG-13 (dTAG-13), a PROTAC-based heterobifunctional degrader, is a selective degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 effectively engages FKBP12F36V and CRBN, thereby selectively degrading FKBP12F36V. FKBP12 PROTAC dTAG-13 Chemical Structure
  62. GC39289 FKBP12 PROTAC dTAG-7

    dTAG-7

     FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional degrader. FKBP12 PROTAC dTAG-7 (dTAG-7) is a degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-7 (dTAG-7) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN. FKBP12 PROTAC dTAG-7 Chemical Structure
  63. GC19509 Gefitinib-based PROTAC 3

    Gefitinib-based Proteolysis-targeting Chimera 3

     A VHL-recruiting PROTAC Gefitinib-based PROTAC 3 Chemical Structure
  64. GC36167 GMB-475 GMB-475 is a degrader of BCR-ABL1 tyrosine kinase based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein. GMB-475 Chemical Structure
  65. GC32831 HaloPROTAC 2

    HaloPROTAC 2

     HaloPROTAC 2 (HaloPROTAC 2) is a conjugate of ligands for E3 and 21-atom-length linker. The connector of linker is Halogen group. HaloPROTAC 2 incorporates the VH032 based VHL ligand and 5-unit PEG linker. HaloPROTAC 2 is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays. HaloPROTAC 2 Chemical Structure
  66. GC40877 Heclin Heclin is an inhibitor of HECT E3 ubiquitin ligases (IC50s = 6.8, 6.3, and 6.9 μM for Smurf2, Nedd4, and WWP1 HECT ligase domains, respectively). Heclin Chemical Structure
  67. GC33391 Homo-PROTAC cereblon degrader 1 Homo-PROTAC cereblon degrader 1 (compound 15a) is a highly potent and efficient Cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3. Homo-PROTAC cereblon degrader 1 Chemical Structure
  68. GC65285 Homo-PROTAC pVHL30 degrader 1 Homo-PROTAC pVHL30 degrader 1 is a potent pVHL30 degrader based on PROTAC, consists of two ligands of von Hippel-Lindau. Homo-PROTAC pVHL30 degrader 1 Chemical Structure
  69. GC65559 INY-03-041 INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor GDC-0068 conjugated to Lenalidomide (Cereblon ligand). INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0 nM, 6.8 nM and 3.5 nM, respectively. INY-03-041 Chemical Structure
  70. GC67757 INY-03-041 trihydrochloride INY-03-041 trihydrochloride Chemical Structure
  71. GC63707 JB170 JB170 is a potent and highly specific PROTAC-mediated AURORA-A (Aurora Kinase) degrader (DC50=28 nM) by linking Alisertib, to the Cereblon-binding molecule Thalidomide. JB170 preferentially binds AURORA-A (EC50=193 nM) over AURORA-B (EC50=1.4 ?M). JB170-mediated S-phase arrest is caused specifically by AURORA-A depletion. JB170 has excellent ability to inhibit non-catalytic function of AURORA-A kinase. JB170 Chemical Structure
  72. GC65471 JH-XI-10-02 JH-XI-10-02 is a PROTAC connected by ligands for Cereblon and CDK. JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader, with an IC50 of 159 nM. JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19. JH-XI-10-02 Chemical Structure
  73. GC69320 JQAD1

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

     JQAD1 Chemical Structure
  74. GC61766 LC-2 LC-2 is a potent and first-in-class von Hippel-Lindau-based PROTAC capable of degrading endogenous KRAS G12C, with DC50s between 0.25 and 0.76 μM. LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines. LC-2 Chemical Structure
  75. GC50669 Lenalidomide 4'-PEG1-amine Lenalidomide 4'-PEG1-amine Chemical Structure
  76. GC50684 Lenalidomide 4'-PEG2-amine Lenalidomide 4'-PEG2-amine Chemical Structure
  77. GC50694 Lenalidomide 4'-PEG3-amine Lenalidomide 4'-PEG3-amine Chemical Structure
  78. GC38812 MD-224 MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 consists of ligands for Cereblon and MDM2. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent. MD-224 Chemical Structure
  79. GC64651 MI-389 MI-389 is a PROTAC translation termination factor GSPT1 degrader. MI-389 disrupts a target that is a shared dependency in different AML and ALL cell lines, and that MI-389 action is dependent on the CRL4CRBN E3 ligase. MI-389 Chemical Structure
  80. GC69501 MS159

    MS159 is an effective nuclear receptor binding SET domain protein 2 (NSD2) PROTAC degrader. MS159 can inhibit the growth of tumor cells. MS159 is an effective chemical tool for exploring the role of NSD2 in health and disease.

