New Products

PI3K/Akt/mTOR
Catalog No. Product Name Information Added
S3462 PS210 PS210 is a potent activator of PDK1 that binds to the PIF-pocket and allosterically modulates the active site of PDK1. Oct 18 2021
E0072 Indirubin-3′-oxime Indirubin-3′-oxime (IDR3O, I3O) is an indirubin analogue that shows favorable inhibitory activity targeting GSK-3β and CDKs. Indirubin-3′-oxime also inhibits JNKs with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM for JNK1, JNK2, and JNK3, respectively. Indirubin-3′-oxime activates Wnt/β-catenin signaling and inhibits adipocyte differentiation and obesity. Oct 18 2021
S0430 MELK-8a Dihydrochloride MELK-8a Dihydrochloride is a novel inhibitor of maternal embryonic leucine zipper kinase (MELK) with an IC50 of 2 nM. Sep 16 2021
E0121 Parsaclisib (INCB050465)

Parsaclisib (INCB050465, INCB-50465, IBI376) is a potent and highly selective PI3Kδ(PI3K delta) inhibitor with an IC50 of 1 nM at 1 mM ATP in biochemical assay and approximately 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases.

Sep 01 2021
S6085 KY19382 (A3051) KY19382 (A3051) is a Wnt/β-catenin signalling activator through inhibitory effects on both CXXC5–DVL interaction and GSK3β activity with IC50s of 19 nM and 10 nM, respectively. Aug 11 2021
S8668 GDC-0077 GDC-0077 (RG6114) is a potent selective inhibitor of PI3K alpha (PI3Kα) with an IC50 of 0.038 nM. GDC-0077 is >300-fold more selective for PI3K alpha over the other class I PI3K isoforms (beta, delta, and gamma) and >2000-fold more selective over PIK family members. GDC-0077 binds to the ATP binding site of PI3K and inhibits the phosphorylation of PIP2 to PIP3. Aug 03 2021
S8779 Parsaclisib (INCB050465) Hydrochloride Parsaclisib (INCB050465, IBI376) Hydrochloride is a potent and highly selective PI3Kδ(PI3K delta) inhibitor with an IC50 of 1 nM at 1 mM ATP in biochemical assay and approximately 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases. Jul 23 2021
S4460 IMM-H007 IMM-H007, an adenosine derivative, is an activator of AMP-Activated Protein Kinase (AMPK). IMM-H007 is a potential drug for treating cardiac dysfunction. IMM-H007 negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling. IMM-H007 inhibits ABCA1 (ATP binding cassette subfamily a member 1) degradation and facilitates its cell-surface localization in macrophages, thereby promotes cholesterol efflux. Jun 01 2021
S9860 BC1618 BC1618 is an orally active Fbxo48 inhibitor that stimulates adenosine monophosphate (AMP)-activated protein kinase (Ampk)-dependent signaling. BC1618 promotes mitochondrial fission, facilitates autophagy and improves hepatic insulin sensitivity. May 24 2021
S9864 Elimusertib (BAY-1895344) Elimusertib (BAY-1895344) is a very potent and highly selective ATR (ataxia telangiectasia and Rad3-related) inhibitor with IC50 of 7 nM. Elimusertib potently inhibits proliferation of a broad spectrum of human tumor cell lines with median IC50 of 78 nM. Apr 27 2021
JAK/STAT
Catalog No. Product Name Information Added
S6789 JAK Inhibitor I (Pyridone 6) JAK Inhibitor I (Pyridone 6, CMP 6, Compound 6) is a pan-JAK inhibitor with IC50s of 1 nM, 1 nM, 5 nM and 15 nM for JAK2, TYK2, JAK3 and JAK1, respectively. Oct 18 2021
S3566 Cerdulatinib (PRT062070) Cerdulatinib (PRT062070, PRT2070) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM. Sep 01 2021
S0981 BD750 BD750 is an immunosuppressant and a dual inhibitor of JAK3 and STAT5 that inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation with IC50 of 1.5 μM and 1.1 μM for mouse and human T-cell proliferation, respectively. Feb 02 2021
S0374 GDC046 GDC046 (Compound 3) is a potent, selective, and orally bioavailable inhibitor of TYK2 with Ki of 4.8 nM, 83.8 nM, 27.6 nM and 253 nM for TYK2, JAK1, JAK2, and JAK3, respectively. Jan 18 2021
S0384 RO495 RO495 (CS-2667) is a potent inhibitor of Non-receptor tyrosine-protein kinase 2 (TYK2). Dec 29 2020
S0918 Ginkgolic acid C17:1 Ginkgolic acid C17:1 (GAC 17:1) inhibits constitutive activation of STAT3 through the abrogation of upstream JAK2 and Src. Ginkgolic acid C17:1 can induce the substantial expression of PTEN and SHP-1. Ginkgolic acid C17:1 induces apoptosis of tumor cells. Nov 27 2020
S9664 Colivelin Colivelin (CLN) is a brain-penetrant neuroprotective peptide with potent long-term capacity against deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin is an activator of STAT3. Nov 27 2020
S0818 STAT3-IN-1 STAT3-IN-1 (compound 7d) is an excellent, selective and orally active inhibitor of STAT3 with IC50 of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 induces apoptosis of tumor cells. Sep 25 2020
S9676 PF-06826647 PF-06826647 (Tyk2-IN-8, compound 10) is a selective and orally administered inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 17 nM for binding to TYK2 catalytically active JH1 domain. PF-06826647 (Tyk2-IN-8, compound 10) also inhibits JAK1 and JAK2 with IC50 of 383 nM and 74 nM, respectively. PF-06826647 (Tyk2-IN-8, compound 10) is used in the treatment of psoriasis (PSO). Sep 11 2020
S0437 SAR-20347 SAR-20347 is a potent inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50 of 0.6 nM, 23 nM, 26 nM and 41 nM, respectively. SAR-20347 inhibits TYK2- and JAK1-mediated IL-12 and IFN-α signaling. Sep 02 2020
Cell Cycle
Catalog No. Product Name Information Added
S0249 Mycro 3 Mycro 3 is a potent and selective inhibitor of c-Myc in whole cell assays. Mycro 3 also shows weak inhibitory activity against AP-1. Oct 18 2021
S6385 Prexasertib (LY2606368)

Prexasertib (LY2606368, ACR 368) is a selective ATP competitor inhibitor of Chk1 and Chk2 with IC50s of 1 nM and 8 nM in cell-free assays, respectively. Prexasertib also inhibits RSK1 with an IC50 of 9 nM in cell-free assay.

