New Products

7-TM Receptors

Cat.No.

Product Name / Activity

Potent, selective CCR1 antagonist

AT₁ receptor antagonist

Prodrug of candesartan, an AT₁ receptor antagonist

Oxytocin analog

Selective S1P₁ agonist

Potent and selective S1P₄ agonist

Potent and selective S1P₄ agonist

Potent NPY Y₂ receptor antagonist

Selective 5-HT_2A antagonist

Highly potent and selective OX₂ antagonist; brain penetrant

PAR₂ peptide antagonist

Selective GPR30 antagonist

Selective LPA₂ receptor non-lipid agonist

Selective A_2B antagonist

Potent and selective LPA₂ receptor antagonist

Potent CXCR4 antagonist

Selective OX₂ receptor antagonist

FP prostaglandin receptor agonist; also exhibits agonist activity at EP₁ and EP₃ receptors

Selective 5-HT₇ ligand

FFA1 (GPR40) agonist. Also inhibits ATP citrate lyase

Apelin receptor (APJ) antagonist

Selective negative allosteric modulator of group II mGlu receptors

Potent and selective EP₂ receptor antagonist

Negative allosteric modulator at PAR₁ receptor

5-HT₂/D₂ antagonist; atypical antipsychotic

Caged GABA; inhibits neural activity

5-HT_2C inverse agonist; α₂ antagonist

Long-acting β₂ agonist; bronchodilator

Urotensin-II (UT) antagonist; attenuates cardiac dysfunction

Inhibits Smoothened (Smo) accumulation

Potent NK₁ receptor antagonist

Selective CB₁ receptor antagonist

Calcium sensing receptor (CaSR) agonist

Potent, high affinity CB₁ receptor inverse agonist

Selective melanin-concentrating hormone receptor 1 (MCH₁R) antagonist

Potent and selective GPR120 agonist

Negative allosteric modulator at mGlu₅

Selective H₄ agonist

Cellular Processes

Cat.No.

Product Name / Activity

Potent and selective kinesin spindle protein (KSP) inhibitor; induces Mcl-1 degradation

Selective Bax activator; induces Bax-mediated apoptosis

Prodrug of 5-Fluorouracil (Cat. No. 3257). Inhibits DNA synthesis

Inhibits TCF-dependent transcription; lowers β-catenin levels

Cytotoxic nucleoside analog; inhibits RNA synthesis

Selectively inhibits PKC-induced NF-κB activation

Selective inhibitor of OXE-R Gβγ signaling

Inhibits Hedgehog signaling

Enables Wnt/β-catenin-driven expansion of ESCs; prevents spontaneous differentiation

Stabilizes F-actin; promotes actin polymerization

Inhibitor of Hedgehog (Hh) signaling; binds directly to Smo

Potent, selective BET bromodomain inhibitor; cell permeable

Wnt pathway inhibitor; induces degradation of active β-catenin

HIF-1α inhibitor; down-regulates HIF-1α protein synthesis

Promotes differentiation of human ESCs and iPSCs into cardiomyocytes

DNA alkylating agent; cytotoxic and antineoplastic

Mcl-1 inhibitor; proapoptotic

Binds mot-2; selectively cytotoxic in cancer cells

HIF pathway activator

NAADP antagonist; inhibits Ca²⁺ release

Induces G₂/M cell cycle arrest; anticancer

Inhibitor of SCD1; selectively eliminates undifferentiated hPSCs from culture

Highly potent and selective DOT1L inhibitor; cell permeable

Nrf2 pathway activator; blocks Nrf2/Keap1 interaction

Potent and selective L3MBTL3 domain inhibitor; cell permeable

Enzyme-Linked Receptors

Cat.No.

Product Name / Activity

TrkB receptor antagonist

Dual IR/IGF1R inhibitor

Glycoprotein IIa/IIIb inhibitor; inhibits platelet aggregation

Potent antagonist of α_vβ₃-vitronectin interaction; antiangiogenic

TLR2/6 agonist; induces TNF-α production

Biotinylated Pam2CSK4 (Cat. No. 4637)

TLR1/2 agonist; induces cytokine production

Biotinylated Pam3CSK4 (Cat. No. 4633)

Enzymes

Cat.No.

