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SML2437 H-151 ≥98% (HPLC) H-151 is an irreversible antagonist of the stimulator of interferon genes (STING) protein, a central signalling component of the cytosolic DNA sensing pathway. Although STING is a vital component of the innate immune pathways, it has also been shown to have a pathogenic role in some inflammatory diseases. H-151 is a potent and selective STING antagonist with inhibitory activity both in human cells and in vivo in mice. Given as a pretreatment, H-151 was shown to attenuate pathological features of autoinflammatory disease in mouse models, reducing systemic cytokine responses in mice treated with the STING agonist 10-carboxymethyl-9-acridanone (CMA)
I6891 H-7 Inhibitor of cyclic nucleotide dependent protein kinase (PKA) and protein kinase C.
human ... CALCRL(10203)
rat ... Calcrl(25029)
I7016 H-7 dihydrochloride ≥98% (HPLC) Inhibitor of cyclic nucleotide dependent protein kinase (PKA) and protein kinase C.
human ... PRKCA(5578), PRKCB(5579), PRKCD(5580), PRKCE(5581), PRKCG(5582), PRKCH(5583), PRKCI(5584)
M9656 H-8 dihydrochloride >98% (HPLC) cAMP and cGMP-dependent protein kinase inhibitor.
human ... CALCRL(10203), PRKAR1A(5573), PRKAR1AP(5574), PRKAR1B(5575), PRKAR2A(5576), PRKAR2B(5577)
rat ... Calcrl(25029)
B1427 H-89 dihydrochloride hydrate ≥98% (HPLC), powder H-89 dihydrochloride hydrate is a selective inhibitor of protein kinase A (PKA). It also inhibits potassium (K+) current in rat myocytes. It mediates Na+ transport by interacting with α subunits of epithelial Na+ channel (ENaC).
Selective, potent inhibitor of cAMP-dependent protein kinase.
human ... PRKAR1A(5573), PRKAR1AP(5574), PRKAR1B(5575), PRKAR2A(5576), PRKAR2B(5577)
SML0989   H2L5186303 ≥98% (HPLC) H2L5186303 is specific antagonist of the lysophosphatidic acid receptor LPA2 (Ki = 7.2 nM). The compound H2L5186303 displays 40- to 1800-fold selectivity over other LPA receptors.
H139 HA-1077 dihydrochloride solid, ≥98% (HPLC) HA-1077/fasudil, is a Rho kinase inhibitor. This ROCK inhibitor has the ability to increase cognitive deficits in animals, that have Alzheimer′s disease (AD). In humans, fasudil possesses high therapeutic effects against cerebral vasospasm after subarachnoid hemorrhage (SAH). HA-1077 also acts as an inhibitor of protein kinases, like myosin light chain kinase and Rho associated kinase. Hence, it can block myosin phosphorylation.
Novel vasodilator agent which inhibits vascular smooth muscle contraction by acting as an intracellular Ca2+ antagonist.
SML2118 HA15 ≥98% (HPLC) HA15 is a selective ligand of BiP/GRP78/HSPA5 chaperone that increases ER stress, leading to autophagic and apoptotic cell death in varies cancer cell lines including melanoma cells. HA15 inhibits inhibit the ATPase activity of BiP. HA15 inhibits tumor development in mice injected with A375 melanoma cells.
SML0914   HA155 ≥98% (HPLC) HA155 is a potent and selective autotaxin inhibitor, which potently blocks thrombin-induced lysophosphatidic acid (LPA) secretion in platelets.
H130 R(+)-HA-966 solid Antagonist of the strychnine-insensitive glycine modulatory site associated with the NMDA receptor. More active enantiomer of (±)-HA-966.
H9414 Halofantrine hydrochloride ≥98% (HPLC), solid Halofantrine is a blocker of delayed rectifier potassium current via the inhibition of hERG channel.
H3041 Halopemide ≥98% (HPLC) Halopemide is a dopamine receptor antagonist and a phospholipase D2 inhibitor. Halopemide may be used as a screen to identify inhibitors of human PLD2 using an in vitro biochemical assay. It is also inhibitory at benzodiazepine binding sites.
H1512 Haloperidol powder Haloperidol is a butyrophenone antipsychotic. It is also classified as a neuroleptic (powerful tranquilizer). Haloperidol acts as a D2, D3, and D4 dopamine receptor antagonist and thus causes Parkinson′s disorder. It also has a negative effect on the central nervous system.
human ... ABCB1(5243), ADRA1A(148), ADRA2A(150), ADRA2C(152), CHRM1(1128), DRD2(1813), DRD3(1814), DRD4(1815), EBP(10682), HRH1(3269), HTR2A(3356), HTR2C(3358), HTR7(3363), KCNH1(3756), KCNH2(3757), PRNP(5621)
rat ... Adra1a(29412), Adra2a(25083), Chrm1(25229), Chrm2(81645), Drd1a(24316), Drd2(24318), Drd3(29238), Drd4(25432), Hrh1(24448), Htr1a(24473), Htr1b(25075), Htr2a(29595), Htr2c(25187), Oprs1(29336), Slc6a3(24898), Slc6a4(25553)
SML1234   HAMNO ≥98% (HPLC) HAMNO is a potent and selective inhibitor of replication protein A (RPA) interactions with proteins involved in the replication stress response. HAMNO binds the N-terminal domain of RPA70 and inhibits both ATR autophosphorylation and phosphorylation of RPA32 Ser33 by ATR. HAMNO enhances DNA replication stress in cancer cells and slow tumor growth in vivo.
SML0456 HBB2 ≥98% (HPLC) HBB2 is an inducer of the KEAP1/NRF2/ARE pathway that reacts with sulfhydryl groups. Also, HBB2 upregulates Hsp70 in an HSF1-dependent manner. It appears that HBB2 reacts with cysteine residues of KEAP1, which leads to activation of NRF2, and binds to Hsp90 Cys that leads to activation of HST1.
SML2289 HBT1 HBT1 is an AMPA-R [alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptor] potentiator that induces production of brain-derived neurotrophic factor (BDNF) and exhibits little agonistic effect in primary neurons. HBT1 binds to ligand-binding domain of AMPA-R in glutamate dependent manner.
H4415 HC-030031 ≥98% (HPLC), powder HC-030031 is a selective TRPA1 channel blocker, antagonizing formalin-evoked calcium influx and formalin-induced pain. IC50 is 5 μM. TRPA1 antagonism is a promising therapeutic target for chronic inflammatory or neurogenic pain.
HC-030031 is a selective TRPA1 channel blocker. HC-030031 antagonizes formalin-evoked calcium influx. IC50 is 5 μM.
SML0143 HC-067047 ≥98% (HPLC) HC-067047 is a potent, selective inhibitor of hTRPV4. The compound inhibits human, rat and mouse TRPV4 with IC50 values of 48, 133 and 17 nM, respectively. HC-067047 does not inhibit other TRPV isoforms at concentrations up to 5 μM. HC-067047 inhibits hERG channel and the menthol receptor TRPM8 with IC50 values of 370 and 780 nM, respectively.
H7270 HC toxin from Helminthosporium carbonum lyophilized powder Cyclic tetrapeptide fungal toxin selectively toxic to plants with susceptible host genotype.
E8656   Heat-Labile Enterotoxin, B subunit (LTB) from E. coli recombinant, expressed in Pichia pastoris, >90% (SDS-PAGE), lyophilized powder Enterotoxigenic Escherichia coli causes diarrhea through its heat-labile enterotoxin (LT). The LT is a periplasmic protein composed of one A subunit (LTA, 27 kDa) and five non-covalently associated B subunits (LTB, 11.6 kDa each) forming a ring-like pentamer. LTB has high affinity towards the toxin receptor ganglioside GM1, a glycosphingolipid found ubiquitously on the surface of mammalian cells. Ganglioside GM1 facilitates the delivery of the A subunit to the cytosol of the target cell resulting in persistent synthesis of cAMP and subsequently diarrhea. This characteristic makes LTB a good label for microglial cells (due to the enrichment of ganglioside GM1 on their cell surface). In addition, studies made mostly with animal models demonstrated that recombinant LTB could stimulate strong serum and mucosal immune responses against LT. Other studies have indicated that LTB could be used as a potent mucosal adjuvant.