Sep 23 2021
S6768 CC-671 CC-671 is a selectively dual inhibitor of TTK (human protein kinase monopolar spindle 1 [hMps1]) and CDC like kinase 2 (CLK2) with IC50s of 5 nM and 3 nM for TTK and CLK2, respectively. Aug 03 2021
S6000 CID44216842 CID44216842 (Cdc42-IN-1) is a potent Cdc42-selective guanine nucleotide binding lead inhibitor with EC50s of 1.0 μM and 1.2 μM for Cdc42WT and Cdc42Q61L mutant in GTP binding assay, respectively. Jul 29 2021
S6390 Y-27632 Y-27632 is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK. Jul 23 2021
S6884 LY3405105 LY3405105 is an orally active CDK7 inhibitor with an IC50 of 92.8 nM. LY3405105 shows potential antineoplastic activity. Jul 16 2021
S6875 CASIN CASIN (Pirl1-related Compound 2) directly inhibits activation of Cdc42/RhoGDI with IC50 of 2 μM. Jul 06 2021
S8911 BOS172722 BOS-172722 is a monopolar spindle 1 (MPS1) checkpoint inhibitor with IC50 of 2 nM. Jul 06 2021
S9859 BSJ-4-116 BSJ-4-116 is a specific degrader of cyclin-dependent kinase 12 (CDK12). BSJ-4-116 exhibits potent antiproliferative effects. Jun 21 2021
S9880 MS140 MS140 is a specific and highly potent CDK4/6 kinase inhibitor and also a CDK4/6 degrader (PROTAC). Jun 21 2021
DNA Damage
Catalog No. Product Name Information Added
S9903 NRD167

NRD167 is a potent and selective SIRT5 inhibitor.

Sep 10 2021
S9775 SCR130 SCR130 is a novel DNA repair inhibitor with IC50s of 14 μM in Reh cells and 2 μM in Nalm6 cells. SCR130 specifically inhibits DNA Ligase IV‐mediated joining with minimal or no effect on Ligase III and Ligase I mediated joining. Jul 26 2021
S3397 FEN1-IN-4 FEN1-IN-4 (FEN1 Inhibitor C2, JUN93587, Compound 2) is an inhibitor of human flap endonuclease-1 (hFEN1) with IC50 of 30 nM for hFEN1-336Δ. Jun 22 2021
S3549 PFM01 PFM01, a cell-permeable N-alkylated Mirin derivative, is a selective inhibitor of MRE11 endonuclease activity. Jun 08 2021
S0858 EG1 EG1 is a specific Paired box 2 (Pax2) inhibitor that targets the DNA binding domain and inhibits embryonic kidney development. Jun 08 2021
S4476 PCNA-I1 PCNA-I1 is a selective inhibitor of proliferating cell nuclear antigen (PCNA, a potential anticancer target). PCNA-I1 selectively binds to PCNA trimers with Kd of ~0.2 to 0.4 μM. PCNA-I1 inhibits the growth of tumor cells of various tissue types with IC50 of ~0.2 μM. PCNA-I1 induces DNA damage and apoptosis in both LNCaP and PC-3 cells. PCNA-I1 also induces autophagy in PC-3 cells. Jun 01 2021
S0841 OGG1-IN-08 OGG1-IN-08 (O8 OGG1 Inhibitor-Bio-X) is a potent inhibitor of 8-oxoguanine DNA glycosylase-1 (OGG1) with IC50 of 0.22 μM. OGG1-IN-08 decreases both the glycosylase and lyase activities of OGG1. May 24 2021
S6997 CHAPS CHAPS is a zwitterionic surfactant that decreases the sequence specificity of the nucleosome. Apr 27 2021
S5026 Irinotecan hydrochloride Irinotecan (CPT-11, (+)-Irinotecan) hydrochloride is an inhibitor of Topoisomerase I (Topo I) that exhibits cytotoxicity in LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively. Apr 21 2021
S5195 Rucaparib Camsylate Rucaparib (Rubraca, AG014699, PF01367338) Camsylate is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Apr 21 2021
TGF-beta/smad
Catalog No. Product Name Information Added
S0069 VTX-27 VTX-27 (Compound 27) is a potent and selective inhibitor of protein kinase C θ (PKC θ) with Ki of 0.08 nM and 16 nM for PKC θ and PKC δ, respectively. Dec 08 2020
S0153 SJ000291942 SJ000291942 is a canonical bone morphogenetic proteins (BMP) signaling pathway activator. Oct 19 2020
S7692 A-83-01 A-83-01 is a potent inhibitor of TGF-β type I receptor (ALK5-TD) with IC50 of 12 nM. A-83-01 also inhibits the transcription induced by activin/nodal type I receptor (ALK4-TD) and nodal type I receptor (ALK7-TD) with IC50 of 45 nM and 7.5 nM, respectively.Solutions are best fresh-prepared. Jun 03 2020
S0523 SB 4 (Eticovo) SB 4 (Eticovo) is a potent and selective agonist of bone morphogenetic protein 4 (BMP4) signaling with EC50 of 74 nM. SB 4 (Eticovo) enhances canonical BMP signaling and activates SMAD-1/5/9 phosphorylation. Jun 02 2020
S2234 BIBF-0775 BIBF-0775 is a selective inhibitor of transforming growth factor β Receptor I (TGFβRI,Alk5) with an IC50 of 34nM. Mar 08 2020
A2113 Anti-human/mouse TGF-β-InVivo The 1D11.16.8 monoclonal antibody reacts with mouse, human, rat, monkey, hamster, canine and bovine TGF-β (transforming growth factor beta) isoforms 1, 2 and 3.The 1D11.16.8 monoclonal antibody is a neutralizing antibody. Mar 06 2020
S7530 Vactosertib (TEW-7197) Vactosertib  (TEW-7197, EW-7197) is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively. Phase 1. Feb 26 2020
S7208 Bisindolylmaleimide I (GF109203X) Bisindolylmaleimide I (GF109203X, GO 6850) is a potent PKC inhibitor with IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ in cell-free assays, respectively, showing more than 3000-fold selectivity for PKC as compared to EGFR, PDGFR and insulin receptor. Feb 24 2020
S6654 SRI-011381 SRI-011381 is a novel agonist of the TGF-beta signaling pathway for treatment of Alzheimer's disease. Jan 09 2020
S9522 Valrubicin Valrubicin is a chemotherapy drug used to treat bladder cancer. Valrubicin is a chemotherapy agent, inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 and 1.25 μM, respectively. Dec 19 2019
GPCR & G Protein
Catalog No. Product Name Information Added
E0102 I-191 I-191 is a potent PAR2 antagonist that inhibits multiple PAR2-induced signaling pathways and functional responses. I-191 also inhibits ERK1/2 phosphorylation, RhoA activation, and inhibition of forskolin-stimulated cAMP accumulation induced by micromolar concentrations of biased ligand GB88. Oct 18 2021
S0837 HJC0197 HJC0197 is a selective Epac 1/2 dual antagonists with an IC50 of 5.9 μM for Epac2. Oct 18 2021
E0039 A-779

A-779 is a potent and selective antagonist for Angiotensin-(1–7) (Ang-(1-7)) with an IC50 of 0.3 nM in a radioligand binding assay. A-779 shows no significant affinity for AT1 or AT2 receptors at a concentration of 1 μM.