     MS159 Chemical Structure
  81. GC65466 MS170 MS170 is a potent and selective PROTAC AKT degrader. MS170 depletes cellular total AKT (T-AKT) with the DC50 value of 32 nM. MS170 binds to AKT1, AKT2, and AKT3 with Kds of 1.3 nM, 77 nM, and 6.5 nM, respectively. MS170 Chemical Structure
  82. GC67710 MS177 MS177 Chemical Structure
  83. GC39407 MS1943 MS1943 is a first-in-class, orally bioavailable EZH2 selective degrader, with an IC50 of 120 nM. MS1943 significantly reduces EZH2 protein levels in numerous triple-negative breast cancer (TNBC) and other cancer and noncancerous cell lines. MS1943 effectively blocks proliferation of multiple TNBC and other cancer cell lines. MS1943 Chemical Structure
  84. GC69502 MS21

    MS21 is a novel AKT degrader that selectively inhibits the growth of mutant cancers through the PI3K/PTEN pathway.

     MS21 Chemical Structure
  85. GC65243 MS4077 MS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 37?nM for binding affinity to ALK. MS4077 Chemical Structure
  86. GC64966 MS4078 MS4078 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 19?nM for binding affinity to ALK. MS4078 Chemical Structure
  87. GC65052 MS4322 MS4322 (YS43-22) is a first-in-class PRMT5 degrader and a valuable chemical tool (PROTAC) for exploring the PRMT5 functions in health and disease. MS4322 Chemical Structure
  88. GC65876 MS4322 (isomer)

    YS43-22 (isomer)

     MS4322 (YS43-22) isomer is an isomer of MS4322. MS4322 is a potent and selective PRMT5 (protein arginine methyltransferase 5) degrader, and inhibits growth of multiple cancer cell lines. MS4322 (isomer) Chemical Structure
  89. GC69505 MS9427

    MS9427 is an effective PROTAC EGFR degrader, with Kd values of 7.1 nM and 4.3 nM for wild-type EGFR and mutant EGFR L858R, respectively. MS9427 selectively degrades mutant variants through the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathway, but does not degrade WT EGFR. MS9427 has a strong inhibitory effect on NSCLC cell proliferation and can be used in cancer research.

     MS9427 Chemical Structure
  90. GC69506 MS9427 TFA

    MS9427 TFA is an effective PROTAC EGFR degrader, with Kd values of 7.1 nM and 4.3 nM for wild-type EGFR and mutant EGFR L858R, respectively. MS9427 TFA selectively degrades mutant variants through the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathway, but not WT EGFR. MS9427 TFA strongly inhibits NSCLC cell proliferation and can be used in cancer research.

     MS9427 TFA Chemical Structure
  91. GC36661 MT-802 MT-802 is a potent BTK degrader based on Cereblon ligand, with a DC50 of 1 nM. MT-802 Chemical Structure
  92. GC69744 MTX-23

    PROTAC AR-V7 degrader-2

    MTX-23 is an AR-based PROTAC. MTX-23 inhibits CaP cell proliferation by degrading AR-V7 and AR-FL. MTX-23 induces apoptosis in cells.

     MTX-23 Chemical Structure
  93. GC18729 MZ1 MZ1 is a hybrid compound that drives the selective proteasomal degradation of bromodomain-containing protein 4 (BRD4). MZ1 Chemical Structure
  94. GC33102 MZP-54 MZP-54 is a PROTAC connected by ligands for von Hippel-Lindau and BRD3/4, with a Kd of 4 nM for Brd4BD2. MZP-54 Chemical Structure
  95. GC33363 MZP-55 MZP-55 is a PROTAC connected by ligands for von Hippel-Lindau and BRD3/4, with a Kd of 8 nM for Brd4BD2. MZP-55 Chemical Structure
  96. GC67889 NJH-2-056 NJH-2-056 Chemical Structure
  97. GC50740 NR 7h NR 7h Chemical Structure
  98. GC50665 Pomalidomide 4'-alkylC3-acid Pomalidomide 4'-alkylC3-acid Chemical Structure
  99. GC50658 Pomalidomide 4'-alkylC3-amine Pomalidomide 4'-alkylC3-amine is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology. Pomalidomide 4'-alkylC3-amine Chemical Structure
  100. GC50674 Pomalidomide 4'-alkylC4-acid Pomalidomide 4'-alkylC4-acid Chemical Structure
  101. GC50546 Pomalidomide 4'-alkylC5-acid Cereblon ligand with alkyl linker and terminal acid for onward chemistry Pomalidomide 4'-alkylC5-acid Chemical Structure

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