SML1396 Heclin ≥98% (HPLC) Heclin is a selective reversible inihbitor of HECT E3 ubiquitin ligases. Heclin inhibited Nedd4, Smurf2 and WWP1 with IC50 values of 6.3 μM, 6.8 μM and 6.9 μM, respectively, and inhibited autoubiquitination of the Smurf2 HECT domain in vivo with an IC50 value of 9 μM. Heclin had no effect on the auto-ubiquitination of the RING domain ligase Mdm2.
Heclin is not effective in inhibiting E1 or E2 proteins.
F5551   Hemagglutinin, Filamentous from Bordetella pertussis lyophilized powder    
H108 Hemicholinium-3 solid, ≥95% (HPLC) Hemicholinium-3 plays a role in blocking the neuronal choline uptake thereby inhibiting acetylcholine synthesis in the brain.
H3042 Hemopressin trifluoroacetate salt ≥98% (HPLC), powder Hemopressin is an endogenous hypotensive nonapeptide derived from hemoglobin. Hemopressin reduces appetite, acting as a cannabinoid CB1 inverse agonist. It blocks signaling by CB(1) receptors but not by other members of family A G protein-coupled receptors (including the closely related CB(2) receptors.
H7640   Heparan sulfate sodium salt from bovine kidney Constituent of membrane-associated proteoglycans suggested to contribute to cell-cell adhesion
Heparan sulphate (HS), a ubiquitous glycosaminoglycan, is a polymer of D-glucuronic acid or L-iduronic acid and D-glucosamine (GlcA) sugars. It is synthesized in the cis-Golgi as heparan. In Golgi, final heparan sulphate is synthesized in by the action of enzymes N- and O-HS-sulphotransferases and HS epimerase. The mature HS has 50 to 200 disaccharide units. It is part of the extracellular matrix (ECM) and plays a key role in the oncogenic pathway. Deregulation of heparin sulfate metabolism is implicated in cancer progression. HS is associated with the onset of infectious diseases and inflammatory conditions. HS interaction with Aβ fibrils contributes to the pathophysiology of Alzheimer′s disease.
SML1118   Hepcidin-25 (human) trifluoroacetate salt ≥95% (HPLC) Hepcidin is the master regulator of iron homeostasis. Hepcidin is found in liver, but also widely distributed in brain, where it may play a role in preventing iron-related neurodegeneration. Hepcidin has anti-inflammatory and antimicrobial activity.
Hepcidin-25 is the major isoform of hepcidin. hepcidin‐25 with reticulocyte hemoglobin content (CHr) in the hepcidin‐25 plot helps to differentiate DA can be differentiated iron‐deficient anemia (IDA) from the anemia of chronic disease (ACD) and the combined state of ACD/IDA. Mutation in the hepcidin gene is associated with the development of severe juvenile hemochromatosis.
H6649 Herbimycin A from Streptomyces hygroscopicus ≥95% (HPLC), powder An antibiotic that inhibits protein tyrosine kinase. Herbimycin A is a potent inhibitor of angiogenesis.
Herbimycin A is an inducer of heat shock protein (HSP). It increases HSP expression resulting in the attenuation of ischemia reperfusion induced pulmonary injury.
SML2416 HET0016 ≥95% (HPLC) HET0016 is a potent and selective inhibitor against cytochrome P450 (CYP450) ω-hydroxylases (human CYP4A11/4A22/4F2/4F3, rat CYP4A1/4A2/4A3/4A8)-mediated 20-hydroxyeicosatetraenoic acid (20-HETE) biosynthesis (IC50 = 8.9/35 nM using human/rat renal microsomes), exhibiting much reduced potency against epoxyeicosatrienoic acids (EETs) biosynthesis (IC50 = 2.8 μM/rat microsome) or the enzyme activities of CYP2C9/2D6/3A4 and COX (IC50 = 3.3/83.9/71 μM and 2.3 μM). HET0016 is widely employed both in cultures (1-10 μM) and in aminals in vivo (1-10 mg/kg via i.v., i.m., i.p. or s.c.) for probing 20-HETE-dependent physiological and pathological processes.
SML0455 1,2,3,4,5,6-Hexabromocyclohexane ≥98% (HPLC) 1,2,3,4,5,6-hexabromocyclohexane binds directly to a pocket within the kinase domain of JAK2 and inhibits autophosphorylation. The compound also blocks growth hormone induced JAK2 autophosphorylation without affecting EFGR autophosphorylation.
H0879 Hexamethonium bromide Preferentially blocks nicotinic receptors at autonomic ganglia; crosses blood-brain barrier only at high doses.
human ... CHRNA1(1134), CHRNA10(57053), CHRNA2(1135), CHRNA3(1136), CHRNA4(1137), CHRNA5(1138), CHRNA6(8973), CHRNA7(1139), CHRNA9(55584), CHRNB1(1140), CHRNB2(1141), CHRNB3(1142), CHRNB4(1143)
H2138   Hexamethonium chloride solid (hygroscopic) Hexamethonium chloride preferentially blocks nicotinic receptors at autonomic ganglia, crosses blood-brain barrier only at high doses. Nicotinic acetylcholine receptor (nAChR) is responsible for cognitive functions. Blocking this receptor results in cognitive impairment. nAChR antagonist is used to study the effect of loss of receptor function. Hexamethonium has a peripheral action over blocking the nAChR.
human ... CHRNA1(1134), CHRNA10(57053), CHRNA2(1135), CHRNA3(1136), CHRNA4(1137), CHRNA5(1138), CHRNA6(8973), CHRNA7(1139), CHRNA9(55584), CHRNB1(1140), CHRNB2(1141), CHRNB3(1142), CHRNB4(1143)
A9561 5-(N,N-Hexamethylene)amiloride Inhibitor of Na+/H+ antiport.
human ... SCNN1A(6337), SCNN1B(6338), SCNN1D(6339), SCNN1G(6340), SLC9A1(6548), SLC9A5(6553)
mouse ... Scnn1a(20276), Scnn1b(20277), Scnn1d(140501), Scnn1g(20278)
rat ... Scnn1a(25122), Scnn1b(24767), Scnn1g(24768), Slc9a1(24782), Slc9a3(24784)
SML1637 Hexaminolevulinate hydrochloride ≥98% (HPLC) Hexaminolevulinate (HAL) hydrochloride is a hexyl ester of 5-Aminolevulinic acid (ALA), a precursor to porphyrins including the photosensitizer protoporphyrin IX (PPIX). Hexaminolevulinate is more lipophilic than ALA, and is 50–100 times more efficient than ALA at inducing PpIX, which accumulates preferentially in neoplastic cells. Hexaminolevulinate administration followed by light activation has been used for fluorescence cystoscopy to enhance detection of bladder cancer, in particular carcinoma in situ (CIS). Hexaminolevulinate is also being studied for use in cancer photodynamic therapy. Hexaminolevulinate followed by irradiation produced DNA oxidative damage and apoptosis.
H6524 N-Hexanoyl-D-sphingosine ≥98% (TLC), synthetic Cell-permeable analog of ceramide; stimulates protein phosphatase 2A; activates MAP kinase; induces apoptosis in human leukemia HL-60 cells
H2036 Rp-8-Hexylaminoadenosine 3′,5′-monophosphorothioate ≥99% (HPLC), solid Membrane permeable metabolically stable inhibitor of cAMP-dependent protein kinases
SML0747   HHQ ≥98% (HPLC) HHQ or 2-Heptyl-4-quinolone is a modulator of swarm motility. HHQ can be converted to PQS (Pseudomonas quinolone signal) by the PqsH protein.
HHQ stimulates vesicle formation but not as much as PQS.
