protac cdk9 degrader 2

PROTAC CDK9/CycT1 Degrader-2 inhibits CDK9 with an IC50 of 45 nM [1].

PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC[1].

(Arg)9 TFA (Peptide R9 TFA) is a cell-penetrating peptide. (Arg)9 TFA (Nona-L-arginine TFA) exhibits neuroprotective activity with an IC50 of 0.78 μM in the glutamic acid model.

2-Aminopurine-9-beta-D-(2’-deoxy)riboside is a derivative of 2-Aminopurine.

VEGFR-2-IN-9 (KDR-in-4) is a potent KDR/VEGFR2 inhibitor (IC50: 7 nM). It can be used to study breast cancer.

Angiotensin 1/2 (1-9)TFA is containing the amino acids 1-9 that are converted from Angiotensin I/II peptide.

CDK9-IN-2 is a special CDK9 inhibitor and has an IC50 of 5 nM and 7 nM in A2058 skin cell line (72 hours) and H929 multiple myeloma cell line (72 hours), respectively.

TLR7/8/9 antagonist 2 is an orally active and highly bioavailable vTLR7/8/9 antagonist. TLR7/8/9 antagonist 2 inhibits HEK/hTLR7, HEK/hTLR8 and HEK/hTLR9 with IC50s of 0.011 μM, 0.029 μM and 0,052 μM, respectively. TLR7/8/9 antagonist 2 can be used to study auto-inflammatory diseases such as systemic lupus erythematosus or lupus nephritis.

Bradykinin (2-9) (Des-Arg1-bradykinin) is an amino-truncated peptide compound that is a metabolite of Bradykinin. It is formed by the cleavage action of Aminopeptidase P.

PROTAC SOS1 degrader-1, a potent compound, demonstrates an effective degradation of PROTAC SOS1 with a DC50 value of 98.4 nM. It exhibits antiproliferative activity against cancer cells harboring diverse KRAS mutations and has shown an antitumor effect with low toxicity [1].

PROTAC EGFR degrader 6 is a potent PROTAC EGFR degrader that effectively reduces EGFR Del19 levels in HCC827 cells, exhibiting a DC50 of 45.2 nM. It notably promotes apoptosis and induces G1 phase arrest in HCC827 cells [1].

PROTAC BRD4 Degrader-1 is an efficacious degrader of BRD4(BRD4 BD1,IC50 of 41.8 nM).

PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 degrader of internal tandem duplication (ITD)(IC50 0.6 nM),with anti-proliferative activity.

PROTAC CBP/P300 Degrader-1 is an effective compound that degrades CBP/P300 in a potent manner. It significantly reduces cell viability in various cancer cell lines.

PROTAC BET Degrader-1 is a potent degrader of BET based on PROTAC.

PROTAC EGFR degrader 8 (T-184) is a PROTAC that selectively degrades the epidermal growth factor receptor (EGFR) with a DC50 of 15.56 nM in HCC827 cells. It effectively inhibits the growth of various cell lines, including H1975, PC-9, and HCC827, with IC50 values of 7.72 nM, 121.9 nM, and 14.21 nM, respectively. This compound is primarily used for cancer research, particularly in the context of non-small cell lung cancer (NSCLC) [1].

PROTAC EED degrader-2 is a PROTAC targeting EED (pKD of 9.27),is a inhibitor of polycomb repressive complex 2 (PRC2) with pIC50 of 8.11.

PROTAC EGFR degrader 4 is a potent molecule designed to target and degrade mutant EGFR, showcasing its effectiveness by inducing degradation of EGFR del19 and EGFR L858R/T790M with DC50 values of 0.51 nM and 126 nM, respectively. Furthermore, it significantly inhibits the growth of HCC827 and H1975 cell lines, demonstrating IC50 values of 0.83 nM and 203.1 nM, respectively. The induced degradation of EGFR by this compound is associated with autophagy [1].

