by 27

BY27, a potent and selective BET BD2 inhibitor (Ki: 3.1 nM) with anticancer activity, inhibits BD1 BD2 of BRD2, BRD3, BRD4, and BRDT, and suppresses tumor growth.

β-Endorphin (1-27) (human) acetate, existing in the hypophysis cerebri and hypothalamus, exhibits antinociception activity. β-Endorphin (1-27) (human) acetate is an agonist of opioid receptor, showing preferred affinity for μ-opioid receptor and δ-opioid

BRD4 Inhibitor-27 is a potent BRD4 inhibitor that inhibits BRD4 BD1 and BRD4 BD2 with IC50s of 9.6 and 11.3 μM, respectively.BRD4 Inhibitor-27 has anticancer activity and can be used for breast cancer research.

LSD1-IN-27 is a potent LSD1 inhibitor with an IC50 value of 13 nM.LSD1-IN-27 inhibited the stemness and migration of gastric cancer cells.LSD1-IN-27 inhibited the expression of PD-L1 in BGC-823 and MFC cells.LSD1-IN-27 potentiated the T-cell immune response against gastric cancer.

Questiomycin A derivatives 27 is a useful organic compound for research related to life sciences and the catalog number is T72086.

HS-27 is a fluorescently-tethered inhibitor of Hsp90 with SNX-5422 tethered via a PEG linker to a fluorescein isothiocyanate or FITC. HS-27 can be used in see-and-treat paradigms.

BPO-27 racemate (BPO-27 (racemate)) is an effective CFTR inhibitor with IC50 of 8 nM.

Gap 27 is a peptide(Ser-Arg-Pro-Thr-Glu-Lys-Thr-Ile-Phe-Ile-Ile) derived from connexin 43 that is a selective gap junction blocker.

Antibacterial agent 27 has potent anti-Candida activity.

ALW-II-41-27 (Eph receptor tyrosine kinase inhibitor), an Eph receptor tyrosine kinase inhibitor, is used for cancer therapy.

AChE-IN-27 is a small molecule used for high-throughput assays.

Pituitary adenylate cyclase-activating peptide (PACAP) (6-27) is a PACAP receptor antagonist with IC50 values of 1,500, 600, and 300 nM, respectively, for rat PAC1, rat VPAC1, and human VPAC2 recombinant receptors expressed in CHO cells. It binds to PACAP receptors on SH-SY5Y and SK-N-MC human neuroblastoma and T47D human breast cancer cells (IC50s = 24.5, 106, and 105 nM, respectively) and inhibits cAMP accumulation induced by PACAP (1-38) (Kis = 457, 102, and 283 nM, respectively, in SH-SY5Y, SK-N-MC, and T47D cells). In vivo, in newborn pigs, PACAP (6-27) (10 μM) inhibits vasodilation of pial arterioles induced by PACAP (1-27) and PACAP (1-38) . It also inhibits PACAP (1-27)-stimulated increases in plasma insulin and glucagon levels and pancreatic venous blood flow in dogs when administered locally to the pancreas at a dose of 500 μg.

β-Endorphin (1-27) (human) is an opioid antagonist that selectively binds to μ-, δ-, and κ-opioid receptors, with dissociation constants (Kis) of 5.31, 6.17, and 39.82 nM, respectively. It inhibits analgesia induced by both β-Endorphin and etorphine [1][2].

SARS-CoV-2-IN-27 disodium, a diphosphate ester featuring a C6 alkyl chain and molecular tweezers of extended length, demonstrates antiviral efficacy by achieving IC50 values of 1.0 μM against SARS-CoV-2 activity and 1.7 μM for spike pseudoparticle transduction. Additionally, it disrupts liposomal membranes, displaying an EC50 value of 6.5 μM [1].

CCK (27-33) is a C-terminal fragment of CCK , a peptide hormone found in the intestine and brain that stimulates digestion, mediates satiety, and is involved in anxiety. Non-sulfated CCK (27-33) inhibits binding of [3H]naloxone in rat cerebellum membranes (IC50 = 4 uM) and inhibits electrically-stimulated contraction of isolated guinea pig ileum (IC50 = 17 uM), an effect that can be reversed by naloxone. Unlike sulfated CCK (27-33), the non-sulfated form does not reduce exploratory behavior in mice when administered at doses up to 1 uMol/kg.

