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Gene Regulation

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13-cis-Retinoic acid ≥98% (HPLC) 13-cis-Retinoic acid (RA) has anti-inflammatory and anti-tumor action. The action of RA is mediated through RAR-β and RAR-α receptors. RA attenuates iNOS expression and activity in cytokine-stimulated murine mesangial cells. It induces mitochondrial membrane permeability transition, observed as swelling and as a decrease in membrane potential, and stimulates the release of cytochrome c implicating mechanisms through the apoptosis pathway. These activities are reversed by EGTA and cyclosporin A. RA also increases MMP-1 protein expression partially via increased transcription.
4759-48-2 R3255
15-Deoxy-Δ12,14-prostaglandin J2 ≥95% (HPLC), methyl acetate solution Selective agonist to PPARγ (peroxisome proliferator-activated receptors). Inhibits the proliferation of cancer cell lines that express PPARγ and cyclooxygenase-2 (COX-2).
89886-60-2 D8440
4-Hydroxytamoxifen Minimum 70% of Z isomer (remainder primarily E-isomer) Metabolite of the chemotherapeutic drug tamoxifen, exhibiting more potent estrogen agonist/antagonist activity than the parent drug. Also active as intra-membranous inhibitor of lipid peroxidation.
The trans (Z) isomer has efficacy against estrogen-sensitive cancers. The cis (E) isomer is an estrogen agonist.
68047-06-3 H6278
5-Aza-2′-deoxycytidine ≥97% 5'-Azadeoxycytidine causes DNA demethylation or hemi-demethylation. DNA demethylation can regulate gene expression by "opening" the chromatin structure detectable as increased nuclease sensitivity. This remodeling of chromatin structure allows transcription factors to bind to the promoter regions, assembly of the transcription complex, and gene expression.
2353-33-5 A3656
5-Azacytidine ≥98% (HPLC) A potent growth inhibitor and cytotoxic agent; inhibits DNA methyltransferase, an important regulatory mechanism of gene expression, gene activation and silencing.
Causes DNA demethylation or hemi-demethylation, creating openings that allow transcription factors to bind to DNA and reactivate tumor suppressor genes.
320-67-2 A2385
9-cis-Retinoic acid ~98% (HPLC) Ligand for both the retinoic acid receptor (RAR) and the retinoid X receptor (RXR) that act as transcription factors to regulate the growth and differentiation of normal and malignant cells.
5300-03-8 R4643
Cholecalciferol ≥98% (HPLC) Vitamin D acts through a receptor that is a member of the ligand-dependent transcription factor superfamily. Modulates the proliferation and differentiation of both normal and cancer cells. Has antiproliferative and antimetastatic effects on breast, colon, and prostate cancer cells. Activated vitamin D receptors in intestine and bone maintain calcium absorbance and homeostasis.
67-97-0 C9756
Ciglitizone ≥99% (TLC) Selective peroxisome proliferator-activated receptor-γ (PPARγ) agonist (EC50 = 3 μM) and antihyperglycemic agent displaying activity in genetically obese C57 B1/6 ob/ob mice.
74772-77-3 C3974
Cyproterone acetate ≥98% Synthetic steroid; androgen antagonist; potent inhibitor of leukocyte migration through endothethial cell monolayers. Liver tumor promoter in experimental animal model.1
427-51-0 C3412
Epitestosterone 481-30-1 E5878
Flutamide Non-steroidal anti-androgen.
13311-84-7 F9397
GW9662 >98% (HPLC), solid GW9662 is an irreversible PPARγ antagonist. GW9662 inhibits connective tissue growth factor and activation of CD36 by IL-4.
22978-25-2 M6191
Glycyrrhizic acid ammonium salt ~75% (HPLC) 100403-24-5 G2137
Melatonin powder, ≥98% (HPLC) Hormone; mediates photoperiodicity in mammals; inhibits cerebellar nitric oxide synthetase; peroxynitrite scavenger. Melatonin has complex effects on apoptotic pathways, inhibiting apoptosis in immune cells and neurons but enhancing apoptotic cell death of cancer cells. Inhibits proliferation/metastasis of breast cancer cells by inhibiting estrogen receptor action.
73-31-4 M5250
Mifepristone ≥98% Progesterone receptor antagonist; stimulates prolactin secretion. Pgp inhibitor.
84371-65-3 M8046
Procainamide hydrochloride Inhibits DNA methyltransferase and modulates epigenetic regulation of gene expression. Na+ channel blocker and Class IA anti-arrhythmic.
614-39-1 P9391
Raloxifene hydrochloride solid Selective estrogen receptor modulator (SERM); acts as an anti-estrogen in both breast and uterine tissue while being estrogenic in bone. May have efficacy against estrogen-sensitive cancers.
82640-04-8 R1402
Retinoic acid p-hydroxyanilide ≥95% Vitamin A acid analogue with antiproliferative activity in cultured human breast cancer cells; induces apoptosis in malignant hemopoietic cell lines.
65646-68-6 H7779
Retinoic acid ≥98% (HPLC), powder all−trans−Retinoic acid (ATRA) is a ligand for both the retinoic acid receptor (RAR) and the retinoid X receptor (RXR). The bound RAR and RXR act as transcription factors that regulate the growth and differentiation of both normal and malignant cells. Cytochromes P450 (CYPs) catalyze the 4-hydroxylation of ATRA. Retinoic acid primes embryonic stem cells to become neurons.
302-79-4 R2625
Retinol synthetic, ≥95% (HPLC), crystalline Ligand for both the retinoic acid receptor (RAR) and the retinoid X receptor (RXR) that act as transcription factors to regulate the growth and differentiation of normal and malignant cells.
68-26-8 R7632
Tamoxifen citrate salt ≥99% Protein kinase C inhibitor. Induces apoptosis in human malignant glioma cell lines. Tamoxifen and its metabolite 4-hydroxytamoxifen are selective estrogen response modifiers (SERMs) that act as estrogen antagonists in mammary gland. Blocks estradiol-stimulated VEGF production in breast tumor cells.
54965-24-1 T9262
Tamoxifen ≥99% Protein kinase C inhibitor. Induces apoptosis in human malignant glioma cell lines. Tamoxifen and its metabolite 4-hydroxytamoxifen are selective estrogen response modifiers (SERMs) that act as estrogen antagonists in mammary gland. Blocks estradiol-stimulated VEGF production in breast tumor cells.
10540-29-1 T5648
Tetradecylthioacetic acid ≥97% (NMR) PPARα agonist; activation in ranking order: PPARα > PPARδ > PPARγ
T1698
Troglitazone >98% (HPLC) PPARγ agonist; anti-diabetic thiazolidinedione (TZD) with anti-inflammatory and anti-tumor activity; induces apoptosis via a p53 pathway.
T2573
all trans-Retinal powder, ≥98% All-trans retinal is converted to retinoic acid in vivo by the action of retinal dehydrogenase. Retinoic acid is a ligand for both the retinoic acid receptor (RAR) and the retinoid X receptor (RXR) that act as transcription factors to regulate the growth and differentiation of normal and malignant cells. Retinal isomers are also chromophores that binds to opsins, a family of G-protein-linked transmembrane proteins, to form photosensitive receptors in visual and nonvisual systems. All-trans retinal is a potent photosensitizer.
116-31-4 R2500

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