1,2,3,10-Tetramethoxy-9-(2-hydroxy-4,5-dimethoxybenzyloxy)oxoaporphine is a natural product of Hernandia, Hernandiaceae. The catalog number is TN2479 and the CAS number is 872729-33-4. 1,2,3,10-Tetramethoxy-9-(2-hydroxy-4,5-dimethoxybenzyloxy)oxoaporphine can be used as a reference standard.

PROTAC GDI2 Degrader-1 (Compound 21) is a potent degrader of PROTAC GDI2, demonstrating outstanding antitumor activity in vivo within pancreatic xenograft models that overexpress GDI2 [1].

PROTAC NSD3 degrader-1 (compound 56) is a targeted degradation agent for the Nuclear receptor binding SET domain protein NSD3. It effectively induces the degradation of NSD3 in NCI-H1703 and A549 lung cancer cell lines, with DC50 values of 1.43 and 0.94 μM, respectively. Additionally, it hinders H3K36 methylation, triggers apoptosis, and arrests the cell cycle. Furthermore, PROTAC NSD3 degrader-1 diminishes the expression of NSD3-related genes, including CDC25A, ALDH1A1, and IGFBP.

CDK ligand for PROTAC hydrochloride is a CDK inhibitor with antitumor activity. It has been used to design PROTAC CDK4/6 degraders.

PROTAC BRD9 Degrader-7 is a selective and orally active BRD9 degrader with a DC50 of 1.02 nM and demonstrates superior pharmacokinetics, evidenced by a Cmax of 3436.95 ng/mL [1].

STAT3 Degrader-2 is a PROTAC-based compound that effectively reduces the total STAT3 protein levels, and is utilized in the research of cancer and various diseases [1].

PROTAC EGFR Degrader 3, a highly potent molecule, exhibits remarkable cellular activity against H1975 and HCC827 cells, maintaining high selectivity. It additionally reveals the lysosome's crucial role in the degradation mechanism of mutant EGFR [1].

PROTAC BRD9 Degrader-5 is a proteolysis targeting chimera (PROTAC) designed for the specific degradation of Bromodomain-containing protein 9 (BRD9).

Androgen Receptor Degrader-2 (Compound 9) is a potent degrader of androgen receptors, with potential application in cancer research [1].

PROTAC KRAS G12C degrader-1, a cereblon-based degrader, promotes CRBN/KRAS G12C dimerization and facilitates the degradation of GFP-KRAS G12C in reporter cells [1].

PROTAC SMARCA2 degrader-2, a selective and powerful degrader of SMARCA2/4, exhibits an IC50 of <0.1 μΜ in the HeLa HiBiT assay.this compound holds promise for research into cancers related to or deficient in SMARCA4 [1].

PROTAC PARP1 degrader is a degrader of PARP1 based on the PROTAC technology. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line (IC50 of 6.12 μM).

Angiotensin 1/2 (1-9) is containing the amino acids 1-9 that are converted from Angiotensin I/II peptide.

PROTAC EGFR degrader 2 is a potent compound with exceptional antiproliferative activity, evidenced by its IC50 of 4.0 nM, and exhibits strong EGFR degradation activity with a DC50 of 36.51 nM. It is suitable for synthesizing nitroreductase (NTR)-responsive PROTACs [1].

PROTAC PTPN2 Degrader-1 (compound example 77) is a potent entity capable of degrading PTPN2, showing promise for research applications in cancer or metabolic diseases [1].

PROTAC STAT3 degrader-2 is a selective and efficacious PROTAC degrader of STAT3 protein with a DC 50 of 3.54 μM in Molm-16 Cell. PROTAC STAT3 degrader-2 has the potential for cancer research [1] .

PROTAC TTK degrader-1, a potent threonine tyrosine kinase (TTK) PROTAC degrader, demonstrates DC50 values of 1.7 nM in COLO-205 cells and 5.8 nM in HCT-116 cells, indicating effective target degradation. Furthermore, it shows anticancer efficacy in a xenograft mouse model with COLO-205 human colorectal cancer cells [1].