SML0224 HI-6 ≥98% (HPLC) HI-6 is an efficient oxime cholinesterase reactivator that is used as an antidote for organophosphates (Ops) exposure.
SML0883   HIF-2 Antagonist 2 ≥98% (HPLC) Hypoxia inducible transcription factors (HIF) control gene expression when oxygen availability is low and are associated with the onset and progression of a variety of cancers. They are heterodimers of an HIF-α (HIF-1α, HIF-2α also known as EPAS-1, or HIF-3α) and aryl hydrocarbon receptor nuclear translocator (ARNT, also known as HIF-β). N-(3-Chloro-5-fluoropheny  
SML2313 Higenamine hydrochloride ≥95% (HPLC) Higenamine is an anti-inflammatory agent that protects cells from oxidant injury. Higenamine is a pharmacological modulator of heme oxygenase 1(HO-1). It also displays agonist activity at adrenergic β2 receptor.
H5257 Hispidin solid, ≥98% (HPLC) Hispidin exhibits robust antioxidant, anticancer and antidiabetic properties. It has the ability to guard against peroxynitrite-mediated cytotoxicity, DNA damage and the development of hydroxyl radicals.
Potent inhibitor of protein kinase Cβ, cytotoxic for cancer cells.
human ... PRKACB(5567), PRKAR2B(5577), PRKCB(5579)
SML0582 Hispidulin ≥98% (HPLC) Hispidulin also exhibits antiosteoporotic anti-atheromatous, antispasmodic and anticancer functionality. It exhibits inhibition on α-glucosidase enzymatic activity. Hispidulin inhibits platelet aggregation and is more effective than theophylline. It also acts as a modulator of the γ-aminobutyric acid receptor (GABA) and blocks the release of glutamate synaptosomes associated with cortical neurons.
Hispidulin is a bioactive flavonoid with a variety of effects including antiproliferative, antifungal, anti-inflammatory, antioxidative and antiepileptic activity. Like EGCG, hispidulin appears to activate AMPK and inhibit the PI3K/Akt/mTOR pathway. The antiepileptic activity may be due to additional activity as a benzodiazepine (BZD) receptor ligand.
H7125 Histamine ≥97.0% Endogenous H1 and H2 histamine receptor agonist; H1 activation mobilizes Ca2+; H2 activation stimulates adenylate cyclase activity in neurons; activates nitric oxide synthetase; potent vasodilator.
Histamine participates in innate and acquired immune response, mediating allergy and inflammation. It helps in intestinal muscle contraction. During anaphylactic shock histamine causes bronchial constriction. Histamine is also involved in gastric acid secretion, epithelial and endothelial barrier control.
human ... CA1(759), CA2(760), HRH1(3269), HRH2(3274), HRH3(11255), HRH4(59340)
rat ... Hrh1(24448), Hrh3(85268)
H7250 Histamine dihydrochloride ≥99% (TLC), powder   human ... HRH1(3269), HRH2(3274)
53300 Histamine dihydrochloride ≥99.0% (AT) Histamine dihydrochloride has been shown to activate nitric oxide synthetase and suppress or inhibit the generation of reactive oxygen species (ROS). Inhibition of ROS by histamine dihydrochloride allows activation of T cells and NK cells by IL-2. In a rat model, histamine dihydrochloride suppressed ROS generated by Kupffer cells through the H2 histamine receptor.
human ... HRH1(3269)
H7375 Histamine bisphosphate monohydrate    
53370 L-Histidine monohydrochloride monohydrate ≥99.0% (AT) L-Histidine is biosynthesized from ATP, 5-phosphoribosyl-1-pyrophosphate (PRPP), and glutamine. This essential amino acid can be degraded to glutamate by histidiase, urocanase and imidazolonepropionase; it is also the precursor of histamine by action of histidine decarboxylase.
SML0796   HI-TOPK-032 ≥98% (HPLC) HI-TOPK-032 belongs to the class of ATP-competitive inhibitors. It can also be used as a potent therapeutic for colorectal cancer.
HI-TOPK-032 is a specific TOPK (T-LAK cell–originated protein kinase) inhibitor both in vitro and in vivo. HI-TOPK-032 suppressed tumor growth in a colon cancer xenograft model.
SML1562   HIV inhibitor 18A ≥98% (HPLC) HIV inhibitor 18A is a broad spectrum viral fusion and viral entry inhibitor. HIV entry requires several steps in sequence starting with HIV surface glycoprotein gp120 binding to the CD4 receptor followed by a conformational change in gp120, exposing a second recognition site that binds the co-receptor C-C chemokine receptor (CCR5) on the host cell, eventually resulting in the fusion of HIV and the T cell membranes, allowing entry of the viral core into the cell. HIV inhibitor 18A prevents the surface envelope glycoprotein from fusing with host cells by blocking envelope glycoprotein transitions critical for entry rather than interfering with CD4 or CCR5 binding.
H5410   HIV Protease Substrate V >98% (HPLC) Substrate for HIV protease
SML0820   HJC0350 ≥98% (HPLC) HJC0350 is a potent inhibitor of the Exchange Protein directly Activated by cAMP (EPAC) family member EPAC2. HJC0350 blocks EPAC2 in enzymatic and cell-based assays, with no detectable acitivity against EPAC1, or protein kinase A (PKA).
SML1260 HLM006474 ≥98% (HPLC) HLM006474 activates p53 and induces DNA damage and apoptosis in mouse tumor models.
HLM006474 is a pan-E2F transcription factor inhibitor. E2F s part of the CDK/Rb/E2F pathway. When phosphorylated by CDKs, the tumor suppressor retinoblastoma protein (Rb) is inactivated, releasing E2Fs and allowing cell cycle progression. HLM006474 inhibited DNA-binding of all E2F complexes and down-regulated expression of E2F4 protein. HLM006474 induced apoptosis of A375 melanoma cells and synergized with paclitaxel in lung cancer cell lines.
SML0833   HLY78 ≥98% (HPLC) HLY78 is an activator of the Wnt/β-Catenin signaling pathway. HLY78 acts upstream of β-catenin synergistically with Wnt. It is believed to bind at a cavity at the dimeric interface of the Axin DIX domain, causing a conformational change of Axin to an active state, potentiating Axin–LRP6 association and promoting Wnt signaling transduction. There are several Wnt inhibitors used to study their potential in cancer therapy but few small molecules that activate the Wnt pathway. In Zebrafish, HLY78 increased the expression of the hematopoietic stem cell (HSC) transcription factors runx1 and cmyb, showing that it might be useful in HSC expansion, which could be important in transplantation and recovery after injury.
H4663 HMBA ≥98% (HPLC), solid HMBA is an Inhibitor of microtubule polymerization; apoptosis inducer.
SML2767 HMR-1098 ≥98% (HPLC) HMR-1098 is a potent and selective blocker of the sarcolemmal ATP-sensitive K+ (sarcKATP) channel. HMR 1098 is inhibits Kir6.2/SUR1-composed KATP channels.
SML2354 HMR-1556 ≥98% (HPLC) HMR-1556 is a potent and selective blocker of the heteromeric KCNQ1-KCNE1 (KvLQT1-MinK) voltage-gated channel-mediated slowly activating K+ current (IKs IC50 = 120 nM in hKCNE1-transfected Xenopus oocytes; little or no inhibition of Herg, Kv1.3 (KCNA3), Kv1.5 (KCNA5), Kir2.1 (KCNJ2), HCN2 (BCNG2) current in respective oocyte transfectants). HMR-1556 is more potent than chromanol 293B (IKs IC50 = 34 nM and 2.1 μM, respectively; guinea pig ventricular myocytes), being inefficient against L-type Ca2+ channel or rapidly delayed & inward rectifier currents (IKr & IK1) in guinea pig ventricular myocytes, nor transient & sustained outward currents, I(to) & I(sus), in rat ventricular myocytes.
H9538 HNE-DMA hexane solution, ≥85% (GC) Stable form of HNE; toxic second messenger of free radicals.
