azd 1775 linker conjugate 1 tfa

AZD 1775 Linker Conjugate 1 TFA is a compound involved in ubiquitinase-targeted chimeric assays

JAG-1, scrambled TFA is a scrambled sequence of JAG-1(188-204).

Aβ-IN-1 TFA inhibits and reverses different types of protein aggregation.

pro-asp TFA(85227-98-1 free base) (TLβ4) down-regulate skin inflammation in mouse skin.

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

Nociceptin (1-13), amide is a potent agonist Opioid receptor-like1 (ORL1) receptor with a pEC50 of 7.9 for mouse vas deferens and a Ki of 0.75 nM for binding to rat forebrain membranes.

TT2-32 TFA induces a biphasic activation of phosphotyrosine phosphatase activity in human colon tumor cell line, SW620

Jagged-1 (188-204) TFA(219127-21-6 free base) is a fragment of the JAG-1 protein. JAG-1 is Notch ligand, a peptide that is the most conspicuously expressed ligand in skin. JAG-1 induces epidermal maturation. Exposing submerged keratinocytes monolayers to JAG-1 with elevated calcium concentration produces stratification with loricrin expression and NF-alphaB activation.

Rotigaptide TFA(355151-12-1 free base) is a novel and specific modulator of Cx43 and is a potent AAP. Rotigaptide TFA(355151-12-1 free base) prevents the uncoupling of Cx43-mediated gap junction communication and normalizes cell-to-cell communication during acute metabolic stress.

740 Y-P(TFA)(1236188-16-1 free base) (740YPDGFR(TFA)) is a potent and cell-permeable activator of PI3K.

Biotin-β-Amyloid (1-42), human TFA, also known as Biotin-Amyloid β-Peptide (1-42) (human) TFA, is a biotin-labeled 42-amino acid peptide implicated in the pathogenesis of Alzheimer's disease.

TPP-1 TFA, a potent inhibitor of the PD-1/PD-L1 interaction, selectively binds to PD-L1 with high affinity (K D =95 nM). It effectively inhibits human tumor growth in vivo by reactivating T-cell function [1].

Protease-Activated Receptor-1 (PAR-1) Agonist TFA is a selective peptide that acts as an agonist for the proteinase-activated receptor-1 (PAR-1). Corresponding to the tethered ligand of PAR-1, this compound mimics the actions of thrombin through the PAR-1 receptor[1][2].

GIP (1-30) amide, porcine TFA is a high-affinity full agonist of the glucose-dependent insulinotropic polypeptide (GIP) receptor, with potency comparable to native GIP(1-42) [1]. It also exhibits potent insulin-stimulating properties and weakly inhibits gastric acid secretion.

αvβ1 Integrin-IN-1 TFA (Compound C8) is a potent, selective inhibitor of αvβ1 integrin, demonstrating an IC 50 value of 0.63 nM. It exhibits antifibrotic effects [1].

Acts as a cardiac hormone with a variety of biological actions including natriuresis, diuresis, vasorelaxation, and inhibition of renin and aldosterone secretion. It is thought to play a key role in cardiovascular homeostasis. Helps restore the body\'s sa

IRL-1620 (TFA) is a potent selective endothelin receptor B (ETB) agonist with a Ki value of 16pm.

Apelin-13 is an endogenous ligand of APJ receptor, and the EC 50 value of activated G protein coupled receptor is 0.37 nM.

Magainin 1 TFA is an antimicrobial amphiphilic peptide isolated from xenopus skin.

S961 TFA is A high affinity insulin receptor (IR) antagonist with IC50 for hir-a, hir-b and human insulin-like growth factor I receptor (higf-ir) at 0.048, 0.027 and 630 nM, respectively.

PD-1/PD-L1-IN 3 TFA inhibits the binding of human PD-1 to PD-Ll with an IC50 of 9 nM.

Angiotensinogen (1-14), human TFA is a fragment of the renin substrate angiotensinogen, which is a precursor for all angiotensin peptides.

β-Melanocyte Stimulating Hormone (MSH), human (Synonyms: Beta-MSH (1-22) (human)) β-Melanocyte Stimulating Hormone (MSH), human, a 22-residue peptide, acts as an endogenous melanocortin-4 receptor (MC4-R) agonist.

PACAP (1-27), human, ovine, rat TFA (PACAP 1-27 TFA), an N-terminal fragment of PACAP-38, is an effective PACAP receptor antagonist with IC50 values of 3 nM for rat PAC1, 2 nM for rat VPAC1, and 5 nM for human VPAC2.

Gastrin I (1-14), human TFA, is the 1-14 fragment of the human gastrin I peptide.

cIAP1 Ligand-Linker Conjugates 1 is composed of an IAP ligand for the E3 ubiquitin ligase and a PROTAC linker. This compound, cIAP1 Ligand-Linker Conjugates 1, is particularly useful in the development of SNIPERs[1].

αvβ1 integrin-IN-1 TFA is an effective and selective αvβ1 integrin inhibitor (IC50: 0.63 nM).

hDDAH-1-IN-1 TFA is a selective non-amino acid catalytic site inhibitor of human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1) (Ki: 18 μM).