Sep 23 2021
S3584 Luzindole Luzindole (N-0774, N-acetyl-2-benzyltryptamine) is a selective melatonin receptor antagonist with Kis of 179 nM for MT1 and 7.3 nM for MT2, respectively. Sep 10 2021
E0014 BIBO 3304 Trifluoroacetate

BIBO 3304 Trifluoroacetate (BIBO-3304 TFA) is a novel neuropeptide Y Y1 receptor (NPY1R) antagonist with IC50 values of 0.38 nM and 0.72 nM for human Y1 receptor and rat Y1 receptor, respectively. BIBO 3304 shows low affinity for the human Y2 receptor, human and rat Y4 receptor as well as for the human and rat Y5 receptor (IC50 values >1000 nM).

Sep 10 2021
E0013 DAMGO

DAMGO (DAGO) is a potent and selective μ opioid receptor agonist with ki of 17 nM.

Sep 10 2021
E0021 Apraglutide (FE 203799)

Apraglutide (FE 203799) is a potent and highly selective GLP-2 agonist with EC50s of 0.03 nM and 0.07 nM for hGLP-2 Receptor and rGLP-2 Receptor, respectively.

Sep 10 2021
S0272 Derenofylline (SLV320) Derenofylline (SLV320) is a selective and potent adenosine A1 antagonist with Ki of 1 nM. Derenofylline shows selective for adenosine A1 over A2A, A2B, and A3 receptors with Ki of 398 nM, 3981 nM, and 200 nM, respectively. Aug 23 2021
S9935 Teduglutide Teduglutide (ALX-0600, Gattex, Revestive, TAK 633) is an analogue of human glucagon-like peptide-2 (GLP-2) and binds to the GLP-2 receptors. Teduglutide prolongs the intestinotrophic properties of GLP-2 in animal models. Aug 19 2021
S9915 FSLLRY-NH2 TFA FSLLRY-NH2 TFA (FSY-NH2) is a selective protease-activated receptor 2 (PAR2) inhibitor with an ic50 of 50 µM in PAR2-KNRK cells. Aug 11 2021
PTK
Catalog No. Product Name Information Added
E0050 Seralutinib (GB002) Seralutinib (PK10571, GB002) is a novel PDGFR kinase inhibitor with IC50s of 8 nM and 10 nM for PDGFRα and PDGFRβ in enzyme assays, respectively. Oct 18 2021
S9620 TPX-0022 TPX-0022 (CSF1R-IN-2) is a potent inhibitor of MET/CSF1R/SRC with enzymatic kinase inhibition IC50s of 0.14 nM, 0.71 nM and 0.12 nM, respectively. TPX-0022 modulates the tumor immune microenvironment in preclinical models. Aug 03 2021
S6881 JND3229 JND3229 is a potent reversible inhibitor of EGFRC797S with an IC50 value of 5.8 nM. JND3229 also potently suppresses EGFRL858R/T790M and EGFRWT with IC50 values of 30.5 nM and 6.8 nM, respectively. Jul 16 2021
S7647 Lucitanib (E3810) hydrochloride Lucitanib (E-3810, AL3810) hydrochloride is a dual inhibitor of Vascular endothelial growth factor receptor (VEGFR) and Fibroblast growth factor receptor (FGFR). Lucitanib hydrochloride (E-3810, AL3810) potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50 of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively. Jun 28 2021
S6515 ALW II-41-27 ALW II-41-27 (compound 7) is a potent inhibitor of Eph receptor tyrosine kinase with Kd of 12 nM for EphA2. May 07 2021
S3187 SBI-477 SBI-477 is an insulin signaling inhibitor that deactivates the transcription factor MondoA, leading to reduced expression of the insulin pathway suppressors thioredoxin-interacting protein (TXNIP) and arrestin domain-containing 4 (ARRDC4). SBI-477 inhibits triacylglyceride (TAG) synthesis and enhances basal glucose uptake in human skeletal myocytes. Apr 27 2021
S4967 Ceritinib dihydrochloride Ceritinib (Zykadia, LDK378) dihydrochloride is a selective, orally bioavailable and ATP-competitive inhibitor of ALK with IC50 of 0.2 nM. Ceritinib dihydrochloride also inhibits InsR, IGF-1R and STK22D with IC50 of 7 nM, 8 nM and 23 nM, respectively. Ceritinib exhibits antitomor activity. Apr 21 2021
S5190 Crizotinib hydrochloride Crizotinib (PF-02341066) hydrochloride (Xalkori) inhibits tyrosine phosphorylation of c-Met and nucleophosmin (NPM)-anaplastic lymphoma kinase (ALK) with IC50 of of 11 nM and 24 nM in cell-based assays, respectively. Crizotinib hydrochloride is also a potent ROS1 inhibitor with Ki less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines. Apr 21 2021
S4947 Regorafenib Hydrochloride Regorafenib (Stivarga, BAY 73-4506) Hydrochloride is a multi-target inhibitor for VEGFR1, Murine VEGFR2/3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM, 4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively. Apr 13 2021
S9711 CH7233163 CH7233163 is a non-covalent ATP competitive inhibitor of EGFR-tyrosine kinase with antitumor activities against tumor with EGFR-Del19/T790M/C797S. Apr 07 2021
Epigenetics
Catalog No. Product Name Information Added
S6389 CPI-455

CPI-455 is a specific KDM5 inhibitor with an IC50 of 10 nM for full-length KDM5A in enzymatic assays. CPI-455 shows over 200-fold selectivity for KDM5 relative to KDM2, 3, 4, 6, and 7 enzymes.

