Bioactive Small Molecules

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SML0374 U-104 ≥98% (HPLC) U-104 is an inhibitor of CA IX that binds only to CA IX under hypoxic conditions in vivo. The binding results in significant inhibition of tumor growth and metastasis formation in both spontaneous and experimental models of metastasis. U-104 reduces the medium acidity by inhibiting the catalytic activity of the CA IX. It binds specifically only to hypoxic cells expressing CA IX.
U120 U0126 monoethanolate ≥98% (HPLC), powder U0126, 1,4-diamino-2,3-dicyano-1,4-bis[2-aminophenylthio] butadiene, is a highly selective inhibitor of both MEK1 and MEK2. U0126 was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition of the dual specificity kinase MEK with IC50 of 72 nM for MEK1 and 58 nM for MEK2. U0126 inhibited anchorage-independent growth of Ki-ras-transformed rat fibroblasts by simultaneously blocking both extracellular signal-regulated kinase (ERK) and mammalian target of rapamycin (mTOR)-p70(S6K) pathways. The effects of U0126 on the growth of eight human breast cancer cell lines shown that U0126 selectively repressed anchorage-independent growth of MDA-MB231 and HBC4 cells, two lines with constitutively activated ERK. Loss of contact with substratum triggers apoptosis in many normal cell types, a phenomenon termed anoikis. U0126 sensitized MDA-MB231 and HBC4 to anoikis, i.e., upon treatment with U0126, cells deprived of anchorage entered apoptosis.
human ... MAP2K1(5604), MAP2K2(5605)
U115 U-101958 maleate salt solid U-101958 maleate salt is a selective D4 dopamine receptor antagonist. Studies have reported that U-101958 maleate cannot inhibit bromocriptine-mediated [3H]thymidine incorporation in opossum kidney (OK) cells.
human ... DRD4(1815)
U3633 U 18666A powder Inhibitor of cholesterol synthesis (inhibits desmosterol Δ24-reductase). Weak inhibitor of hedgehog (hh) signaling.
U111 (−)-trans-(1S,2S)-U-50488 hydrochloride hydrate solid, ≥98% (HPLC) Potent κ opioid receptor agonist; more potent enantiomer of (±)-trans-U-50488.
human ... OPRK1(4986)
D8040 (±)-trans-U-50488 methanesulfonate salt Selective κ-opioid receptor agonist.
human ... OPRK1(4986)
U105 U-62066 solid Highly selective κ opioid receptor agonist; antitussive.
human ... OPRK1(4986)
U103 U-69593 solid U-69593 is a selective κ opioid receptor agonist. U-69593 is known to inhibit cocaine sensitization in meso-limbic dopamine neurons by normalizing basal overflow of dopamine.
human ... OPRD1(4985), OPRK1(4986), OPRM1(4988)
mouse ... Oprk1(18387)
rat ... Oprd1(24613), Oprk1(29335), Oprm1(25601)
U6756 U-73122 hydrate powder Inhibits the hydrolysis of PPI to IP3, which leads to a decrease in cytosolic free calcium. Inhibits the coupling of G protein-phospholipase C activation, while remaining unaffected by production of cAMP.
U6881 U-73343 Inactive analog of U73122; used as a negative control.
U5882 U-74389G Free radical lipid peroxidation inhibitor in cultured brain cells, monocytic THP1 cells, and LLC-PK1 cell layers.
U116 U-99194 maleate salt ≥98% (HPLC), solid U-99194 is a putative D3 antagonist with a 30-fold preference for the dopamine D3 vs. D2 receptor.
human ... DRD3(1814)
U3385 UA62784 ≥98% (HPLC) Studies have also reported that UA62784 associates with tubulin at or near the colchicine-binding sites in cells and functions as a cytotoxic, microtubule inhibitor.
UA62784 is a specific inhibitor of centromere protein E (CENPE) kinesin-like protein; mitotic inhibitor. CENP-E is a kinesin-like motor protein that localizes to the kinetochore during mitosis and is essential for bipolar spindle formation. UA62784 is a novel specific inhibitor of CENP-E, which likely binds within the motor domain of CENP-E. UA62784 causes reversible cell cycle arrest in mitosis before metaphase, which leads to apoptosis. The compound is not interacting with microtubules directly.
U1632 Ubiquitin, Methylated from bovine erythrocytes semisynthetic, ≥90% (SDS-PAGE), essentially salt-free, lyophilized powder Methylated ubiquitin is known to block the degradation of cyclin in extracts of clam embryos.