AhR Ligand-Linker Conjugates 1, also known as E3 Ligase Ligand-Linker Conjugates 57, is a chemical compound that combines an IAP ligand for the E3 ubiquitin ligase with a SNIPER linker. It is specifically designed to be used in the development of SNIPER[1].

K-Ras ligand-Linker Conjugate 4 is a chemical compound combining a K-Ras recruiting ligand with a PROTAC linker, responsible for recruiting E3 ligases such as VHL, CRBN, MDM2, and IAP. It has the potential to be used in synthesizing PROTAC K-Ras Degrader-1, which shows a degradation efficacy of ≥70% in SW1573 cells[1].

PD-1-IN-17 TFA is a potent inhibitor of programmed cell death-1 (PD-1), effectively inhibiting 92% of splenocyte proliferation at a concentration of 100 nM.

β-Amyloid (1-43)(human) TFA exhibits greater aggregation tendencies and heightened toxicity compared to Aβ1-42. This compound also associates with sAPPα and sAPPβ and has the potential to serve as an additional biomarker for Alzheimer’s disease (AD), complementing existing markers [1].

ACTH (1-14) (TFA) is a regulatory fragment of adrenocorticotropin, involved in controlling cortisol and androgen synthesis [1].

Super-TDU (1-31) TFA, a peptide fragment of Super-TDU, acts as an inhibitor of the YAP-TEAD complex. Demonstrating potent anti-tumor activity, it effectively suppresses tumor growth in a gastric cancer mouse model [1] [2].

E3 Ligase Ligand-linker Conjugate 7, a conjugate of E3 ligase ligand and linker, consists of Thalidomide and the corresponding Linker. It serves as a Cereblon ligand to recruit CRBN protein and is a key intermediate for the synthesis of complete PROTAC molecules.

E3 Ligase Ligand-Linker Conjugate 34 comprises Thalidomide linked to a corresponding linker, serving as a conjugate between an E3 ligase ligand and a linker. This compound acts as a cereblon ligand, recruiting the CRBN protein and functioning as an essential intermediate in the synthesis of complete PROTAC molecules.

Hemokinin 1, human TFA acts as a selective full agonist at the tachykinin neurokinin 1 (NK1) receptor, while also being a full agonist at NK2 and NK3 receptors. It is capable of inducing opioid-independent analgesia [1] [2].

Dynorphin B (1-13) TFA, an agonist of the opioid κ-receptor.

HIV Protease Substrate 1 TFA, a fluorogenic substrate for HIV protease, facilitates the investigation of the enzyme's activity [1].

Defensin HNP-1 Human TFA, a human neutrophil peptide (HNP), plays a role in the early development of atherosclerosis by contributing to endothelial cell dysfunction. Additionally, it has demonstrated broad-spectrum antimicrobial and anti-leishmanial effects [1] [2].

[Nphe1]Nociceptin(1-13)NH2 is a novel endogenous ligand for the nociceptin/orphanin FQ (NC) receptor, acting as a selective and competitive antagonist without any agonist effects. It binds specifically to recombinant nociceptin receptors with high affinity (pKi=8.4) and effectively blocks nociceptin's ability to inhibit cyclic AMP accumulation in CHO cells (pA2=6.0), showcasing potential as an analgesic agent.

MIF-1 TFA (Melanostatin), an intrinsic brain peptide, serves as a powerful allosteric modulator of the dopamine receptor. It plays a crucial role in regulating melanin production and modifies the analgesic efficacy by inhibiting the opioid receptor's effects. Significantly, MIF-1 TFA can cross the blood-brain barrier (BBB) directly, facilitating its access from the bloodstream to the central nervous system (CNS) [1] [2] [3].

GLP-1(9-36)amide TFA, a predominant metabolite of glucagon-like peptide-1-(7-36)amide synthesized through dipeptidyl peptidase-4 (DPP-4) activity, functions as an antagonist to the human pancreatic GLP-1 receptor [1] [2].

187-1, N-WASP Inhibitor TFA, a 14-amino acid cyclic peptide, serves as an allosteric inhibitor of the neural Wiskott-Aldrich syndrome protein (N-WASP). This compound effectively suppresses actin assembly triggered by phosphatidylinositol 4,5-bisphosphate (PIP2), exhibiting a potent inhibitory concentration (IC 50) of 2 μM. Furthermore, 187-1, N-WASP Inhibitor TFA inhibits the activation of the Arp2/3 complex by N-WASP, maintaining the protein in its autoinhibited state, ensuring the prevention of its activation.

GLP-1(28-36)amide TFA, a C-terminal nonapeptide derived from GLP-1 cleavage by neutral endopeptidase (NEP), is an antioxidant that targets mitochondria and inhibits mitochondrial permeability transition (MPT), demonstrating anti-diabetic and cardioprotective effects [1].

Zn-DPA-maytansinoid conjugate 1, a small molecule-based immune checkpoint-targeting maytansinoid conjugate, effectively induces sustained tumor growth regression and transforms the tumor microenvironment (TME) into an inflamed hot tumor [1].

Galanin (1-16), mouse, porcine, rat is a potent agonist of the hippocampal galanin receptor with a Kd of 3 nM, and it exhibits high biological activity on locus coeruleus neurons.

ACTH (1-17) TFA is a corticotrophin analogue and an effective human melanocortin 1 (MC1) receptor agonist with Ki value of 0.21 nM.