β-Endorphin (1-27) is an endogenous peptide that binds to μ-, δ-, and κ-opioid receptors (Kis = 5.31, 6.17, and 39.82 nM, respectively, in COS-1 cells expressing rat receptors). It binds to rat and mouse brain membrane preparations (IC50s = 1.1 and 5.7 nM, respectively) and induces chemotaxis of human monocytes in vitro when used at a concentration of 1 nM. Intracerebroventricular administration of β-endorphin (1-27) increases the latency to tail withdrawal in response to thermal stimulation in mice with a median antinociceptive dose (AD50) of 1,500 pmol per animal. It inhibits antinociception induced by β-endorphin in mice in response to thermal stimuli when administered at a dose of 65 pmol per animal. In rats, β-endorphin (1-27) does not affect drug-associated place preference when administered at doses up to 20 μg, i.c.v., but inhibits β-endorphin-induced place preference when administered at a dose of 10 μg per animal.

SARS-CoV-2-IN-27, a diphosphate ester featuring a C6 alkyl chain and extended-length molecular tweezers, demonstrates antiviral efficacy, with IC50 values of 1.0 μM and 1.7 μM against SARS-CoV-2 activity and spike pseudoparticle transduction, respectively. Additionally, it disrupts liposomal membranes, evidenced by an EC50 of 6.5 μM [1].

Antitubercular agent-27 (compound 1) exhibits potent antitubercular properties with an IC50 of 3.2 μM, an MIC of 7.8 μM, and an IC90 of 7.0 μM, effectively targeting resistant Mycobacterium tuberculosis H37Rv isolates and displaying significant intracellular antimycobacterial activity with low cytotoxicity [1].

4-oxo-27-TBDMS Withaferin A is a derivative of the steroidal lactone withaferin A that has anticancer activity.1 It is cytotoxic to A2780 ovarian cancer cells (IC50 = 17 μM) but not to carboplatin-resistant A2780 (A2780/CP70) cells (IC50 = >100 μM). It is selective for A2780 cells over non-cancerous ARPE19 cells (IC50 = 1,660 μM). 4-oxo-27-TBDMS Withaferin A induces DNA fragmentation in A2780 cells.References1. Perestelo, N.R., Llanos, G.G., Reyes, C.P., et al. Expanding the chemical space of withaferin A by incorporating silicon to improve its clinical potential on human ovarian carcinoma cells. J. Med. Chem. 62(9), 4571-4585 (2019). 4-oxo-27-TBDMS Withaferin A is a derivative of the steroidal lactone withaferin A that has anticancer activity.1 It is cytotoxic to A2780 ovarian cancer cells (IC50 = 17 μM) but not to carboplatin-resistant A2780 (A2780/CP70) cells (IC50 = >100 μM). It is selective for A2780 cells over non-cancerous ARPE19 cells (IC50 = 1,660 μM). 4-oxo-27-TBDMS Withaferin A induces DNA fragmentation in A2780 cells. References1. Perestelo, N.R., Llanos, G.G., Reyes, C.P., et al. Expanding the chemical space of withaferin A by incorporating silicon to improve its clinical potential on human ovarian carcinoma cells. J. Med. Chem. 62(9), 4571-4585 (2019).

GRP (14-27) (human, porcine, canine) serves as a ligand for bombesin receptors, with specific binding inhibited by GTP and GDP, but unaffected by GMP [1].

high affinity agonist of the translocator protein

JAK-IN-27, also known as compound 1, is an orally active, potent inhibitor of the JAKS family kinases, displaying inhibitory concentrations (IC50s) of 3.0 nM for TYK2, 7.7 nM for JAK1, and 629.6 nM for JAK3. Moreover, JAK-IN-27 impedes IFN-α2B-induced phosphorylation of STAT3 in Jurkat cells with an IC50 of 23.7 nM [1].

α-Glucosidase-IN-27 (compound 8l), an α-glucosidase inhibitor with an IC50 of 25.78 μM, demonstrates potential for type 2 diabetes (D2M) research [1].

Antiproliferative Agent-27 (Compound 11) is a notable antiproliferative agent that markedly diminishes tumor cell colony formation and induces apoptosis, demonstrating potential for utilization in cancer research [1].

PD-1 PD-L1-IN-27 is a potent inhibitor of PD-1 PD-L1, with an IC50 of 134 nM, and demonstrates antitumor effects with minimal T cell cytotoxicity. It activates CD8+ T cells and mitigates T cell exhaustion [1].

STING agonist-27 (CF509) is a non-nucleotide, small-molecule STING agonist that activates STING and shows activity against SARS-CoV series strains [1].

VEGFR-2-IN-27 (compound 7a) is a potent VEGFR-2 inhibitor (IC50: 14.8 nM) suitable for anticancer research.

HDAC-IN-27 is a potent and orally active inhibitor of HDAC Class I (0.43 nM - 3.01 nM for HDAC1-3). HDAC-IN-27 shows activity against anti-acute myeloid leukemia (AML).