Sep 27 2021
S9691 BMS-986158 BMS-986158 is a potent inhibitor of BET with IC50s of 6.6 nM and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively. Jul 16 2021
S8996 SNDX-5613 SNDX-5613 is a potent and selective inhibitor of menin-MLL binding with a Ki of 0.15 nM. SNDX-5613 shows anti-proliferative activity against multiple cell lines harboring MLLr translocations (MV4;11, RS4;11, MOLM-13, KOPN-8) with IC50 values ranging from 10-20 nM. Jul 16 2021
S9882 PFI-90

PFI-90 is a selective inhibitor of the histone demethylase KDM3B. PFI-90 induces apoptosis and cell differentiation resulting in delayed tumor progression in vivo.

Jul 15 2021
S9805 WM-3835 WM-3835 is a novel and high-specific small molecule Lysine Acetyltransferase 7 (KAT7, MYST2, HBO1) inhibitor, able to potently suppressed OS cell proliferation and migration, and leads to apoptosis activation. Jun 28 2021
S9667 CCS-1477 (CBP-IN-1) CCS1477(CBP-IN-1, CBP/p300-IN-4)is a potent and selective inhibitor of p300/CBP bromodomain. CCS1477 works by inhibiting the expression and function of the androgen receptor (AR), as well as inhibiting c-Myc. Apr 27 2021
S3573 CC-90010 CC-90010 is a reversible, orally active and central nervous system-penetrant inhibitor of bromodomain and extra-terminal (BET) proteins. CC-90010 is applied in the study for advanced solid tumors. Apr 21 2021
S9685 GSK620 GSK620 is a pan-BD2 inhibitor, which shows an anti-inflammatory phenotype in human whole blood with excellent broad selectivity, developability, and in vivo oral pharmacokinetics. Mar 30 2021
S8665 GNE-781 GNE-781 (compound 19) is an orally active, highly potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element binding protein (CBP) with IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50 of 6.2 nM and 5100 nM, respectively. GNE-781 exhibits antitumor activity. Jan 25 2021
S9684 GSK046 GSK046 (iBET-BD2) is a selective and orally active inhibitor of BET (bromodomain and extraterminal domain) with IC50 of 264 nM, 98 nM, 49 nM and 214 nM for BRD2BD2, BRD3BD2, BRD4BD2 and BRDTBD2, respectively. GSK046 exhibits immunomodulatory activity. Jan 05 2021
NF-κB
Catalog No. Product Name Information Added
S3384 (E/Z)-IT-603 (E/Z)-IT-603 is a mixture of E-IT-603 and Z-IT-603. IT-603 is a NF-κB family member c-Rel inhibitor with an IC50 of 3 μM in electrophoretic mobility shift assay (EMSA). Jul 29 2021
S5899 (R)-(-)-Ibuprofen (R)-(-)-Ibuprofen ((R)-Ibuprofen) inhibits the activation of NF-κB in response to T-cell stimulation with IC50 of 121.8 μM. R(-)-ibuprofen exerts anti-inflammatory and antinociceptive effects. May 06 2021
S4611 TCEP Hydrochloride TCEP (Tris(2-carboxyethyl)phosphine) hydrochloride, a non-thiol reducing agent, promotes NF-κB-DNA binding in a dose-related manner. Apr 07 2021
S8935 BAY-985 BAY-985 is a potent and highly selective TBK1/IKKε inhibitor. BAY-985 shows high potency toward TBK1 (IC50 = 2 nM, low ATP assay; 30 nM, high ATP assay) and IKKε(IC50 = 2 nM), as well as high potency in the mechanistic pIRF3 assay (IC50 = 74 nM), and an antiproliferative effect on SK-MEL-2 cells (IC50 = 900 nM). Feb 09 2021
S1321 Urolithin B Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα. Urolithin B suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass. Nov 18 2020
A2020 Denosumab (anti-RANK ligand) Denosumab (anti-RANK ligand) (AMG-162, Prolia, Xgeva) is a fully human monoclonal antibody that selectively inhibits primate RANKL. Denosumab inhibits the ability of human RANKL (143–317) to stimulate the formation of osteoclasts derived from murine RAW 264.7 cells with an IC50 value of 1.64 nM. Sep 15 2020
S8941 NIK SMI1 NIK SMI1 is a highly potent and selective NF-κB-inducing kinase (NIK) inhibitor with Ki of 0.23 nM for NIK-catalyzed hydrolysis of ATP to ADP. Aug 18 2020
S0507 CBL0137 CBL0137 (Curaxin-137) is an inhibitor of the histone chaperone FACT (facilitates chromatin transcription) that simultaneously suppresses NF-κB and activates p53 with EC50 of 0.47 μM and 0.37 μM, respectively. Jul 20 2020
S0425 TBK1/IKKε-IN-2 TBK1/IKKε-IN-2 (Ikk epsilon-in-1, IKKε-IN-1, MDK10496) is a dual inhibitor of TBK1 and IKKε. Jul 06 2020
S8922 TBK1/IKKε-IN-1(compound 1) TBK1/IKKε-IN-1 (compound 1) is a dual inhibitor of TANK-binding kinase 1 (TBK1) and IκB kinase-ε (IKKε/IKK-i) with IC50 of 1.0 nM and 5.6 nM for TBK1 and IKKε, respectively. TBK1/IKKε inhibition enhances response to PD-1 blockade, which effectively predicts tumor response in vivo. May 14 2020
Metabolism
Catalog No. Product Name Information Added
E0092 KEA1-97 KEA1-97 selectively modulates certain functions of thioredoxin (TXN) through protein interactions with caspase 3 without affecting its catalytic activity. Oct 18 2021
E0116 PF-06446846 hydrochloride PF-06446846 (PF846) Hydrochloride is an orally bioavailable and specific inhibitor of PCSK9 with an IC50 of 0.3 µM in Huh7 cells. Oct 18 2021
E0049 Pizuglanstat (TAS-205) Pizuglanstat (TAS-205) is a highly selective hematopoietic prostaglandin D synthase (HPGDS) inhibitor with an IC50 of 55.8 nM. Oct 18 2021
S6971 Ervogastat Ervogastat (PF-06865571, DGAT2i) is a potent diacylglycerol acyltransferase 2 (DGAT2) inhibitor that reduces steatosis and hepatic triglyceride levels in non-alcoholic steatohepatitis (NASH). Sep 18 2021
S9706 OT-82 OT-82 is a novel nicotinamide phosphoribosyltransferase (NAMPT) inhibitor with average IC50s of 13.03   nM in non-HP cancer cells and 2.89   nM in HP cancer cells, respectively. Sep 16 2021
S9914 CITCO

CITCO is a potent and selective constitutive androstane receptor (CAR) agonist with EC50 of 49 nM. CITCO displays >50-fold selectivity for CAR over PXR in the transient transfection assay.