U4135 UBP302 ≥98% (HPLC) UBP302 is a selective GluR5 antagonist. UBP302 is the active enantiomer of UB296 and is one of the most potent GluR5 antagonists available for research use.
SML0606   UBP608 ≥98% (HPLC) UBP608 is NMDA receptor family allosteric modulator that selectively inhibits GluN1/GluN2A receptors with a 23-fold selectivity compared to GluN1/GluN2D receptors. It appears to distinguish between GluN2A and GluN2B, and between GluN2C and GluN2D. UBP608 does not act at either the glutamate or glycine binding sites, the ion channel, or the NTD. It appears that UBP608 is acting at the dimer interface between individual subunit ligand-binding domains.
SML0718   UBP714 ≥95% (HPLC) UBP714 is a derivative of the NMDA receptor negative allosteric modulator UBP608 (SML0606). UBP714 potentiates the activity of recombinant GluN1/GluN2 NMDA receptors, and enhances NMDA receptor mediated EPSPs in the CA1 region of the hippocampus.
SML0821 UCD38B hydrochloride ≥98% (HPLC) UCD38B is a cell permeable inhibitor of intracellular uPA (urokinase plasminogen activator) that is cytotoxic to proliferating and non-proliferating glioma cell lines. UCD38B induces caspase-independent necrosis in U87 glioma MDA231 breast cancer cells. It appears that the necrotic pathway is mediated by AIF (apoptotic inducible factor).
SML1105 UCF-101 ≥98% (HPLC) UCF-101 is a selective inhibitor of the pro-apoptotic mitochondrial serine protease Omi/HtrA2, involved in the cellular response to thermal and oxidative stress. Like SMAC/Diablo, Omi/HtrA2 is an inhibitor of IAPs (inhibitor of apoptosis proteins), inhibiting the apoptosis inhibitors, thus resulting in pro-apoptotic activity. In septic rat studies, UCF-101 was found to inhibit apoptosis and have neuroprotective effects on cerebral oxidative injury and cognitive impairment. In aging rats with induced myocardial ischemia/reperfusion (MI/R) injury, UCF-101 treatment decreased XIAP degradation and caspase-3 activity and exerted cardioprotective effects.
U8881 UCL 1684 ditrifluoroacetate hydrate UCL 1684 ditrifluoroacetate hydrate is a potent non-peptide blocker of the apamin-sensitive Ca2+-activated K+ channel.
U5883 UCL-1848 trifluoroacetate salt ≥98% (HPLC), solid Selective Ca2+-activated, SK potassium channel blocker
U6758 UCL 2077 ≥98% (HPLC), solid UCL 2077 is a slow afterhyperpolarization (sAHP) channel blocker.
SML0514 UCM710 ≥98% (HPLC) UCM710 is a dual inhibitor of fatty acid amide hydrolase (FAAH) and α/β hydrolase domain 6 (ABHD6) the enzymes that hydrolyze endocannabinoids. UCM710 augments both N-arachidonoylethanolamine (AEA) and 2-arachidonoylglycerol (2-AG) levels in neurons. UCM710 does not inhibit monoacylglycerol lipase (MAGL).
U6508 UCN-01 ≥97% (HPLC), powder UCN-01 is a selective inhibitor for conventional PKC isotypes over novel PKC isotypes.
SML1799 UCPH-102 ≥98% (HPLC) UCPH-102 is a selective inhibitor of the Excitatory Amino Acid Transporter subtype-1 (EAAT1, GLAST) with an IC50 value of 420 nM for EAAT1 and >300 μM for EAAT2-5. UCPH-102 has been shown to cross the blood-brain barrier, so should become a valuable tool for studying the role of EAAT1 in brain.
SML1431 UF010 ≥98% (HPLC) UF010 is a potent class I HDAC (HDAC1, HDAC2, HDAC3, and HDAC8) selective inhibitor that suppresses cancer cells proliferation through class I HDAC inhibition of oncogenic signaling and activation of tumor suppression pathways.