PROTAC BTK Degrader-1, a powerful, selective, and orally bioavailable degrader of PROTAC BTK, demonstrates effective reduction in BTK protein levels and tumor suppression. It exhibits IC50 values of 34.51 nM for BTK WT and 64.56 nM for BTK-481S, highlighting its potency and efficacy in targeting and diminishing BTK protein abundance [1].

PROTAC K-Ras Degrader-1 is potent degrader of K-Ras based PROTAC.

GSPT1 degrader-2 is a potent degrader of GSPT1 [1].

PROTAC AR-V7 degrader-1 (Compound 6) is an orally bioavailable, potent, and selective degrader targeting the androgen receptor (AR) variant V7, achieving degradation with a DC50 of 0.32 µM by directing the VHL E3 ligase to the AR DNA-binding domain (DBD). It demonstrates efficacy in the 22Rv1 cell line expressing AR-V7, with an EC50 of 0.88 µM [1].

PROTAC BRD4 Degrader-22 (Compd 44h) is a PROTAC-based degrader targeting BRD4, exhibiting a pDC50 of 9.2 in MOLT4 cells over 24 hours [1].

PROTAC BTK Degrader-3 is a potent degrader of Bruton's tyrosine kinase (BTK), exhibiting a DC50 (median degradation concentration) of 10.9 nM in Mino cells. This compound shows promise for research into B-cell malignancies, such as chronic lymphoid malignancies [1].

PROTAC BRD9 Degrader-1 is a lead PROTAC BRD9 chemical degrader with IC50 of 13.5 nM.

PROTAC MLKL Degrader-1 (Compound 36) is a selective PROTAC degrader targeting MLKL, achieving a degradation maximum (D max) over 90%. The compound encompasses modified cereblon (CRBN) ligands and a lenalidomide-linker as part of its structure. It effectively inhibits cell death in a TSZ-induced model of necroptosis.

PROTAC EZH2 Degrader-1 (Compound 150d), a potent inhibitor, effectively suppresses EZH2 methyltransferase activity, demonstrating an IC50 of 2.7 nM. EZH2 is crucial in various tumorigenesis and development processes [1].

PROTAC EGFR degrader 7 (compound 13b) is a potent, selective, CRBN-recruiting EGFRL858R/T790M degrader with a DC50 of 13.2 nM. It effectively inhibits proliferation of NCI-H1975 cells with an IC50 of 46.82 nM, induces apoptosis, and causes a G2/M phase arrest in these cells. Demonstrating antitumor activity, this compound is applicable in non-small cell lung cancer (NSCLC) research.

PROTAC RIPK degrader-6 (example 1) is a PROTAC designed for the targeted degradation of RIP Kinase, featuring a RIP2 kinase inhibitor connected through a linker to a cereblon binder[1].

PROTAC TTK Degrader-2 is a potent threonine tyrosine kinase (TTK) PROTAC degrader, achieving DC50 values of 3.1 nM in COLO-205 cells and 12.4 nM in HCT-116 cells. It demonstrates effective target degradation and anticancer activity in a COLO-205 human colorectal cancer cell xenograft mouse model [1].

PROTAC BRD9 Degrader-3 is a bifunctional degrader targeting BRD9, utilized in cancer research.

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

PROTAC EGFR degrader 7 (compound 13b) is a potent, selective CRBN-recruiting agent targeting EGFR L858R/T790M mutations with a DC50 of 13.2 nM. It effectively inhibits proliferation in NCI–H1975 cells with an IC50 of 46.82 nM and significantly triggers apoptosis and G2/M phase arrest in these cells. Demonstrating antitumor efficacy, PROTAC EGFR degrader 7 holds promise for non-small cell lung cancer (NSCLC) research [1].