Product Name / Activity

Selective IKKα and IKKβ inhibitor

Selective SIRT2 inhibitor; brain penetrant

Potent and selective p38α inhibitor

Inhibitor of TBK1 and IKKε; antiallergic agent

Histone deacetylase inhibitor

Potent PKC inhibitor and nicotinic receptor antagonist

ATP citrate lyase inhibitor; orally bioavailable

Selective cathepsin B inhibitor

Pan protein kinase D (PKD) inhibitor; cell permeable

Potent JAK inhibitor

Fluorescent cytochrome P450 substrate

Selective inhibitor of PI 3-Kinase γ

Potent LRRK2 inhibitor; neuroprotective

γ-secretease inhibitor; inhibits Notch pathway

Sphingosine kinase inhibitor

Potent COMT inhibitor; blocks α-synuclein aggregation

Cyclin-dependent kinase inhibitor

Geranylgeranyltransferase I (GGTase I) inhibitor

Potent, selective LRRK2 inhibitor; brain penetrant

Furin inhibitor

Selective T-LAK-cell-originated protein kinase (TOPK) inhibitor

Pan kinase inhibitor; potently inhibits MEK-1

Histone demethylase inhibitor; cell permeable

Protein kinase C inhibitor; selective for β isozymes

Cyclooxygenase-inhibiting nitric oxide donor

USP7 inhibitor

Reversible inhibitor of MKLP-2

Selective Epac activator; cell-permeable analog of 8CPT-2Me-cAMP (Cat. No. 1645)

Potent, selective Cdk4/6 inhibitor; brain penetrant

Protein kinase C activator

Aurora kinase A and B inhibitor

Dual PI 3-K/mTOR inhibitor

Potent and selective dual PI 3-kinase/mTOR inhibitor

Potent inhibitor of interleukin-2 inducible T cell kinase (ITK). Also inhibits BTK

Inhibits Skp2-mediated p27 degradation; induces cell cycle arrest

Potent and selective 17β-hydroxysteroid dehydrogenase type 3 inhibitor

Potent and selective ERK2 inhibitor

Inhibitor of IP6K; also inhibits IP3K

Tankyrase inhibitor; inhibits Wnt signaling

ALDH1a2 inhibitor

Potent and selective mTOR inhibitor

Ion Channels

Cat.No.

Product Name / Activity

Positive allosteric modulator of α7 nAChR

Selective TRPA1 channel blocker

Potent and selective K_V1.3 channel blocker

ASIC3 channel blocker

Calcium-activated chloride channel (CaCC) inhibitor

Potassium channel blocker; neuroprotective

Positive allosteric modulator of GluA2 receptors

Activator of Ca²⁺-activated Cl^- channel transmembrane protein 16A (TMEM16A)

Inhibits TRPP3-mediated currents; also inhibits the Na⁺/H⁺ exchanger (NHE)

Stretch-activated calcium channel blocker; calcium-sensing receptor agonist

Selective Na_V 1.7 channel blocker

Selective TRPC4 blocker

Activator of TRPML channels

Potent K_Ca3.1 channel blocker

Inhibits TRPP3-mediated currents; also inhibits epithelial Na⁺ channels

Ca_V3.1 channel blocker; also inhibits Na_V1.8 and K_V2.1

Negative allosteric modulator of 5-HT₃

TRPV1 antagonist; displays in vivo activity

Selective α3β4 nAChR antagonist

Selective P2X₃, P2X_2/3 antagonist

Nuclear Receptors

Cat.No.

Product Name / Activity

High affinity thyroid receptor α (TRα) and TRβ agonist; thyromimetic

Synthetic progesterone analog

High affinity PPARγ ligand; blocks Cdk5-dependent PPARγ phosphorylation

REV-ERBα antagonist

Constitutive androstane receptor (CAR) agonist

Transporters

Cat.No.

Product Name / Activity

NCX inhibitor, Deg/ENaC channel blocker; amiloride (Cat. No. 0890) derivative

PMAT inhibitor

Potent 5-HT and NE reuptake inhibitor; also blocks dopamine reuptake

P-gp inhibitor

Selective serotonin reuptake inhibitor (SSRI)

Inhibitor of BCRP-mediated multidrug resistance

Mood stabilizer; inhibits Na⁺/K⁺ ATPase pump activity

Potent and selective GlyT2 inhibitor

Na⁺/Ca²⁺ exchange inhibitor (reverse mode); neuroprotective