U5635 UFP-101 trifluoroacetate salt ≥98% (HPLC), powder UFP-101 is a potent antagonist of nociceptin/orphanin FQ receptor; ORL1
U109 R(+)-UH-301 hydrochloride solid R(+)-UH-301 hydrochloride is a potent and selective 5-HT1A serotonin receptor agonist. R(+)-UH-301 is also known to function as an antinociceptive agent, as it has been shown to significantly decrease formalin-induced flinching in rats.
human ... HTR1A(3350)
U104 UK 14,304 UK 14,304 is an α2-adrenoceptor agonist.
human ... ADRA1A(148), ADRA2A(150), ADRA2B(151), ADRA2C(152)
PZ0152 UK-356618 ≥98% (HPLC) UK-356,618 is a potent, selective inhibitor of Matrix metalloproteinase MMP3 (stromelysin-1). MMP-3 IC50 = 5.9 nM, selectivity is 140-fold vs MMP-1, -2, -9, and -14.
PZ0156 UK-383,367 ≥98% (HPLC) UK-383,367 is a procollagen C-proteinase (PCP) inhibitor.
PZ0160 UK-5099 ≥98% (HPLC) UK-5099 is a potent inhibitor of the mitochondrial pyruvate transporter. n rat heart mitochondria, UK-5099 inhibits pyruvate-dependent O2 consumption with an IC50 of 50 nM.
U3885 UK-78282 monohydrochloride ≥98% (HPLC) UK-78282 blocks both Kv1.3 and Kv1.4. Kv1.3 and Kv1.4 are members of the Shaker family of voltage-gated potassium channels. Kv1.3 is expressed in brain and in effector memory T (Tem) cells, and Kv1.4 is expressed in brain. Both channels are involved in setting the membrane potential of neurons. In addition, Kv1.3 maintains the membrane potential for T memory cells and is up-regulated upon T cell activation, contributing to multiple immune processes and disorders. Blockers of Kv1.3 have long been sought for therapeutic benefit, and they are also valuable tools for studying the immune system. Selective blockers of Kv1.4 are desired, as there are few if any currently available. UK-78282 is valuable for immune system studies, where the absence of Kv1.4 makes it functionally selective for Kv1.3, and it has shown suppression of T cell activation. UK-78282 is also valuable for the study of Kv1.4 function.
SML1469 Ulipristal acetate ≥98% (HPLC) Ulipristal acetate is a selective progesterone receptor modulator (SPRM) with tissue-selective partial antagonist activity. It has clinical use both as an emergency contraceptive and as a treatment for uterine fibroids. Ulipristal acetate acts as a partial antagonist on the hypothalamic–pituitary–ovarian axis to inhibit or delay ovulation without affecting human embryo implantation. As a progesterone antagonist, Ulipristal acetate selectively suppresses neo-vascularization, cell proliferation, and survival in uterine fibroid cells, but not in normal myometrial cells.
SML0782   (-)-Umbellulone ≥98% (HPLC) (-)-Umbellulone, isolated from the"headache tree" Umbellularia californica Nutt, is a selective activator of Transient Receptor Potential Anykrin 1 (TRPA1) channels. (-)-Umbellulone activates TRPA1 channels on nociceptive trigeminal afferents, resulting in release of CGRP and CGRP-mediated neurogenic vasodilatation, causing a painful cold sensation and headache/migraine.
SML1492 UMI-77 ≥98% (HPLC) UMI-77 is an inhibitor of Induced myeloid leukemia cell differentiation protein Mcl-1, a member of the Bcl-2 family that inhibits apoptosis. UMI-77 acts by binding to the BH3-binding groove of Mcl-1, blocking the heterodimerization of Mcl-1/Bax and Mcl-1/Bak. UMI-77 is selective for Mcl-1 over other members of the antiapoptotic Bcl-2 family with a Ki of 490 nM. It inhibited cell growth and induced apoptosis in pancreatic cancer cells.
U4885 UNC0638 hydrate ≥98% (HPLC) UNC0638 hydrate is a histone methyltransferase (HMT) inhibitor. UNC0638 shows selectivity for G9a (EHMT2) and GLP (EHMT1) methyltransferases, which catalyze the methylation of lysine 9 of histone 3 (H3K9) as well as other non-histone substrates. For full characterization details, please visit the UNC0638 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML1037 UNC0642 ≥98% (HPLC) UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a (EHMT2) and GLP (EHMT1), which catalyze the mono and dimethylation of lysine 9 of histone 3 (H3K9), and other non-histone substrates such as p53 and WIZ. UNC0642 has an in vitro IC50 <15 nM with greater than 100-fold selectivity over 13 other HMTs and selected representatives of kinases, ion channels, 7TMs, and other epigenetic proteins. UNC0642 has the same potency with improved PK properties relative to UNC0638, which should make it a more useful probe in an in vivo setting. For full characterization details, please visit the UNC0642 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML0633   UNC0646 ≥98% (HPLC) UNC0646 is potent, selective inhibitor of the methyltransferase G9a, which catalyzes lysine-methylation of histones, and nonhistone proteins including p53.