SML0503 9(S)-HODE ≥98% (HPLC) 9(S)-HODE is produced by the lipoxygenation of linoleic acid. It is a major component of plasma oxidized low-density lipoprotein. 9-HODE has been shown to stimulate cell proliferation and and extracellular matrix synthesis in human mesangial cells via PPARgamma. Pro-inflammatory effects of 9-HODE, acting through the receptor GPR132, can contribute to atherosclerosis progression. 9-HODE has also been shown to activate spinal TRPV1, leading to inflammatory hyperalgesia.
H1267 22(S),23(S)-Homobrassinolide 22(S),23(S)-Homobrassinolide is a brassinosteroid. It might play a role in the control of plant embryogenesis.
SML1091 Homoharringtonine ≥98% (HPLC) Homoharringtonine (Omacetaxine mepesuccinate) is a translation elongation inhibitor, a cytotoxic alkaloid originally isolated from the evergreen tree, Cephalotaxus hainanensis. Homoharringtonine binds to the 80S ribosome in eukaryotic cells and inhibits protein synthesis by interfering with chain elongation. Homoharringtonine blocks progression of leukemic cells from G1 phase into S phase and from G2 phase into M phase. Homoharringtonine (Omacetaxine mepesuccinate) was approved in October 2012 (Synribo) for the treatment of adult patients with Chronic Myelogenous Leukemia (CML) with resistance and/or intolerance to two or more tyrosine kinase inhibitors.
Homoharringtonine is a cephalotaxine ester that is also known as (HHT; 4-methyl (2R)-2-hydroxy-2-(4-hydroxy-4-methylpentyl)butanedioate). In gefitinib-resistant lung cancer cells, homoharringtonine promotes apoptosis and prevents signal transducer and activator of transcription 3 (STAT3) through IL-6 (interleukin-6) /JAK1 (janus kinase 1)/STAT3 signal pathway. It plays an important role in the treatment of malaria.
SML2157 Homoplantaginin ≥98% (HPLC) Homoplantaginin is and anti-inflammatory and antioxidant flavonoid isolated from medical herb Salvia plebeian (Sage weed) that improves hepatic injury, hyperlipidemia, and hyperglycemia. Homoplantaginin ameliorates endothelial insulin resistance by inhibiting inflammation and modulating cell signalling via the IKKβ/IRS-1/pAkt/peNOS pathway. Homoplantaginin protects endothelial cells from Palmitic acid -induced inflammation by suppression of TLR4 expression, and NLRP3 inflammasome activation.
H4914 Honokiol ≥98% (HPLC), powder Honokiol is a natural biphenyl neolignan from magnolia extract. It is antiangiogenic, antitumor, and anxiolytic.
SML2894 HPA-12 ≥98% (HPLC) (1R,3S)-HPA-12 is a ceramide (Cer) analog that acts as a Cer transporter (CERT) antagonist and selectively inhibits cellular Cer conversion to sphingomyelin (SM), but not to glucosylceramide, by blocking CERT-mediated Cer ER-to-Golgi transport. Common culture dosing range: 1-10 μM.
SML1696 HPB ≥98% (HPLC) HPB is a cell-permeable, non-cytotoxic N-hydroxybenzamide derivative that acts as a HDAC6-selective deacetylase inhibitor (IC50 = 31/376/677/842/1133 nM against HDAC6/8/10/1/7, >2 μM against HDAC2/3/4/11/9/5). HPB treatment results in reduced growth, but not viability (up to 64 μM and 72 hrs), of LNCaP prostate cancer cells and non-cancer human foreskin fibroblasts (IC50 = 8 and 16-32 μM, respectively), causing upregulated acetylation levels of alpha-tubulin and peroxiredoxin, but not histones, both in cultures and in mice in vivo. Intraperitoneal injection is efficacious in suppressing the expansion of prostate cancer CWR22 xenograft-derived tumors in mice (by 73% in 4 wks; Five daily 300 mg/kg i.p. dosings a week) without detectable weight loss.
H1542 HPI-1 hydrate HPI-1 is a Hedgehog pathway inhibitor; Gli1/Gli2 inhibitor.
H4541 HPI-4 ≥98% (HPLC) HPI-4 is a Hedgehog pathway inhibitor; ciliogenesis inhibitor. The Hedgehog (HH) signaling pathway is targeted for anti-cancer therapeutics. A key signaling molecule in HH pathway, Smoothened (Smo), has been the target of pharmacological intervention, which has resulted in multiple Smo antagonists including Cyclopamine. However, the oncogenic form of Smo is resistant to Cyclopamine, so the identification of inhibitors of downstream effectors, such as the transcription factors Gli1 and Gli2, is important. Four small molecules were identified to inhibit HH downstream of Smo, HPI-1, HPI-2, HPI-3, and HPI-4. HPI-4 blocked HH pathway activation by SAG, decreased Smo ciliary accumulation, decreased HH activity in a consitutively active HH cell line, and decreased Gli1 and Gli2, processing, and stability. HPI-4 inhibited proliferation of cerebellar granula neuron precursor cells, an important model of HH signaling. Cilia in HPI-4-treated cells were either truncated or absent. The mechanism of action of HPI-4 is hypothesized to be directly through perturbation of ciliogenesis, leading to disruption of Gli1/Gli2 activity, which is distinctly different from that of Cyclopamine.
SML2163 HPN-07 ≥98% (HPLC) Originally characterized for its NO-mimicking activity in preventing peroxynitrite formation and in vivo neuroprotective efficacy in animal models of cerebral ischemia (100 mg/kg i.v. in rabbits; 30-60 mg/kg plus 30-60 mg/kg/h i.v. or 50 mg/kg plus 8.8 mg/kg/h s.c. in rats; 28 mg/kg plus 16 mg/kg/h i.v. in monkeys), OKN-007 (HPN-07, NXY-059) is an orally available α-phenyl-tert-butylnitrone (PBN) derivative that is also shown to exhibit sulfatase 2 (SULF2) inhibitory activity and anticancer efficacy both in cultures (effective conc. 170-200 μM in Huh7 heptoma cultures) and in several rodent glioma models in vivo (C6, RG2, and GL261; 75 mg/kg/day for rats and 168 mg/kg/day for mice via drinking water).
SML0906   HPOB ≥98% (HPLC) HPOB is a very potent, selective inhibitor of HDAC6. HPOB inhibits proliferation of normal and transformed cell lines but does not induce cell death. The compound HPOB potentiates the effects of DNA-damaging cytotoxic anti-cancer drugs.
H9415 5HPP-33 ≥98% (HPLC), solid 5HPP-33 is a thalidomide derivative which was reported to be active as anticancer agent through stabilization of the microtubules. 5HPP-33 has shown inhibition of cell proliferation of both estrogen-dependent (MCF-7) and estrogen-independent (MDA-MB-231) breast cancer cells as well as other cell lines. A study in tubulin forming assay reported that 5HPP-33 acts as a microtubule formation inhibitor (IC50=810 nM).
SML0857   HQL 79 ≥98% (HPLC) HQL-79 is a selective inhibtor of hematopoietic prostaglandin D (PGD) synthase, one of two synthases involved in the production of Prostaglandin D2 (PGD2) from arachidonic acid. PGD2 is a lipid signaling molecule, which activates two receptors, DP1 involved in centrally mediated processes such as sleep and pain and DP2 involved and inflammation. The two PGD synthases involved in its synthesis are lipocalin-type (L-PGDS) and hematopoietic (H-PDGS), which acts to form PGD2 in mast cells, Th2 cells, microglia, and other inflammatory cells/tissues. HQL-79 selectively inhibited the activity of recombinant H-PGDS with an IC50 of 6 μM and had almost no effect on COX-1, COX-2, m-PGES, or L-PGDS up to 300 μM. HQL-79 has anti-inflammatory activity in vitro and in vivo.
SML1325   HS-72 ≥98% (HPLC) HS-72 is a cell permeable, highly selective allosteric inhibitor of inducible Hsp70 (Hsp70i) over constitutively active Hsc70. HS-72 inhibits cancer cell proliferation and promotes a survival in a HER2+ mouse model of breast cancer.
