10-nle-neurokinin a

Neurokinin A (4-10), nle(10)- is a neurologically active peptide translated from the pre-protachykinin gene. Neurokinin A has many excitatory effects on mammalian nervous systems and on the mammalian inflammatory and pain responses.

Androgen receptor antagonist 1, an orally available full androgen receptor antagonist (IC50: 59 nM), is utilized in the synthesis of PROTAC AR degraders, achieving 24% and 47% AR protein degradation in LNCaP cells at concentrations of 1 μM and 10 μM, respectively.

CDK9-IN-10 is a potent inhibitor of CDK9 and serves as the ligand for the PROTAC CDK9 degrader-2.

QCA570 is an effective BET degrader based on PROTAC (IC50: 10 nM for BRD4 BD1 Protein).

Br-C10-methyl ester, a PROTAC linker characterized by its alkyl ether composition, plays a crucial role in the synthesis of a series of PROTACs (MS432). This compound incorporates a dual-ligand system connected via a linker; notably, one ligand interacts with the VHL portion.

MS 39 is a highly effective, highly affinity and selective depressant of mutant epidermal growth factor receptor (EGFR) with high efficiency, high affinity and selectivity. MS 39, conjured by gefitinib to VHL ligand via a linker, effectively induced the degradation of mutant EGFR (DC50 values in HCC827(exon 19 del) and H3255 (L858R mutation) lung cancer cell lines were 5 nM and 3.3 nM, respectively). However, there was no significant effect in wild-type EGFR cell lines with concentrations up to 10 μM. MS 39 inhibited the proliferation of H3255 lung cancer cells in vitro and was bioavailable in mice after administration.

Monomethyl auristatin E (MMAE) (MMAE), an antimitotic agent, inhibits cell division by blocking the polymerization of tubulin and also has inhibition of antibody-drug conjugates (ADCs) activity.

Azido-PEG10-alcohol, a PEG-based PROTAC linker, is utilized in PROTAC synthesis [1].

Amino-PEG10-acid is a PEG-based PROTAC linker utilized in PROTAC synthesis.

Thalidomide-O-amido-PEG2-C2-NH2 TFA (E3 Ligase Ligand-Linker Conjugates 24 TFA) is a synthesized E3 ligase ligand-linker conjugate incorporating the Thalidomide-based cereblon ligand and a 2-unit PEG linker, utilized in PROTAC technology.

Fmoc-NH-PEG10-acid, a PEG-based PROTAC linker, is utilized in the synthesis of PROTACs.

Hydroxy-PEG10-acid (HO-PEG10-CH2CH2COOH) is a PEG-based PROTAC linker that can be used to synthesize PROTACs[1].

MMAD (Demethyldolastatin 10) is a potent tubulin inhibitor. MMAD is a toxin payload in antibody drug conjugates (ADCs).

Boc-NH-PEG3 (PROTAC Linker 10) is a PEG derivative featuring a hydroxyl group and a Boc-protected amino group, used as a PROTAC linker.

CP-10 is a PROTAC with highly selective and remarkable CDK6 degradation (DC50: 2.1 nM). It inhibits the proliferation of several hematopoietic cancer cells including multiple myeloma and can degrade mutated and overexpressed CDK6.

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 is a potent and selective degrader of CDK8, with an IC50 of 159 nM, based on PROTAC.

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).

(10-BRomodecyl)phosphonic acid is an alkyl chain-derived PROTAC linker suitable for PROTAC synthesis [1].

The compound [10-(diethoxy-phosphoryl)-decyl]-phosphonic acid is a suitable alkyl chain-based PROTAC linker for the synthesis of PROTACs [1].

Amino-PEG10-amine is a PEG-based PROTAC linker employed for the conjugation of two mono diethylstilbestrol (DES)-based ligands. This compound offers an alternative approach to the synthesis of highly selective and active ER antagonists, which are crucial for the advancement of endocrine therapy in breast cancer treatment[1].

Amino-PEG10-Boc is a PEG-based linker for PROTACs that connects two essential ligands, facilitating selective protein degradation through the ubiquitin-proteasome system within cells.

Amino-PEG10-OH is a non-cleavable 10-unit PEG ADC linker employed in the synthesis of antibody-drug conjugates (ADCs)[1].

Azido-PEG10-acid is a PEG-based linker for PROTACs, joining two essential ligands crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.

Azido-PEG10-amine is a PEG-based linker for PROTACs that connects two essential ligands, facilitating the formation of PROTAC molecules and enabling selective protein degradation through the ubiquitin-proteasome system within cells.