SML0662 UNC1215 ≥98% (HPLC) UNC1215 is a potent, selective antagonist of L3MBTL3 with cellular activity. Lethal (3) malignant brain tumor-like protein 3 (L3MBTL3) is a putative polycomb group (PcG) protein with gene-repressing activity, a member of the MBT family of methyllysine binders. Methyl-lysine binding proteins are a family of proteins that are important epigenetic regulators that “read” the post-translational methylation state of histone lysine residues and modulate protein-protein interactions that regulate gene expression. UNC1215 has an IC50 of 20 nM and > 100-fold selectivity over 13 HMTs and selected representatives of kinases, ion channels, 7TMs, and other epigenetic proteins. UNC1215 showed a significant decrease in FRAP recovery (Fluorescence Recovery After Photobleaching) time below 1 microM in cells using GFP-L3MBTL3. For full characterization details, please visit the UNC1215 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML0778 UNC1999 ≥98% (HPLC) The polycomb repressive complex 2 (PRC2), which represses gene expression through methylation of histone H3 on lysine 27 (H3K27), contains either EZH1 or EZH2 as its catalytic subunit, with EZH1 being found in both dividing and non-dividing cells, whereas EZH2 is only found in actively dividing cells. UNC1999 is an orally bioavaliable selective inhibitor of both EZH2 and EZH1 lysine methyltransferases with IC50 < 10 nM for EZH2 and 45 nM for EZH1. UNC1999 potently inhibited both wild-type and mutant Y641N EZH2 methyltransferase activity with less than a 5-fold difference in potency, and selectively killed diffused large B cell lymphoma (DLBCL) cells bearing Y641 point mutations. It was selective for EZH2 and EZH1 over 15 other lysine, arginine and DNA methyltransferases. UNC1999 is competitive with the cofactor S-adenosylmethionine (SAM) and non-competitive with the peptide substrate. Because it inhibits both EZH2 and EZH1, UNC1999 has potential advantages over EZH2 selective inhibitors in the disease settings where both PRC2 – EZH2 and PRC2 – EZH1 contribute to the methylation of H3K27. For full characterization details, please visit the UNC1999 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML1434 UNC2170 trifluoroacetate ≥98% (HPLC) UNC2170 is an inhibitor of DNA damage response protein 53BP1, which recognizes dimthyl lysine residues on lysine 20 on histone H4 that is involved in double-strand DNA breaks. 17-fold selectivity for 53BP1 as compared to other methyl-lysine (Kme) binding proteins tested.
SML1163 UNC2881 ≥98% (HPLC) UNC2881 is a selective inhbitor of Mer kinase, a member of the TAM (Tyro3, Axl, Mer) receptor tyrosine kinase family. The IC50 values for inhibition of Mer, Axl and Tyro 3 are 4.3, 360 and 250 nM, respectively.
SML0554 UNC926 ≥98% (HPLC) UNC926 is a specific antagonist of the methyl-lysine binding protein L3MBTL1, a member of a protein family that reads the methylation state of histone lysine residues to direct gene expression. UNC926 dose dependently blocks the interaction of recombinant L3MBTL carrying three tandem MBT reader domains (L3MBTL3XMBT) and a methylated histone peptide H4K20me1 with an IC50 of 3.9 μM.
SML1576 Undecylprodigiosin hydrochloride ≥95% (HPLC) New Undecylprodigiosin is a tri-pyrolle antibiotic isolated from Streptomyces coelicolor A3 that exhibits immunosuppressive and apoptotic activities as well as antibacterial, antioxidative and UV protective properties. Undecylprodigiosin selectively induces p53 independent apoptosis in cancer cells.
U5760 (4R)-2-Undecyl-4-thiazolidinecarboxylic acid ≥98% (HPLC) BML-241 is a S1P3 (shingosine-1-phosphate receptor) specific antagonist. Treatment with 10 uM BML-241 results in a 40% inhibition of Ca influx in HeLa cells.