HS-72 is also termed as ((S)-N-(1-propyl-1H-benzo[d]imidazol-2-yl)-1-(pyrazin-2-yl)piperidine-3-carboxamide). It is considered as a powerful anti-dengue virus (DENV) therapeutic agent. It displays anti-DENV activity in monocyte and liver cell lines. HS-72 stimulates the accumulation of cellular proteins.
SML0929   HS38 ≥95% (HPLC) HS38 is a potent and selective ATP-competitive inhibitor of Death-associated protein kinases DAPK1 (IC50 = 200 nM, 89% inhibition at 10 RM) and ZIPK (Zipper-interacting protein kinase, also called DAPK3) that regulate programmed cell death, and also inhibits the closely related PIM3 kinase (IC50 = 200 nM, 76% inhibition at 10 RM). In addition to mediating apoptosis, DAPK1 and ZIPK regulate both non-muscle and smooth muscle myosin phosphorylation. HS38 specifically targeted ZIPK in smooth muscle, and decreased contractile force generated in mouse aorta, rabbit ileum, and calyculin A stimulated arterial muscle.
SML2474 HS56 ≥98% (HPLC) HS56 is a highly selective and potent dual Pim/DAPK3 inhibitor that significantly reduces contractile intensity and phosphorylation levels of myosin light chain (LC20) in rat caudal arterial smooth muscle strips. HS56 decreases blood pressure in spontaneously hypertensive mice without affecting heart rate.
SML0251 anti-HS peptide trifluoroacetate salt ≥98% (HPLC) LRSRTKIIRIRH is an anti-HS peptide that binds specifically to heparan sulfate (HS) and prevents HSV-1 infection in vivo and in cell culture. It also prevents entry of of various HSV-1 strains. LRSRTKIIRIRH exhibits protective effects against HSV-1 infection of the mouse cornea.
H0167 HT1171 ≥98% (HPLC) Selective inhibitor of mycobacterial proteosomes; 1000-fold selective for mycobacterial proteosomes over human proteosomes.
SML1446 HTH-01-015 ≥98% (HPLC) HTH-01-015 is a potent and selective inhibitor of NUAK1 kinase, a member of the AMPK family that are that are activated by the LKB1 (liver kinaseB1) tumour suppressor kinase and involved in development and proliferation. HTH-01-015 has an IC50 of 100 nM for NUAK1, >100-fold higher than NUAK2, and has no significant inhibition of 139 other kinases tested, including ten AMPK-related kinase family members. Treatment with HTH-01-015 was found to suppress proliferation, restricting cells from entering into mitosis.
SML2374 HTS01037 ≥98% (HPLC) HTS01037 is a selective, high-affinity fatty acid-binding protein FABP4 (AFABP; aP2) antagonist (aP2 Ki = 0.67 μM; EFABP/HF/IFABP/LFABP Ki = 3.40/9.07/6.57/8.17 μM) that targets aP2 long-chain fatty acid-binding site. HTS01037 is shown to downregulate basal and fatty acid-stimulated LTC4 levels in primary murine peritoneal macrophages (0.2-20 μM), upregulate murine macrophage RAW 264.7 intracellular free fatty acids and uncoupling protein 2 (UCP2) mRNA levels (30 μM), as well as suppress PPARγ target genes expression in IL-4 polarized human primary macrophages (10-25 μM).
H7909 HU-210 solid (air sensitive) Cannabinoid receptor agonist.
human ... CNR1(1268), CNR2(1269)
rat ... Cnr1(25248)
SML2899   Humanin Trifluoroacetate ≥95% (HPLC) Humanin is 24-amino acid mitochondria-associated peptide that is involved in numerous biological processes including apoptosis, cell survival, substrate metabolism, inflammatory response, and response to stressors such as oxidative stress, ischemia, and starvation. Humanin exhibits protective effects against cellular apoptosis. Apparently it inhibits BAX translocation to the mitochondrial outer membrane.
SML1129 HUP30 ≥98% (HPLC) HUP30 is a potent vasodilating agent that stimulates soluble guanylyl cyclase, activate K+ channels, and blocks extracellular Ca2+ influx. Also, HUP30 directly modulates L-type Ca2+ channels.
H5777 (±)-Huperzine A synthetic, ≥98% (TLC) Huperzine A is an effective acetylcholinesterase inhibitor and can cross the blood-brain barrier. Huperzine A is known to prevent cognitive defects, glutamate-induced nerve cell death.It is recognized for its use in the treatment of Alzheimer′s disease and organophosphate poisoning.
human ... BCHE(590)
rat ... Ache(83817)
SML2170 HX531 ≥98% (HPLC) HX-531 is a potent antagonist of the retinoid X receptor (RXR) with an IC50 value of 18 nM. HX531 has been used in many studies of the various effects of retinoids and RXR activity in diseases such as diabetes, Parkinson′s disease, often as a control for agonists such as Bexarotene. It was recently shown to promote white adipogenic differentiation and inhibit both basal and Bexarotene-induced brown adipogenic differentiation.
H7630 Hyaluronic acid sodium salt from bovine vitreous humor High molecular mass polymer composed of repeating dimeric units of glucuronic acid and N-acetyl glucosamine which forms the core of complex proteoglycan aggregates found in extracellular matrix.
Hyaluronic acid (HA) is abundantly present in the bovine vitreous humor. It corresponds to a molecular weight of 69293.9Da and has an isoelectric pH of 5.82. Bovine HA has high levels of endotoxins and it polydisperse with DNA and RNA contaminants. The enzyme HA synthases at the plasma membrane (HASs) aids in the synthesis of circulatory HA. HA is implicated in many physiological processes including inflammation, immune regulation, adhesion, embryo development and tumor progression.
H1753 Hydralazine hydrochloride Inhibits DNA methyltransferase and modulates epigenetic regulation of gene expression. Non-selective MAO-A/B inhibitor; antihypertensive; semicarbazide-sensitive amine oxidase inhibitor.
human ... MAOA(4128), MAOB(4129)
H4516 Hydrocodone (+)-bitartrate salt μ opioid receptor agonist; narcotic analgesic and antitussive.
H4001 Hydrocortisone ≥98% (HPLC) Primary glucocorticoid secreted by the adrenal cortex. It has three times the anti-inflammatory potency of corticosterone but much lower Na2+ retention potency.
human ... ABCB1(5243), CYP3A4(1576), NR3C1(2908), SERPINA6(866)
mouse ... Abcb1a(18671), Abcb1b(18669), Ifng(15978), Nos2(18126)
rat ... Ar(24208), Nr3c1(24413)
H4126 Hydrocortisone 21-acetate ≥98% (HPLC)   human ... NR3C1(2908), SERPINA6(866)
H5270 Hydrocortisone 17-butyrate   human ... NR3C1(2908)
H6635 Hydrocortisone 3-(O-carboxymethyl)oxime Hydrocortisone 3-(O-carboxymethyl)oxime is used as the analog of cortisol. It is used to modify the surface of an Au chip.
H4881 Hydrocortisone 21-hemisuccinate sodium salt ≥90% (HPLC)   human ... NR3C1(2908)
H1009 Hydrogen peroxide solution 30 % (w/w) in H2O, contains stabilizer    
H5136 Hydromorphone hydrochloride Narcotic opiate analgesic; μ opioid receptor agonist.
human ... OPRM1(4988)
H2161 8-Hydroxyadenosine-3′,5′-monophosphorothioate, Rp-isomer >99% (HPLC), solid Phosphodiesterase-resistant, polar, membrane-impermeable inhibitor of cAMP-dependent protein kinase (PKA).
H9149 α-Hydroxyalprazolam powder, ≥98% (TLC)    
H7278 NG-Hydroxy-L-arginine acetate salt Intermediate in the conversion of arginine to NO and citrulline by NO synthase.
NG-Hydroxy-L-arginine acts as a physiological inhibitor of arginase.