Sep 16 2021
S9606 Galloflavin Galloflavin (NSC 107022) is a novel inhibitor of lactate dehydrogenasee (LDH) with Ki values of 5.46 μM and 15.06 μM for LDH-A and LDH-B, respectively. Sep 16 2021
E0032 Olesoxime (TRO 19622)

Olesoxime (TRO19622) is a novel, orally active and CNS-penetrant mitochondrial-targeted neuroprotective compound.

Sep 01 2021
S3486 AQX-016A AQX-016A is a potent agonist of SHIP1. AQX-016A inhibits DNFB induced inflammation in a mouse ear edema/cutaneous anaphylaxis model. Jul 29 2021
S6388 SHP099 SHP099 is a highly potent, selective and orally bioavailable small-molecule SHP2 inhibitor with an IC50  value of  71 nM and shows no activity against SHP1. Jul 28 2021
Proteases
Catalog No. Product Name Information Added
E0073 CL-82198 CL-82198 is a selective, orally bioavailable MMP-13 inhibitor with an IC50 of 3.2 μM. Oct 18 2021
E0122 Gemigliptin

Gemigliptin (Zemiglo, LC15-0444) is a potent, selective and long-acting dipeptidyl peptidase 4 (DPP 4) inhibitor with a Ki of 7.25 nM. Gemigliptin shows at least >23,000-fold selectivity for DPP-4 over various proteases and peptidases, including DPP-8, DPP-9, and fibroblast activation protein (FAP)-α.

Sep 27 2021
S9896 JNJ-67856633

JNJ-67856633 (JNJ-6633) is a potent, selective, allosteric inhibitor of MALT1 protease.

Sep 23 2021
S9909 ARP 100 ARP 100 (MMP-2 Inhibitor III, Compound 10a) is a potent and selective inhibitor of MMP-2 with an IC50 of 12 nM and displays less inhibitory activity at MMP-9, MMP-3, MMP-1 and MMP-7 with IC50s of 200 nM, 4500 nM, >50,000 nM and >50,000 nM respectively. Sep 01 2021
S5960 Dabigatran etexilate mesylate Dabigatran etexilate mesylate (Pradaxa, BIBR 1048MS, Dabigatran etexilate methanesulfonate) is an orally active prodrug of Dabigatran which is a reversible and selective, direct thrombin inhibitor (DTI). Dabigatran selectively and reversibly inhibits human thrombin with Ki of 4.5 nM and thrombin-induced platelet aggregation with IC50 of 10 nM. Apr 27 2021
S4432 Ixazomib Citrate (MLN9708) Ixazomib citrate (MLN9708, Ninlaro) is a prodrug of Ixazomib (MLN2238), which is a selective, orally bioavailable inhibitor of 20S proteasome that inhibits the chymotrypsin-like proteolytic (β5) site with IC50 of 3.4 nM and Ki of 0.93 nM, respectively. Ixazomib (MLN2238) also inhibits caspase-like (β1) and trypsin-like (β2) proteolytic sites with IC50 of 31 nM and 3500 nM, respectively. Apr 13 2021
S0042 Fulacimstat Fulacimstat (BAY1142524) is an orally available inhibitor of chymase with IC50 of 4 nM and 3 nM for human and hamster chymase enzyme, respectively. Mar 30 2021
S4426 Sacubitril hemicalcium salt Sacubitril (AHU-377) hemicalcium salt, a component of the heart failure medicine LCZ696, is a potent inhibitor of neprilysin (neutral endopeptidase, NEP). Mar 30 2021
S0479 ZK824859 ZK824859 is a potent, selective and orally bioavailable inhibitor of urokinase plasminogen activator (uPA) with IC50 of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively. Mar 15 2021
S3388 Sacubitrilat Sacubitrilat (Sac, LBQ-657) is an active inhibitor of neprilysin (NEP). Feb 09 2021
Microbiology
Catalog No. Product Name Information Added
E0052 Merafloxacin Merafloxacin (CI-934) is a fluoroquinolone antibacterial thats inhibit -1 frameshifting efficiency of SARS-CoV-2 and other betacoronaviruses. Oct 18 2021
S0793 ML188 ML188 is a non-covalent SARS-CoV 3CLpro inhibitor with IC50 of 1.5 μM. ML188 has antiviral activity. Sep 16 2021
E0005 Enfuvirtide Acetate Enfuvirtide Acetate (T20 Acetate, DP178 Acetate) is an HIV fusion inhibitor with ic50s of 13.63  nM and 30.21  nM on infection by HIV-1IIIB in MT-2 cells and HIV-1Bal in M7 cells, respectively. Aug 11 2021
S6090 JFD01307SC JFD01307SC ([(1,1-dioxidotetrahydrothien-3-yl)amino]acetic acid) shows activity against M.tuberculosis with minimum inhibitory concentrations (MICs) in the range of 8 to 16 µg/ml. JFD01307SC may targets enzymes involved in glutamine biosynthesis. Aug 11 2021
S7739 Telacebec (Q203) Telacebec (Q203, IAP6) is a novel antituberculosis drug that targets Mycobacterium tuberculosis cellular energy production through inhibition of the mycobacterial cytochrome bc1 complex. Telacebec (Q203, IAP6) is active against Mycobacterium tuberculosis H37Rv with MIC50 of 2.7 nM in culture broth medium. Jul 28 2021
S0754 Bisindolylmaleimide IV Bisindolylmaleimide IV (Arcyriarubin A, BIM IV, Compound 5/1a) is a potent inhibitor of protein kinase C (PKC) with IC50 of 0.55 μM. Bisindolylmaleimide IV also inhibits PKA with IC50 of 11.8μM. Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with IC50 of 0.2 μM. May 24 2021
S0081 DDD107498 DDD107498 (M-5717, DDD-498) is a P. falciparum translation elongation factor 2 inhibitor. DDD107498 exhibits a potent and novel spectrum of antimalarial activity against multiple life-cycle stages of the Plasmodium parasite. May 24 2021
S5235 Cefodizime Cefodizime (CEF, CDZ) is an aminothiazolyl cephalosporin with a broad spectrum of antibacterial activity. Apr 27 2021
S5979 2',3'-Dideoxyadenosine 2',3'-Dideoxyadenosine (ddA, ddAdo) is an anti-human immunodeficiency virus agent against human immunodeficiency virus (HIV) and human hepatitis B virus (HBV) replication. Apr 27 2021
S5330 Amikacin Sulfate Salt Amikacin (BAY 41-6551) sulfate, a semisynthetic analog of kanamycin, is an aminoglycoside antibiotic which is very active against most gram-negative bacteria including gentamicin- and tobramycin-resistant strains. Apr 27 2021
Apoptosis
Catalog No. Product Name Information Added
E0108 LQZ-7I LQZ-7I is a novel selectively inhibitor of survivin dimerization with IC50s of 4.8 µM and 3.1 µM in prostate cancer cell lines PC-3 and C4-2, respectively. LQZ-7I orally effectively inhibits xenograft tumor growth and induces survivin loss in tumors. Oct 18 2021
S0167 RO8994 RO8994 is a potent and selective small-molecule MDM2 inhibitor with IC50 values of 5 nM in HTRF binding assays and 20 nM in MTT proliferation assays, respectively. Sep 18 2021
S6709 Obatoclax (GX15-070)