SML1674 UPCDC30245 ≥98% (HPLC) UPCDC30245 is an allosteric inhibitor of AAA ATPase p97, also called valosine containing protein (VCP). p97 is an integral component of the ubiquitin fusion degradation (UFD) pathway. It plays a role in degradation of misfolded proteins, Golgi membrane reassembly, membrane transport, myofibril assembly, autophagosome maturation, and cell division, and is overexpressed in many tumor types. UPCDC30245 has an IC50 value of 27 nM, and has been shown to bind at the junction between the D1 and D2 domains of p97. UPCDC30245 has been used in cryo-ECM to show how such inhibitor binding prevents the confomational changes necessary for p97 function.
U6010 UPF-1069 ≥98% (HPLC), powder UPF-1069 is a PARP inhibitor with modest selectivity for PARP-2 (0.3 uM) over PARP-2 (8.0 uM).
U4760 UR-AK57 dihydrochloride ≥98% (HPLC) Histamine receptors are ubiquitously expressed and activated endogenously by the neurotransmitter histamine. Histamine receptors are GPCRS and have long been therapeutic targets for allergic rhinitis. In brain, histamine receptors are targets for psychotherapeutics.
UR-AK57 is known to function as an effective, partial histamine H1-receptor (H1R) and H2-receptor (H2R) agonist.
U100 Urapidil hydrochloride solid α1-adrenoceptor antagonist; 5-HT1A serotonin receptor partial agonist; anti-hypertensive.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), HTR1A(3350)
U4133 URB597 ≥98% (HPLC), powder Potent, selective fatty acid amide hydrolase (FAAH) inhibitor.
U3010 URB602 ≥98% (HPLC) URB602 is an inhibitor of monoacylglycerol lipase (MGL). The IC50 = 28 μM and Km = 20 μM. URB602 increases 2-arachidonoylglycerol (2-AG) concentrations. When URB602 is injected into the periaqueductal grey matter, it enhances stress-induced analgesia (tail-flick test) in a CB1-dependent manner. An effect that is prevented by a CB1 cannabinoid receptor antagonist, Rimonabant (SR141716). URB602 is not suitable for systemic administration due to relatively low potency, but useful for research of pain and stress-related disorders, which identifies MGL as a previously unrecognized therapeutic target (highlighted in Chemical Engineering News, June 27, 2005).
SML0448   URB937 ≥95% (HPLC) URB937 is a fatty acid amide hydrolase (FAAH) inhibitor that is actively excluded from the CNS by the membrane transporter ABCG2. The ED50 for inhibition of FAAH activity in the brain is 200 times higher than inhibition of renal FAAH activity. In vivo administration of URB937 elevates anandamide levels in peripheral tissues, and attenuates acetic acid-induced writhing, hyperalgesia in a sciatic nerve ligation model, and pain and edema in carrageenan injected paws.
U4125 Uridine 5′-(trihydrogen diphosphate) sodium salt from Saccharomyces cerevisiae 95-100% P2Y receptor agonist.
human ... LPAR4(2846), LTB4R(1241), P2RY1(5028), P2RY10(27334), P2RY11(5032), P2RY12(64805), P2RY13(53829), P2RY14(9934), P2RY2(5029), P2RY4(5030), P2RY5(10161), P2RY6(5031), P2RY8(286530)
U6875 Uridine 5′-triphosphate tris salt Type VI, ≥90% P2Y receptor agonist.
U6625 Uridine 5′-triphosphate trisodium salt hydrate from yeast, Type III, ≥96% P2Y receptor agonist.
U6750 Uridine 5′-triphosphate trisodium salt hydrate Type IV, 90-95% P2Y receptor agonist.
U6883 cis-Urocanic acid ≥98% (HPLC), solid (fluffy) cis-Urocanic acid, a 5-HT agonist, is a product of uv isomerization of trans-urocanic acid in skin, which leads to immunosuppression via activation of 5-HT2A receptor.
SML1791 Urolithin A ≥97% (HPLC) Urolithin A is a natural product with antiproliferative and antioxidant activity. Urolithin A is formed by metabolism from polyphenols found in some nuts and fruits, particularly pomegranates. Urolithin A has been shown to cross the blood brain barrier, and may have neuroprotective effects against Alzheimer’s Disease.
SML1649 Urolithin B ≥95% (HPLC) Urolithin B is a natural product with antiproliferative and antioxidant activity. Urolithin B is formed by metabolism from polyphenols found in some nuts and fruits, particularly pomegranates. Urolithin B has been shown to cross the blood brain barrier, and may have neuroprotective effects against Alzheimer’s Disease.