UC169 Hydroxybufuralol maleate salt ≥98% (HPLC) Metabolite of bufuralol; product of microsomal oxidation
H3167 (2S,3S)-Hydroxybupropion hydrochloride ≥98% (HPLC) (2S,3S)-hydroxybupropion is a dopamine transporter (DAT) and norepinephrine transporter (NET) transporters inhibitor and nicotinic acetylcholine receptor (nAChR) family modulator. Hydroxybupropions were reported to contribute to antidepressant and perhaps smoking cessation activities. Both (2S,3S) and (2R,3R) metabolites reverse affective and somatic withdrawal signs in nicotine-dependent mice, but (2S,3S)-hydroxybupropion is more potent. (2S,3S)-hydroxybupropion significantly decreases the development of nicotine reward in mice.
H0915 Hydroxychloroquine sulfate ≥98% (HPLC), powder Hydroxychloroquine is also used for treating rheumatoid arthritis and systemic lupus erythematosus.
Hydroxychloroquine sulfate is an anti-inflammatory (via TNF), disease-modifying antirheumatic drug (DMARD), and a heme polymerase inhibitor. It is used in treating malaria.
human ... TLR7(51284), TLR9(54106)
UC148 6-Hydroxychlorzoxazone ≥98% (HPLC)    
SML1648   24(S)-Hydroxycholesterol ≥98% (HPLC) 24(S)-Hydroxycholesterol is the major brain metabolite formed from cholesterol in the brain and is important for brain cholesterol homeostasis in addition to being an an endogenous agonist of the nuclear liver X receptors (LXRs). Impairment of brain cholesterol metabolism has been associated with several neurodegenerative diseases, including multiple sclerosis, Alzheimer′s, and Huntington diseases. The exact role role of 24(S)-Hydroxycholesterol is unclear, and it may have differing effects depending on concentration. Low concentrations can protect neuronal cells against oxidative stress, while high concentrations induce necroptosis-like neuronal cell death. 24(S)-Hydroxycholesterol has also been found to be a potent allosteric modulator of N-methyl-d-aspartate receptors, potentiating NMDAR-mediated EPSCs in rat hippocampal neurons with an EC50 of 1.2 μM.
H6779 6α-Hydroxycortisol ≥98%    
H6904 6β-Hydroxycortisol ≥98% 6β-Hydroxycortisol is a metabolite of cortisol.
UC263 7-Hydroxycoumarin glucuronide sodium salt    
UC283 7-Hydroxycoumarin sulfate potassium salt ≥95% (HPLC)    
UC261 (±)-4-Hydroxydebrisoquin sulfate CYP2D6 metabolite of debrisoquin.
H135 5-Hydroxydecanoic acid sodium salt ≥97% (HPLC) Blocks post-ischemic actions of the K+ channel activator cromakalim.
H5653 8-Hydroxy-2′-deoxyguanosine ≥98% (TLC) A marker compound typically indicative of DNA damage associated with mutagenesis and carcinogenesis
The levels of 8-hydroxy-2′-deoxyguanosine helps in evaluating oxidative stress and DNA damage in individuals suffering from laryngeal cancer. Hence it serves as a major biomarker of DNA damage, induced by reactive oxygen species (ROS).
162957 6-Hydroxydopamine hydrobromide 95% Neurotoxin that destroys catecholaminergic terminals.
H4381 6-Hydroxydopamine hydrochloride ≥97% (titration), powder Neurotoxin that destroys catecholaminergic terminals.
H168 R(+)-7-Hydroxy-DPAT hydrobromide >98%, solid Selective D3 dopamine receptor agonist; active enantiomer of (±)-7-hydroxy-DPAT.
human ... DRD3(1814)
H140 (R)-(+)-8-Hydroxy-DPAT hydrobromide ≥98% (HPLC), solid (R)-(+)-8-Hydroxy-DPAT is a full 5-HT1A serotonin receptor agonist; active enantiomer of (±)-8-hydroxy-DPAT.
(R)-(+)-8-Hydroxy-DPAT administration reduces aggressive behavior. It decreases food intake by modifying the sensitivity of 5-HT1A receptor during food deprivation.
human ... HTR1A(3350)
H141 S(−)-8-Hydroxy-DPAT hydrobromide solid Partial 5-HT1A serotonin receptor agonist.
SML0340 Hydroxy-Dynasore ≥98% (HPLC) Hydroxy-Dynasore is a cell permeable and potent dynamin inhibitor that prevents uptake of recombinant botulinum neurotoxin A heavy chain binding domain (BoNT/A-Hc). Apparently, Hydroxy-Dynasore prevents dynamin-mediated fission of endocytic vesicles from the plasma membrane.
H5142 20-Hydroxyecdysone ≥93% (HPLC), powder 20-Hydroxyecdysone is an ecdysteroid hormone that plays a key role in insect development, cell proliferaton, growth and apoptosis by controlling gene expression involved in molting and metamorphosis. It acts through a heterodimeric receptor comprising the ecdysone receptor and the ultraspiracle proteins (USP).
H6785 15(S)-Hydroxy-(5Z,8Z,11Z,13E)-eicosatetraene-(2-biotinyl)hydrazide ≥98%, ethanol solution Potent 5-lipoxygenase inhibitor.
H7768 12(S)-Hydroxy-(5Z,8Z,10E,14Z)-eicosatetraenoic acid ~100 μg/mL in ethanol, ≥95% (HPLC) 12(S)-HETE is a bioactive lipid implicated in angiogenesis, growth, and metastasic action in tumor cell lines and in animal models. Arachidonate 12-lipoxygenase (12-LOX) converts arachidonic acid to 12(S)-(HETE). Alteration in 12-LOX expression or activity has been reported in various carcinomas including prostate carcinoma.
Prometastatic metabolite of arachidonic acid via the 12-lipoxygenase pathway that is expressed in many tumor cell lines. It is produced in coronary microvasculature and is a potent inducer of relaxation and hyperpolarization of these microvessels. It activates large-conductance Ca2+-activated K+ currents in coronary microvascular smooth muscle.
H3023 20-Hydroxy-(5Z,8Z,11Z,14Z)-eicosatetraenoic acid ~100 μg/mL in ethanol, ≥90% (HPLC) 20-Hydroxy-(5Z,8Z,11Z,14Z)-eicosatetraenoic acid (20-HETE) is an arachidonic acid metabolite via cytochrome P4504A, that is an activator of the Ras/MAP (microtubule-associated protein) pathway. 20-HETE acid is a predominant arachidonic acid present in the kidney. It is involved in the regulation of sodium, potassium and chloride transport in the renal tubules. 20-HETE is often excreted in urine in the form of glucuronide conjugate and sometimes as free acids. Increased urine 20-HETE is observed during pregnancy in rats.
H3131 2-Hydroxyestradiol ≥95% (HPLC)   rat ... Ar(24208)
H6012 4-Hydroxyestrone ≥90% (HPLC) 4-Hydroxyestrone is an endogenous estrogen metabolite, which exhibits a strong neuroprotective effect against oxidative damage. It also provides effective protection against kanic acid-induced hippocampal oxidative damage in rats when compared to 17β-estradiol. 4-Hydroxyestrone regulates the angiogenic process during corpus luteum formation. It might be involved in an increased risk of cancer. 4-Hydroxyestrone is found in the early and mid-luteal phases.
H9006 7-(β-Hydroxyethyl)theophylline solid Pharmacological profile similar to theophylline.
human ... ADORA2B(136)
H4413 Hydroxyfasudil hydrochloride hydrate ≥98% (HPLC), solid Hydroxyfasudil possessantispastic action. It is an active metabolite of fasudil. Hydroxyfasudil might enhance the dynamics of blood flow and prevent damage caused by neutrophils.
Rho-kinase inhibitor.