Obatoclax (GX15-070) is an antagonist of Bcl-2 with an Ki of 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis.

Sep 10 2021
S3469 Shield-1 Shield-1 is a specific, cell-permeant and high-affinity ligand of FK506-binding protein-12 (FKBP). Shield-1 reverses the instability by binding to mutated FKBP (mtFKBP), allowing conditional expression of mtFKBP-fused proteins. Shield-1 stabilizes the entire fusion protein. Sep 01 2021
S9705 Apostatin-1 Apostatin-1 (Apt-1) is a novel TRADD inhibitor. Apostatin-1 binds to a pocket on the N-terminal TRAF2-binding domain of TRADD (TRADD-N). Apostatin-1 inhibits bortezomib-induced apoptosis and RIPK1-dependent apoptosis (RDA) with an IC50 of about 1 μM. Sep 01 2021
E0035 CP-31398 Dihydrochloride

CP-31398 Dihydrochloride stabilizes the active conformation of p53 and promotes p53 activity in cancer cell lines with mutant or wild-type p53.

Sep 01 2021
S9726 Rimiducid (AP1903) Rimiducid (AP1903) is a chemical protein dimerizer and binds tightly to the target FKBP fusion protein while binding minimally to the abundant natural FKBP. Rimiducid elicites potent and dose-dependent apoptosis of cells in culture expressing dimerizer-dependent Fas constructs, with an EC50 of ≈0.1 nM. Aug 23 2021
E0011 Linderalactone Linderalactone inhibits human lung cancer growth by modulating the expression of apoptosis-related proteins (Bax and Bcl-2) with an IC50 of 15 µM in A-549 cells. Linderalactone induces G2/M cell cycle arrest and could also suppress the JAK/STAT signalling pathway. Linderalactone can be isolated from Radix linderae. Aug 11 2021
S6078 ICCB-19 hydrochloride ICCB-19 hydrochloride is an inhibitor of TNFRSF1A Associated Via Death Domain (TRADD) with IC50 of 1.12 μM and 2.01 μM for protecting Velcade-induced apoptosis in Jurkat cells and protecting RDA in MEFs, respectively. ICCB-19 indirectly inhibits Receptor-interacting serine/threonine-protein kinase 1 (RIPK1). ICCB-19 effectively induces autophagy. Jun 22 2021
S9840 SRS16-86 SRS16-86, a novel third-generation ferrostatin, is an inhibitor of ferroptosis. Jun 07 2021
MAPK
Catalog No. Product Name Information Added
S0542 R1487 R1487 is an orally bioavailable and highly selective inhibitor of p38α with an ic50 value of 10 nM. Jul 16 2021
S6930 MK2 Inhibitor III   Jul 15 2021
S4484 Trametinib DMSO solvate Trametinib (GSK1120212, JTP-74057, Mekinist) DMSO solvate is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assay. Trametinib activates autophagy and induces apoptosis. Apr 07 2021
S8569 KO-947 KO-947 is a potent and selective inhibitor of ERK1/2 kinases. KO-947 blocks ERK signaling and proliferation of tumor cells exhibiting dysregulation of MAPK pathway signaling at low nanomolar concentrations. Dec 08 2020
S0872 ASTX-029 ASTX-029 is an orally bioavailable inhibitor of the extracellular signal-regulated kinases (ERK) 1 and 2, with potential antineoplastic activity. ASTX-029 inhibits ERK-dependent tumor cell proliferation and survival. Nov 03 2020
S6905 MCP110 MCP110 is an inhibitor of Ras/Raf-1 interaction. MCP110 disrupts the interaction of activated Ras with Raf and is potential for the treatment of human tumors. Sep 24 2020
S6882 HI-TOPK-032 HI-TOPK-032 is a potent and specific inhibitor of TOPK. HI-TOPK-032 also reduces ERK-RSK phosphorylation, regulates of the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells. Sep 24 2020
S6888 SEL201 SEL-201 (SLV-2436, SEL201-88) is a highly potent and ATP-competitive inhibitor of MNK1 and MNK2 with IC50 of 10.8  nM and 5.4 nM, respectively. Sep 10 2020
S9621 Donafenib (Sorafenib D3) Donafenib (Sorafenib D3, Bay 43-9006 D3, CM-4307) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 15 nM, 20 nM and 22 nM for Raf-1, mVEGFR-2, mVEGFR-3 and B-RAF, respectively. Jul 20 2020
S8896 BAY-885 BAY-885 is a highly potent and selective ERK5 inhibitor. Jul 20 2020
Angiogenesis
Catalog No. Product Name Information Added
E0041 Tolebrutinib (SAR442168) Tolebrutinib (SAR442168, PRN2246, BTKi'168, BTKi('168)) is an oral, CNS-penetrant, irreversible inhibitor of Bruton's tyrosine kinase (BTK) with IC50s of 0.4 nM and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. Oct 18 2021
E0047 Vodobatinib (K0706) Vodobatinib (K0706, SCO-088, SUN K706, SUN-K0706) is a novel BCR-ABL1 tyrosine kinase inhibitor with an IC50 of 7 nM. Vodobatinib exhibits activity against most BCR-ABL1 point mutants with IC50s of 167 nM, 154 nM,165 nM and 1967 nM for BCR-ABL1L248R, BCR-ABL1Y253H , BCR-ABL1E255V and BCR-ABL1T315I, respectively. Oct 18 2021
S6383 1-NM-PP1 1-NM-PP1 (PP1 Analog II, 1NM-PP1, analogue 9) is a potent inhibitor of Src family kinases with IC50 of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively. 1-NM-PP1 also inhibits CDK2-as1, CAMKII-as1 and c-Abl-as2 with IC50 of 5.0 nM, 8.0 nM and 120 nM, respectively. Jun 15 2021
S6966 MT-802 MT-802 is a potent PROTAC that induces Bruton's tyrosine kinase (BTK) knockdown. MT-802 recruits BTK to the cereblon E3 ubiquitin ligase complex to trigger BTK ubiquitination and degradation via the proteasome. MT-802 has potential for treatment of C481S mutant chronic lymphocytic leukemia (CLL). Jun 01 2021
S4895 Nilotinib hydrochloride monohydrate Nilotinib (AMN-107, Tasigna) hydrochloride monohydrate is a selective and orally bioavailable inhibitor of Bcr-Abl with IC50 < 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition. Apr 07 2021
S4944 Fostamatinib disodium hexahydrate Fostamatinib (R788) disodium (Tamatinib Fosdium) hexahydrate, a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM in a cell-free assay. Apr 07 2021
S8948 SRX3207 SRX3207 is an orally active dual inhibitor of Syk-PI3K with IC50 of 39.9 nM, 31200 nM, 3070 nM, 3070 nM, 244 nM, 388 nM, 9790 nM for Syk, Zap70, BRD41, BRD42, PI3K alpha, PI3K delta, PI3K gamma, respectively. SRX3207 blocks tumor immunosuppression and increases anti-tumor immunity. Mar 30 2021
S9715 Lanraplenib (GS-9876) Lanraplenib (GS-9876, GS-SYK) is a potent, highly selective and orally active inhibitor of Spleen Tyrosine Kinase (SYK) with IC50 of 9.5 nM. Lanraplenib inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans. Feb 22 2021
S8351 PT2399 PT2399 is a potent and orally available antagonist of HIF-2 that selectively disrupts the heterodimerization of HIF-2α with HIF-1β. Dec 23 2020
S0373 CZC-8004 CZC-8004 (CZC-00008004) is a pan-kinase inhibitor that binds a range of tyrosine kinases including ABL kinase. Nov 27 2020
Stem Cell & Wnt
Catalog No. Product Name Information Added
E0033 IWP-4

