isoform

MPI_5a is an effective and selective inhibitor of HDAC6 (IC50=36 nM). MPI_5a weakly inhibits other HDAC isoforms and it also inhibits acyl-tubulin accumulation in cells (IC50: 210 nM).

Beta-defensin 103 isoform X1, pig, is an antimicrobial peptide found in various organisms, essential for the initial defense mechanisms of the innate immune system against pathogens [1].

Beta-defensin 103 isoform X1, pig TFA, is an antimicrobial peptide found in various living organisms, crucial for the initial defense of the innate immune system against pathogens [1].

Prokineticin 2 Isoform 2 (human), a hypothalamic neuropeptide, regulates thermoregulation and energy metabolism while decreasing food intake in rodents. This isoform is implicated in the study of metabolic syndrome (MetS), obesity, and hyperglycemia [1].

Isoformononetin (IFN) is a methoxy isoflavone present in human dietary supplements that exhibits immune-protective effects by preventing neuroinflammation in a streptozotocin-induced rat model through inhibition of the NLRP3 ASC IL-1 axis activation.

Epristeride (ONO-9302) is an orally active, selective and non-competitive steroidal 5-α-reductase isoform 2 inhibitor that inhibits SR isoform 2.Episteride reduces prostate size and improves symptoms in men with BPH.Episteride induces atrophy and apoptosis of the ventral prostate in rats.

TGX-115 is a cell-permeable and potent inhibitor of the PI 3-K isoform p110β p110δ (IC50 values of 0.13 μM for p110β and 0.63 μM for p110δ), an enzyme that regulates platelet adhesion and inhibits phosphoinositide (PI) 3-kinase, and can be used to treat coronary artery occlusion, stroke, acute coronary artery It can be used to treat cardiovascular diseases such as coronary occlusion, stroke, acute coronary syndrome, acute myocardial infarction, restenosis, atherosclerosis and unstable angina.

AKP-001 is a selective inhibitor of MAPK of the p38α isoform and is used in the study of immune and digestive disorders.

FR-167356 is a specific inhibitor of a3 isoform vacuolar type H⁺-ATPase with IC50s of 170 nM, 370 nM and 220 nM for osteoclast plasma membranes, renal brush border membranes and macrophage microsomes. FR-167356 reduces bone metastasis of B16-F10 cells.

L-797,591 hydrochloride is active for somatostatin receptor isoform 1 (SSTR1). L-797,591 hydrochloride is commonly used in combination with AG1478 to enhance p-ERK5 expression in SSTR1 cells. L-797,591 hydrochloride significantly enhanced p38 phosphorylation in cotransfected cells, and this effect was reversed in combination with AG1478.

5,6-trans-Vitamin D3(5,6-trans-Cholecalciferol) is an isoform of Vitamin D3, which is converted from Vitamin D3 on the skin surface after light exposure.

CNX-1351 is a potent, isoform-selective, and targeted covalent inhibitor of PI3Kα.

Alizarin (Mordant Red 11), a red dye derived from the roots of plants of the madder genus, inhibits P450 isoform CYP1A1( IC50 = 6.2 μM), CYP1A2 (IC50 =10.0 μM )and CYP1B1(IC50 = 2.7 μM).

(-)-(S)-Equol (4',7-Dihydroxyisoflavan) is an orally bioavailable, non-steroidal estrogen naturally produced by the metabolism of the isoflavonoid daidzein by human intestinal microflora, with potential chemoprotective and estrogen receptor (ER) modulating activities. S-equol preferentially binds to and activates the beta isoform of ER in certain target tissues, while having an antagonistic effect in other tissues. This modulates the expression of ER-responsive genes in a tissue-specific manner. This agent may increase bone mineral density, affect vasomotor symptoms, and may decrease the proliferation rate of susceptible cancer cells. In addition, this agent interferes with the activity of enzymes involved in steroid biosynthesis. S-equol inhibits dihydrotestosterone (DHT) production and may inhibit the proliferation of androgen-driven prostate cancer. S-equol is the biologically active enantiomer while R-equol is essentially inactive and has a weak affinity for alpha-ER.

MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4).

Taselisib (GDC-0032) is an orally bioavailable inhibitor of the class I phosphatidylinositol 3-kinase (PI3K) alpha isoform (PIK3CA), with potential antineoplastic activity.

BVT 2733 is a new, non-steroidal, isoform-specific inhibitor of 11β-HSD1.

(E Z)-Endoxifen ((E Z)-Endoxifen) is an active metabolite of tamoxifen produced by the sequential action of cytochrome P450 (CYP) isoforms, including CYP2D6. It is a strong anti-estrogen, as it has an approximately 100-fold greater affinity for estrogen receptors than tamoxifen. As the efficient conversion of tamoxifen to endoxifen depends on CYP2D6, polymorphisms in this CYP isoform can impact the effectiveness of TMX treatment.

PF-543 hydrochloride (PF-543) inhibits SphK1 with a K(i) of 3.6 nM, is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform.

AC-55649 is a potent and highly isoform-selective agonist of the human RARβ2 receptor, characterized by a pEC50 of 6.9.

NKY80 regulates the adenylyl cyclase catalytic activity in heart and lung tissues. NKY80 is a non-competitive inhibitor of adenylyl cyclase type V isoform (IC50s: 8.3 µM, 132 µM, and 1.7 mM for type V, III and II, respectively).

AS-041164 is a selective and orally active PI3Kγ isoform inhibitor(IC50 of 70 nM), and shows less activity against PI3Kα, PI3Kβ, and PI3Kδ (IC50s of 240 nM, 1.45 μM, and 1.70 μM, respectively). It has anti-inflammatory effects.

GDC-0326 is a potent and selective inhibitor of the α-isoform of Phosphoinositide 3-Kinase (PI3Kalpha inhibitor).

AGI-41998 tautomers is a tautomerism of pyrido[4,3-d]pyrimidin-7(6H)-one, 8-(4-bromophenyl)-6-(4-methoxyphenyl)-2-[(2,2,2-trifluoroethyl)amino]-. pyrido[4,3-d]pyrimidin-7(6H)-one, 8-(4-bromophenyl)-6-(4-methoxyphenyl)-2-[(2,2,2-trifluoroethyl)amino]- is a S-adenosylmethionine synthase isoform type-2 inhibitor, IC50= 0.022μM.