H4166 Hydroxyflutamide ≥98% (HPLC) Hydroxflutamide is an AR antagonist. Androgen receptors (ARs) are nuclear hormone receptors/transcription factors. Hydroxyflutamide is an androgen antagonist with publications going back to 1981. It is one of a few gold standard AR antagonists; activities of new antagonists are measured against hydroxyflutamide.
Hydroxyflutamide plays a role in preventing the binding of 5α-dihydrotestosterone (DHT) and testosterone to the androgen receptors.
H8876 5-Hydroxyindole-3-acetic acid ≥98% (HPLC), crystalline Major serotonin metabolite.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR4(3360), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363)
H0627 6-Hydroxymelatonin 6-Hydroxymelatonin (6-OHM) is an antioxidant with a free radical scavenging role. Like melatonin, it reduces the impact of UVB-induced oxidative stress in melanocytes. It also aids protection during iron (Fe2+)-induced neurotoxicity. 6-OHM effectively reduces lipid peroxidation and superoxide anion production induced by potassium cyanide (KCN).
human ... MTNR1A(4543), MTNR1B(4544)
UC126 4-Hydroxymephenytoin 4-Hydroxymephenytoin catabolism displays genetic polymorphism and is a direct indicator of Cytochrome P450 2C19 (CYP2C19) activity. Detection and quantification of 4-hydroxymephenytoin in biological samples by HPLC method is well optimized.
H0131 DL-4-Hydroxy-3-methoxymandelic acid ≥98% (HPLC), powder Epinephrine and norepineprine metabolite.
H3132 3-Hydroxy-4-methoxyphenethylamine hydrochloride Dopamine metabolite.
human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816)
H1377 4-Hydroxy-3-methoxyphenylglycol hemipiperazinium salt Cerebral norepinephrine metabolite.
H8759 4-Hydroxy-3-methoxyphenylglycol sulfate potassium salt ≥98% (HPLC), powder Norepinephrine metabolite that is often used as an index of adrenergic stimulation.
UC430 1′-Hydroxymidazolam 1′-Hydroxymidazolam is the major hydroxylated metabolite of Midazolam (MDZ), forms due to rapid and extensive metabolization of MDZ by the CYP 450 3A isoenzymes in the liver. The product contributes to the pharmacological impact of MDZ.
UC431 4-Hydroxymidazolam 4′-Hydroxymidazolam is the minor hydroxylated metabolite of Midazolam (MDZ). The product contributes in the pharmacological impact of MDZ.
CYP3A4 metabolite of midazolam.
SML0106   N-Hydroxy-4-(1-naphthalenyl)-benzamide ≥98% (HPLC) N-Hydroxy-4-(1-naphthalenyl)-benzamide is a cell-permeable, potent and selective HDAC8 inhibitor.
SML1873 (2R,6R)-Hydroxynorketamine hydrochloride ≥98% (HPLC) (2R,6R)-Hydroxynorketamine is a ketamine metabolite that has rapid antidepressant activity without ketamine-related side effects. The NMDAR antagonist (R,S)-ketamine must be metabolized to (2S,6S;2R,6R)-hydroxynorketamine (HNK) to have antidepressant effects. The (2R,6R)-HNK enantiomer appears to be the enantiomer most responsible for antidepressant effects in a mouse study and unlike (2S,6S)-HNK, (2R,6R)-HNK caused no significant changes in locomotion or coordination. (2R,6R)-HNK does not seem to have the same addiction potential as ketamine, since mice did not self-administer pharmacologically relevant doses of (2R,6R)-HNK under the same conditions where ketamine was readily self-administered. The (2R,6R)-HNK antidepressant appears to involve activation of AMPA glutamate receptors rather than inhibition of NMDA glutamate receptors.
SML1875 (2S,6S)-Hydroxynorketamine hydrochloride ≥98% (HPLC) (2S,6S)-Hydroxynorketamin  
H6910 13S-Hydroxy-9Z,11E-octadecadiene-(2-biotinyl)hydrazide ≥98%, ethanol solution Modulates the platelet-activating factor, leukotriene B4, and formyl-Met-Leu-Phe-induced calcium influx in human polymorphonuclear leukocytes.
H9146 13(S)-Hydroxyoctadeca-9Z,11E-dienoic acid 90-100 μg/mL in ethanol, ≥98% Expression of 15-lipoxygenase-1 (15-LOX-1) and its main product, 13(S)-HODE, are decreased in human colorectal and esophageal cancers. Certain non-steroidal anti-inflammatory drugs (NSAIDs) can induce apoptosis in human colon cancer cells by increased expression of 15-LOX-1, which down-regulates PPAR-delta through 13-HODE.
PPARγ agonist
P102 R(+)-3-(3-Hydroxyphenyl)-N-propylpiperidine hydrochloride solid D2 dopamine receptor agonist. Also functions as σ1 receptor antagonist with essentially no affinity for the phencylidine site on the NMDA receptor.
human ... DRD2(1813)
H5002 17α-Hydroxypregnenolone 17α-hydroxypregnenolone acts as a precursor for cortisol and sex steroids.
H5752 17α-Hydroxyprogesterone ≥95% 17α-Hydroxyprogesterone (17OHP) is converted to 11-deoxycortisol in the presence of enzyme 21-hydroxylase. Deficiency of 21-hydroxylase results in the accumulation of 17OHP. High levels of 17OHP are observed in congenital adrenal hyperplasia (CAH).
human ... PGR(5241), SERPINA6(866)
rat ... Ar(24208)
D6875 21-Hydroxyprogesterone ≥97% (HPLC)   human ... SERPINA6(866)
P0618 cis-8-Hydroxy-3-(n-propyl)-1,2,3a,4,5,9b-hexahydro-1H-benz[e]indole hydrobromide ≥98% (HPLC), solid D3 dopamine receptor agonist.
human ... DRD3(1814)
H6278 4-Hydroxytamoxifen ≥70% 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.
human ... ESR1(2099), ESR2(2100), ESRRG(2104), IL6(3569)
rat ... Ar(24208), Esr1(24890), Esr2(25149)
H7904 (Z)-4-Hydroxytamoxifen ≥98% Z isomer 4-Hydroxytamoxifen (4-HT) is the active metabolite of tamoxifen which binds estrogen receptors (ER) and estrogen-related receptors (ERR) with estrogenic and anti-estrogenic effects. It is a cell permeable, selective estrogen receptor modulator (SERM). In Cas9 variants engineered with ligand-dependent inteins 4-Hydroxytamoxifen was used control Cas9 function, which reduced off target effects in CRISPR-mediated gene editing.
human ... ESR1(2099), ESR2(2100), ESRRG(2104), IL6(3569)
rat ... Ar(24208), Esr1(24890), Esr2(25149)
SML1666   4-Hydroxytamoxifen Ready Made Solution 5 mg/mL in ethanol: isopropanol (95:5) 4-Hydroxytamoxifen is an active metabolite of Tamoxifen. 4-Hydroxytamoxifen is formed by cytochrome P450 2D6 in human liver and is a potent and selective estrogen receptor antagonist. 4-Hydroxytamoxifen has been used to stimulate LC3 lipidation and to form autophagic vesicles in a superoxide-dependent manner. Tamoxifen and 4-Hydroxytamoxifen markedly induce cytochrome P450 3A4 (a major drug-metabolizing enzyme) in primary cultures of human hepatocytes. 4-Hydroxytamoxifen undergoes a cis-trans (E-Z) isomerization, a process that occurs in all common laboratory solvents.
Trans isoform of 4-hydroxytamoxifen possesses antiestrogenic activity, while the cis 4-hydroxytamoxifen serves as a key agonist for estrogen receptor. 4-Hydroxytamoxifen promotes apoptosis via activation of p38 pathway in breast cancer cell cultures.
H2898 6β-Hydroxytestosterone ≥97% (HPLC) 6β-Hydroxytestosterone is a CYP3A4 metabolite; androgenic.
UC287   7α-Hydroxytestosterone 7α-Hydroxytestosterone is known to block the synthesis of dihydrotestosterone and 5α-androstane-3α, 17β-diol in mature rat testis.