IWP-4 is a potent Wnt/β-catenin signaling pathway inhibitor with an IC50 of 25 nM.

Sep 01 2021
S5992 Heparan Sulfate Heparan sulfate (HS, Heparitin sulfate, Alpha-idosane, HHS 5, N-Acetylheparan Sulfate, Suleparoid, Tavidan), a constituent of HS proteoglycans (HSPGs), is a linear polysaccharide present on the cell surface. Heparan sulfate influences the binding affinity of intestinal epithelium cells (IECs) to Wnt, thereby promoting activation of canonical Wnt signaling and facilitating regeneration of small intestinal crypts after epithelial injury. May 17 2021
S9828 WAY-262611 WAY-262611 (BML-WN110, Compound 5) is a beta-catenin (β-Catenin) agonist that increases bone formation rate with EC50 of 0.63 μM in TCF-Luciferase assay. WAY-262611 is also an inhibitor of dickkopf 1 (DKK1). May 06 2021
S0733 Tegatrabetan (BC-2059) Tegatrabetan (BC2059) is an antagonist of β-Catenin. Tegatrabetan (BC2059) treatment disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1) and proteasomal degradation and declines in the nuclear levels of β-catenin. Mar 08 2021
S6961 Foxy-5 Foxy-5, a Wnt-5a mimicking hexapeptide, is a WNT signalling pathway modulator potentially for the treatment of metastatic breast cancer, prostate cancer and colorectal cancer. Jan 11 2021
S2962 NP-G2-044 NP-G2-044 is a potent, orally active inhibitor of the actin-bundling activity of fascin with IC50 of ~0.2 μM. NP-G2-044 blocks tumor metastasis and increases antitumor immune response. Nov 30 2020
S6901 MSAB MSAB is a selective inhibitor of Wnt/β-catenin signaling that binds to β-catenin, promoting its degradation, and specifically downregulates Wnt/β-catenin target genes. MSAB shows potent anti-tumor effects. Nov 27 2020
S8968 PRI-724 PRI-724 (C-82 prodrug, ICG-001 analog) is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP. Aug 24 2020
S7981 CCT251545 CCT251545 is a potent, orally bioavailable inhibitor of WNT signaling with IC50 of 5 nM in 7dF3 cells. CCT251545 also act as a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. Aug 18 2020
S0458 KY1220 KY1220 is a small molecule that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway with IC50 of 2.1 μM in HEK293 reporter cells. Jul 14 2020
Ubiquitin
Catalog No. Product Name Information Added
S6943 IU1-47 IU1-47 is a potent and specific inhibitor of USP14 with an IC50 of 0.6 μM. IU1-47 shows ∼33-fold selectivity for USP14 over USP5 (IsoT). Sep 10 2021
S8300 CC-885

CC-885 is a novel cereblon (CRBN) modulator. CC-885 selectively promotes CRBN- and p97-dependent PLK1 ubiquitination and degradation.

