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.

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

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.

SM27 is a fibroblast growth factor 2 (FGF2) inhibitor with anti-angiogenic activity and can be used to study tumours.

BAY-27-9955 is a glucagon receptor antagonist.

high affinity agonist of the translocator protein

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.

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

Compound 55052-27-2, with CAS No. 55052-27-2, is a fragment molecule that serves as an important scaffold for molecular linking, expansion, and modification. Compound 55052-27-2 provides a structural basis and research tool for the design and screening of novel drug candidates, and is commonly used in drug discovery, drug synthesis, and related research.

Compound 4265-27-4, with CAS No. 4265-27-4, is a fragment molecule that serves as an important scaffold for molecular linking, expansion, and modification. Compound 4265-27-4 provides a structural basis and research tool for the design and screening of novel drug candidates, and is commonly used in drug discovery, drug synthesis, and related research.

FLT3-IN-27 (compound 49) is an inhibitor of FLT3-ITD with an IC50 of 174 nM. It impedes cell growth by causing cell cycle arrest at the G1 phase, making it suitable for research in acute myeloid leukemia.

HDAC-IN-27 dihydrochloride (Compound 11h) is a potent, orally active, HDACI class-selective inhibitor, with IC50 values ranging from 0.43 to 3.01 nM for HDAC1-3. This compound exhibits both in vivo and in vitro anticancer activity. HDAC-IN-27 shows significant antiproliferative effects against acute myeloid leukemia (AML) cell lines by inducing apoptosis and histone acetylation (AcHH3 and AcHH4). It is useful for research on acute myeloid leukemia (AML).

AKT-IN-27 (4a) is a potential anticancer drug that functions by selectively targeting Akt-driven signaling pathways. It induces apoptosis by activating caspase-3, causing G2/M phase cell cycle arrest, and disrupting mitochondrial membrane potential. AKT-IN-27 (4a) is applicable in research on triple-negative breast cancer (TNBC).

ATX inhibitor 27 (Compound 31) is an ATX inhibitor. It demonstrates IC50 values of 13 nM against human autotaxin (hATX) and 23 nM against lysophosphatidylcholine (LPC). By inhibiting the ATX enzyme, ATX inhibitor 27 reduces LPA levels in the body. This compound is applicable in research related to ATX-LPA-associated conditions such as inflammation, neurodegenerative disorders, and cancer.

MDM2-IN-27 primarily targets the MDM2 protein with a Ki value of 0.4 nM. By blocking the negative regulation of p53 by MDM2, it activates the tumor-suppressing activity of p53 and induces apoptosis.

SDH-IN-27 (Compound Q18) is a succinate dehydrogenase inhibitor (SDHI) with an IC50 of 9.7 mg/L. It induces hyphal morphological changes and lipid peroxidation, demonstrating antifungal activity against C. camelliae with an EC50 of 6.0 mg/L. SDH-IN-27 also acts as an ergosterol biosynthesis inhibitor (EBI) by binding to the active site of CYP51, ultimately resulting in the death of pathogenic fungal cells.

AChE/BChE-IN-27 is a brain-permeable dual inhibitor of AChE and BChE, with IC50 values of 3.72 μM and 9.65 μM, respectively, and a permeability coefficient (Pe) of 4.12. It exhibits significant antioxidant activity with an IC50 of 6.32 μM in DPPH assays and also demonstrates strong in vitro antioxidant capabilities. The compound shows metal-chelating properties and has neuroprotective potential against oxidative stress by significantly reducing intracellular reactive oxygen species (ROS). In vivo experiments reveal that AChE/BChE-IN-27 effectively restores AChE and BChE levels and improves cognitive function, indicating its potential application for Alzheimer’s disease (AD).

IDO1-IN-27 (Compound I-1) is an inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), displaying an IC50 of 0.3951 μM against recombinant hIDO1. It also inhibits hIDO1 expression in HeLa cells with an EC50 of 62 nM. By reducing the mRNA expression of pro-inflammatory factors (TNF-α, IL-6, and IL-1β), IDO1-IN-27 effectively stimulates T cell proliferation and simultaneously inhibits the growth of LLC cells.

27-Hydroxy oncosterone is a metabolite that inhibits the proliferation of breast cancer (BC) cells, and it also prevents the proliferation of BC cells induced by cancerosterone and 27-Hydroxycholesterol.

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).

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.

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.