CYP2A1 (rat) metabolite; androgenic
UC289 16β-Hydroxytestosterone CYP3A2/2B1 (rat) metabolite; androgenic
H6771 2-Hydroxytetradecanoic acid ≥98% (capillary GC) An analog of myristic acid that becomes metabolically activated in cells to form 2-hydroxymyristoyl-CoA. Inhibitor of protein myristoylation.
UC160 4-Hydroxytolbutamide ≥98% (HPLC)    
H2529 α-Hydroxytriazolam Triazolam metabolite
H9772 5-Hydroxy-L-tryptophan powder Hydroxylation of L-tryptophan occurs in the brain during serotonin synthesis. This is a step that controls the production of serotonin and also yields 5-hydroxy-l-tryptophan (5-HTP) as a metabolite. Thus, consumption 5-HTP, increases the serotonin level, which might result in depression, lack of sleep and severe headache.
Immediate precursor of serotonin; L-aromatic amino acid decarboxylase substrate.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR4(3360), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363)
H8627 Hydroxyurea 98%, powder Anti-neoplastic. Inactivates ribonucleoside reductase by forming a free radical nitroxide that binds a tyrosyl free radical in the active site of the enzyme. This blocks the synthesis of deoxynucleotides, which inhibits DNA synthesis and induces synchronization or cell death in S-phase.
human ... CA1(759), CA2(760), CYP1A2(1544), RRM1(6240), RRM2(6241), RRM2B(50484)
UC209 4-Hydroxywarfarin Minor CYP3A4 metabolite od (S)-warfarin.
UC211 7-Hydroxywarfarin CYP2C9 metabolite of (S)-warfarin.
UC223 10-Hydroxywarfarin Major CYP3A4 metabolite of (R)-warfarin.
H8885 Hydroxyzine dihydrochloride ≥98% Hydroxyzine dihydrochloride (HDH) is used to regulate anxiety. It is also used to treat bronchial asthma and to relax patients before surgery.
human ... HRH1(3269)
H0409   Hylambatin >96% (HPLC) Tachykinin that increases plasma glucose and plasma insulin.
SML0301   Hymeglusin ≥98% (HPLC), from Fusarium sp. Hymeglusin is a specific β lactone inhibitor of eukaryotic hydroxymethylglutaryl-CoA synthase (HMGCS), a key enzyme in the cholesterol biosynthetic pathway. Unlike other fungal metabolites, Hymeglusin inhibits mevalonate biosynthesis by acting on HMG-CoA synthase, while other fungal metabolites such as Lovastatin (Mevinolin) and Compactin act as specific competitive inhibitors of the HMG-CoA reductase. Inhibition results from covalent modification of the active Cys129 residue by the enzyme by the formation of a thioester adduct in the active site. Hymeglusin show no inhibitory effect against fatty acid synthetase purified from Sacharomyces serevisiae. Hymeglusin was found to block the growth of Enterococcus faecalis. After removal of the inhibitor from the culture medium, a growth curve inflection point is observed. Upon Hymeglusin inactivation, enzyme activity is restored at a rate that is 8-fold faster for human HMGCS than for the bacterial enzyme (mvaS). Structural studies explain these differences. Hymeglusin was also found to inhibit the replication of the dengue live virus (DEN-2 NGC virus) in K562 cells. Lovastatin inhibits DEN-2 NGC live virus replication in human peripheral blood mononuclear cells.
H3878 Hyodeoxycholic acid ≥98%   human ... NR1H2(7376), NR1H3(10062)
H2517 Hyodeoxycholic acid methyl ester ≥98%    
H9791 Hyp9 Hyperforin is the active ingredient in St. John′s Wort. It is used to treat depression, known to indirectly inhibit reuptake of serotonin and norepinephrine at the synapse, and recently discovered to exert its actions by directly activating TRPC6. TRPC6 is a member of the canonical transient receptor potential (TRPC) family of ion channels. DAG is the endogenous activator of this channel, and Hyperforin is the only known TRPC6-selective activator. Although it is broadly used, Hyperforin is chemically unstable. Efforts to find a stable but pharmacologically similar TRPC6 activator resulted in the discovery of Hyp9, a simplified phloroglucinol derivative. Like Hyperforin, Hyp9 inhibits serotonin reuptake and induces neurite outgrowth. It increases calcium entry into the cell and selectively increases current through TRPC6 channels.
H5160 Hyperforin ≥85% (HPLC) Hyperforin is an active antidepressant and an inhibitor of cytochrome P450 3A4 (CYP3A). It elicits antioxidant and antibacterial activity. Hyperforin is also embryotoxic and inhibits tumor proliferation. It effectively inhibits dopamine, serotonin and norepinephrine.
H1792 Hyperforin (dicyclohexylammonium) salt Hyperforin is believed to be the primary active constituent responsible for the antidepressant and anxiolytic properties of the extracts of St. John′s wort. It acts as a reuptake inhibitor of monoamines, including serotonin, norepinephrine, dopamine, and of GABA and glutamate by activating the transient receptor potential ion channel TRPC6. It also is an activator of the pregnane X receptor (PXR), which serves as a key regulator of CYP3A4 transcription, a member of the cytochrome (CYP) P450 enzyme system. Recent studies have found it to have neuroprotective effects against Alzheimer′s disease (AD) neuropathology, including the ability to disassemble amyloid-β aggregates in vitro and improve spatial memory in vivo.
Stable salt of hyperforin. Hyperforin is believed to be the primary active constituent responsible for the antidepressant and anxiolytic properties of the extracts of St. John′s wort. It acts as a reuptake inhibitor of monoamines, including serotonin, norepinephrine, dopamine, and of GABA and glutamate by activating the transient receptor potential ion channel TRPC6. Activation of TRPC6 induces the entry of sodium and calcium into the cell which causes inhibition of monoamine reuptake. It also is an activator of the pregnane X receptor (PXR), which serves as a key regulator of CYP3A4 transcription, a member of the cytochrome (CYP) P450 enzyme system. Recent studies have found other neurological effects, effects on inflammation, as well as antibacterial, antitumoral and antiangiogenic effects.
H1667 Hypothemycin from Hypomyces trichothecoides, ≥98% (HPLC) Hypothemycin, one of the highly oxygenated analogues in the group of 14-membered resorcylic acid lactones (RAL), has minor antifungal and cytotoxic activity and exhibits an in vitro anti-malarial activity with an IC50 of 2.2 μg/mL. Hypothemycin is also reported to selectively and irreversibly inhibit protein kinases that contain a conserved cysteine residue (Cys166) that is located within the ATP-binding domain. Though this group accounts for less then 10% of all identified kinases, there are several targets implicated in aberrant cellular proliferation such as ERKs, MEK, FMS-like tyrosine kinase protein (FLT), and platelet-derived growth factor receptors (PDGFR). In cell culture, hypothemycin displays potent cytotoxicity against cancer cell lines that are dependent on certain activating kinase mutations. Additionally, hypothemycin demonstrates significant tumor growth inhibition in at least three separate murine xenograft models. Hypothemycin also inhibits the production of several cytokines such as IL2, IL6, IFNγ, and TNFα.
SML1158 (2S)-Hypusine dihydrochloride ≥95% (HPLC) (2S)-Hypusine is an unusual amino acid found only in eukaryotic translation initiation factor 5A (eIF5A) and a similar protein in archaebacteria. (2S)-Hypusine is formed by posttranslational modification of a lysine with the addition of the 4-aminobutyl moiety from the polyamine spermidine. There is increasing interest in the polyamine-hypusine axis and eIF5A, its a role in cell growth and differentiation, and a recent paper on the polyamine-hypusine axis as a potential new tumour suppressor network.
SML2462 HZ-166 ≥98% (HPLC) HZ-166 is a potent, non-sedative GABAA receptor subtype-selective benzodiazepine site agonist exhibits preference toward α2- and α3-GABAARs. HZ-166 exhibits antihyperalgesic properties in mice models of neuropathic and inflammatory pain, without sedation and motor impairment.