Sep 01 2021
S9832 CC-90009 CC-90009 is a novel cereblon (CRBN) E3 ligase modulator and specifically targets GSPT1 (G1 to S phase transition 1) for proteasomal degradation. Aug 19 2021
S6883 HBX 19818 HBX19818 is a specific inhibitor of USP7 with an IC 50 of 28.1 μM. Jul 23 2021
S2881 Homo-PROTAC cereblon degrader 1 Homo-PROTAC cereblon degrader 1 (OUN20985) is a potent and efficient cereblon (CRBN) degrader with minimal effects on IKZF1 and IKZF3. Jul 06 2021
S4453 NPD8733 NPD8733 is an inhibitor of cancer cell-enhanced fibroblast migration that specifically binds to valosin-containing protein (VCP)/p97, a member of the ATPase-associated with diverse cellular activities (AAA+) protein family. Jun 15 2021
S0322 BC-1215 BC-1215 is an inhibitor of F-box protein 3 (Fbxo3, a ubiquitin E3 ligase component) with IC50 of 0.9 μg/mL and LC50 of 87 μg/ml for IL-1β release. BC-1215 inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1-6. Jun 01 2021
S8967 XL177A XL177A is a potent, selective and irreversible inhibitor of Ubiquitin specific peptidase 7 (USP7) with IC50 of 0.34 nM. May 24 2021
S9724 SZL P1-41 SZL P1-41 (compound #25) is a specific inhibitor of S-phase kinase-associated protein 2 (Skp2) that indeed binds to Skp2, prevents Skp2-Skp1 interaction and inhibits Skp2 SCF E3 ligase activity, which consequently suppresses survival of cancer cells and cancer stem cells. SZL P1-41 causes higher apoptosis rates in cancer cells. Apr 27 2021
S3502 (S,R,S)-AHPC-PEG4-NH2 hydrochloride (S,R,S)-AHPC-PEG4-NH2 hydrochloride (VH032-PEG4-NH2 hydrochloride, VHL Ligand-Linker Conjugates 4 hydrochloride, E3 ligase Ligand-Linker Conjugates 7) is a PROTAC E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker. Feb 08 2021
Neuronal Signaling
Catalog No. Product Name Information Added
S9498 5-BDBD

5-BDBD is a potent P2X4R selective antagonist with an IC50 of 0.75 μM when applied for 2 min prior and during ATP stimulation.

Sep 27 2021
S6985 Varenicline Varenicline is highly selective and blocks more potently to α4β2 receptors than to other common nicotinic receptors (>500-fold α3β4, >3,500-fold α7, >20,000-fold α1βγδ), or to non-nicotinic receptors and transporters (>2,000-fold). Varenicline also acts as an agonist of 5-HT3 serotonine receptors. Jul 26 2021
S0446 TCN 201 TCN-201 is a selective GluN1/GluN2A (NR1/NR2A) NMDA receptor antagonist with pIC50 6.8 for NR1/NR2A and <4.3 for NR1/NR2B (GluN1/GluN2B),respectively. Jul 23 2021
S6853 ONC206 ONC206 is a selective antagonist of dopamine D2-like receptors (DRD2/3/4) with broad-spectrum anti-tumor activity. May 24 2021
S4358 Pimozide Pimozide (Orap, R6238) is an antagonist of Dopamine Receptors with Ki of 0.83 nM, 3.0 nM and 6600 nM for dopamine D3, D2 and D1 receptors, respectively. Pimozide also exhibits binding affinity at α2-adrenoceptor and 5-HT1A with Ki of 360 nM and 310 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity. May 24 2021
S3520 AZ10606120 dihydrochloride AZ10606120 dihydrochloride (2HCl) is a potent and selective antagonist for P2X7 receptor (P2X7R) with IC50 of ~10 nM. AZ10606120 dihydrochloride exhibits anti-depressant effects and reduces tumour growth. May 18 2021
S4359 Carbamoylcholine chloride (Carbachol) Carbamoylcholine chloride (Carbachol, Carbamylcholine chloride, Carbastat, Miostat) is a cholinergic agonist that mimics the effect of acetylcholine on both the muscarinic and nicotinic receptors. May 10 2021
S0717 Varenicline (CP 526555) dihydrochloride Varenicline (CP 526555, Chantix, Champix) dihydrochloride is a potent, partial agonist of α4β2 nicotinic acetylcholine receptor (nAChR) and α3β4 nAChR with EC50 of 2.3 μM and 55 μM, respectively. Varenicline dihydrochloride is a potent, full agonist of α7 nAChRs with EC50 of 18 μM. Varenicline is a prescription medication used for smoking cessation. May 07 2021
S3913 Pimethixene maleate Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively. Apr 27 2021
S5770 Pizotifen Pizotifen (Pizotyline, BC-105) is a potent antagonist of 5-Hydroxytryptamine (5-HT, Serotonin) 5-HT2 receptor with a high affinity for 5-HT1C binding site. Apr 27 2021
Others
Catalog No. Product Name Information Added
E0069 DFHBI DFHBI is a mimic of green fluorescent protein (GFP) fluorophore and binds to RNA aptamers. DFHBI can be used for imaging RNA in living cells. Oct 18 2021
E0112 INH154 INH154 is a potent inhibitor of Nek2 and Hec1 binding. NH154 binds to Hec1, thus blocking Hec1 phosphorylation by NEK2, and kills cancer cells at the nanomolar range. Oct 18 2021
E0076 Simufilam dihydrochloride Simufilam (PTI-125) Dihydrochloride is a small molecule modulator that preferentially binds altered FLNA and restores its native conformation, restoring receptor and synaptic activities and reducing its α7nAChR/TLR4 associations and downstream pathologies. Oct 18 2021
S6177 CP 43 Cp 43 (Compound 43, TAO Kinase inhibitor 1, TAOK inhibitor 43) is a ATP-competitive and selective TAO Kinase inhibitor with IC50s of 11 nM and 15 nM for TAOK1 and TAOK2, respectively. Oct 18 2021
S3191 Azumolene Azumolene (EU4093 free base), an equipotent dantrolene analog, is a ryanodine receptor (RyR) modulator that inhibits the calcium-release. Oct 18 2021
S6396 HOIPIN-1 HOIPIN-1 (JTP-0819958, HOIP inhibitor-1) is a linear ubiquitin chain assembly complex (LUBAC) inhibitor with an IC50 of 2.8 μM for inhibiting the in vitro linear ubiquitination activity of the petit-LUBAC. Oct 18 2021
S6318 Biotinyl Tyramide

Biotinyl Tyramide is a biotin derivative used for signal amplification in IHC and fluorescent in situ hybridization (ISH).

Oct 14 2021
S6946 Gap19 Gap19 is a nonapeptide derived from the cytoplasmic loop (CL) of Cx43 and acts as a selective connexin 43 (Cx43) hemichannel blocker. Gap19 blocks Cx43 hemichannels without inhibiting gap junctions (GJs) at IC50 of 6.5 μM when applied intracellulary. Sep 28 2021
E0120 2-Bromohexadecanoic acid

2-Bromohexadecanoic acid (2-BP, 2-bromopalmitate) is a nonmetabolisable analogue of palmitate and acts as a palmitoylation inhibitor. 2-Bromohexadecanoic acid can directly and irreversibly inhibit the palmitoyltransferase activity of all DHHC (Asp-His-His-Cys) proteins.

Sep 27 2021
E0038 [SER140]-PLP(139-151)

[SER140]-PLP(139-151) is a polypeptide fragment of the lipid protein of myelin.

Sep 27 2021