PACAP (6-27) (human, ovine, rat) is an antagonist for the PACAP receptor, inhibiting the catecholamine response of the canine adrenal gland to vasoactive intestinal peptide (VIP), making it a valuable compound for research into cardiovascular and neurological disorders [1].

ICMT-IN-27, also known as compound 64, is an inhibitor of the enzyme ICMT, demonstrating potent activity with an IC50 value of 0.1 µM [1].

Acetyl-(D-Phe2,Lys15,Arg16,Leu27)-VIP(1-7)-GRF(8-27) is a selective antagonist for the vasoactive intestinal peptide 1 (VIP 1) receptor.

BTK-IN-27 (example 8), a potent BTK inhibitor with an IC50 of 0.2 nM, demonstrates anti-proliferative effects in TMD8 cells with an IC50 of less than 5 nM. It is suitable for the research of various conditions including cancer, lymphoma, leukemia, and immunological diseases [1].

27-Hydroxycholesterol (25(R)-27-hydroxy Cholesterol) is a selective modulator of estrogen receptor and an agonist of the liver X receptor.

HBV Seq1 aa:18-27 is a hepatitis B virus (HBV) core antigen peptide fragment spanning amino acids 18-27 [1].

BMAP-27, an antimicrobial peptide, disrupts the membrane integrity of microorganisms, exhibiting inhibitory activity against bacteria and cancer cells due to its membrane permeability [1].

Tubulin Inhibitor 27 (DYT-1), a compound that inhibits tubulin polymerization with an IC50 of 25.6 μM, exhibits anti-angiogenesis and antitumor activities [1].

PHI-27 (porcine) is a 27-amino acid peptide derived from pigs, used to identify peptide hormones and other bioactive peptides [1].

Antibiotic JBIR 27 is a useful organic compound for research related to life sciences. The catalog number is T126295 and the CAS number is 1172094-65-3.

27-Alkyne Cholesterol, an alkyne derivative of cholesterol, facilitates the investigation of cholesterol metabolism and localization through click chemistry with reporter azides in both fixed and living cells. It serves as a substrate for enzymes across diverse species such as bacteria, yeast, rat, and human.

Antimalarial agent 27 (compound 11a) potently inhibits P. falciparum with an IC50 of 0.37 μM, targeting the parasite's 1-deoxy-D-xylulose-5-phosphate reductoisomerase (DXR) enzyme with an IC50 of 0.11 μM, indicating its mechanism of action [1].

CDK9-IN-27 (Compound 6a), a CDK9 inhibitor with an IC50 of 0.424 μM, induces apoptosis and S-phase cell cycle arrest. It exhibits cytotoxicity against HepG2, HCT-116, and MCF-7 cell lines, with IC50 values ranging from 10.31 to 40.34 μM, rendering it applicable in cancer research [1].

HPK1-IN-27 is a potent inhibitor of HPK1 [MAP4K1, also known as hematopoietic progenitor kinase 1], a member of the germinal center kinase family and a serine threonine kinase, and has shown research potential for cancer diseases.

Antifungal agent 27 (compound 7) is a chemical compound with antifungal properties, exhibiting moderate antibacterial activity and weak antifungal activity against MRSA and C. albicans SS5314, with minimal inhibitory concentration (MIC) values of 8 and 32 μg mL, respectively [1].

PHI 27 (human) trifluoroacetate is a useful organic compound for research related to life sciences and the catalog number is T64705.

7β,27-dihydroxy Cholesterol is an oxysterol and agonist of retinoic acid receptor-related orphan receptor γ (RORγ) and RORγt. [1] It activates RORγ- or RORγt-dependent signaling with EC50 values of 691 and 1,045 nM, respectively, in reporter assays using HEK293T cells expressing the recombinant human receptors. 7β,27-dihydroxy Cholesterol is selective for RORγ and RORγt over a panel of eight additional nuclear receptors at 30 µM. It increases IL-17A production in Th17-polarized isolated human na ve CD4+ T cells when used at a concentration of 300 nM. 7β,27-dihydroxy Cholesterol (60 mg/kg) increases IL-17A production in isolated mouse γδ T cells stimulated with 12-myristate 13-acetate and ionomycin .

Dc-y13-27, a derivative of DC-Y13, is a potent YTHDF2 inhibitor (KD: 37.9 μM). DC-Y13-27 has antitumor activity that enhances the response of radiotherapy and immunotherapy to tumors.

MAO-B-IN-27 (Compound 12c), a monoamine oxidase B (MAO-B) inhibitor, exhibits a potent and selective inhibitory effect on hMAO-B with an IC50 value of 8.9 nM, and is utilized in Parkinson's disease (PD) research [1].