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CTX0294885 chemical structureDC7904

CTX0294885

CTX-0294885 is a novel broad-spectrum kinase inhibitor. CTx-0294885 exhibits inhibitory activity against a broad range of kinases in vitro. Use of a quantitative proteomics approach confirmed the selectivity of…

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SGI-1027 chemical structureDC7293

SGI-1027

SGI-1027 is a DNA methyltransferase (DNMT) inhibitor, with IC50s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate.

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Tranylcypromine HCl chemical structureDC8710

Tranylcypromine HCl

Tranylcypromine HCl is an inhibitor of monoamine oxidase (MAO) and prostacyclin synthase, potently suppresses the enzymatic activity of Lysine-Specific Demethylase 1 (LSD1) (IC50 <2 μM for BHC110/LSD1).

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JIB-04 chemical structureDC7437

JIB-04

JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC50s of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively.

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Apatinib Mesylate chemical structureDC4101

Apatinib Mesylate

Apatinib is a highly selective VEGFR2 inhibitor with an IC50 of 1 nM. Apatinib also potently suppresses the activities of Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively.

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D927 chemical structureDC60864

D927

D927 is a molecular glue and promotes glucose uptake in the absence of insulin. D927 also increases the affinity of RAS binding to PI3Kα by ~500-fold. In vivo, D927 mimicks the effects of insulin and rapidly lowers…

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IT 901 chemical structureDC10768

IT 901

IT-901 is an orally active and potent NF-κB subunit c-Rel inhibitor with an IC50 of 0.1 µM, 3 μM for NF-κB DNA binding and c-Rel DNA binding, respectively. IT-901, a bioactive naphthalenethiobarbiturate derivative, has…

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GLPG0187 chemical structureDC10034

GLPG0187

GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM.

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Cediranib chemical structureDC3170

Cediranib

Cediranib maleate (AZD-2171 maleate) is a highly potent, orally available VEGFR tyrosine kinase inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.

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Belinostat (PXD101) chemical structureDC7082

Belinostat (PXD101)

Belinostat inhibits the growth of tumor cells (A2780, HCT116, HT29, WIL, CALU-3, MCF7, PC3 and HS852) with IC50 from 0.2-0.66 μM. PD101 shows low activity in A2780/cp70 and 2780AD cells, which are cisplatin and…

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Favipiravir (T-705) chemical structureDC5105

Favipiravir (T-705)

Favipiravir is a novel viral RNA polymerase inhibitor, it is phosphoribosylated by cellular enzymes to its active form, Favipiravir-ribofuranosyl-5′-triphosphate (RTP). Favipiravir-RTP inhibits the influenza viral…

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HPGDS-inhibitor-1 chemical structureDC7424

HPGDS-inhibitor-1

HPGDS inhibitor 1 is a novel and selective Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50 Value of 0.7 nM.IC50 Value: 0.7 nM [1]Target: HPGDSHPGDS inhibitor 1 was elected for further profiling…

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OF-1 chemical structureDC7850

OF-1

OF-1 is a selective BRPF1B and BRPF2 bromodomain inhibitor with Kd values of 100 nM/500 nM for BRPF1B/BRPF2; 39-fold selectivity over BRD4.

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E7080 (Lenvatinib) chemical structureDC7116

E7080 (Lenvatinib)

Lenvatinib is an oral, multi-targeted tyrosine kinase inhibitor with IC50s of 4 and 5.2 nM for VEGFR2(KDR) and VEGFR3(Flt-4), respectively. Lenvatinib is less potent against VEGFR1/Flt-1 and shows approximately 10-fold…

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NSC348884 chemical structureDC9641

NSC348884

NSC348884 is a nucleophosmin inhibitor disrupts oligomer formation and induces apoptosis, inhibits cell proliferation at an IC50 of 1.7-4.0 μM in distinct cancer cell lines.

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Clozapine N-oxide chemical structureDC7991

Clozapine N-oxide

Clozapine N-oxide (CNO) is a major metabolite of the anti-psychotic drug clozapine. Clozapine N-oxide is a agonist for the chemogenetic Designer Receptors Exclusively Activated by Designer Drug (DREADD) system.

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SB1317(TG-02) chemical structureDC7493

SB1317(TG-02)

SB1317 is a potent inhibitor of CDK2, JAK2, and FLT3 for the treatment of cancer, with IC50 of 13, 73, and 56 nM for CDK2, JAK2 and FLT3, respectively.

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Kobe0065 chemical structureDC7443

Kobe0065

Kobe0065 is a novel and effective inhibitor of Ras-Raf interaction, competitively inhibiting the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46±13 μM.

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EPZ011989 chemical structureDC7927

EPZ011989

EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.IC50 value: < 3 nM ( Ki for wt…

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CFTRinh 172 chemical structureDC7100

CFTRinh 172

CFTR(inh)-172 is a potent and selective blocker of the CFTR chloride channel; reversibly inhibited CFTR short-circuit current in less than 2 minutes with a Ki of 300 nM.

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Ribociclib (LEE011) chemical structureDC7453

Ribociclib (LEE011)

LEE011, as dual CDK4/CDK6 inhibitor, significantly inhibits the growth of 12 of 17 neuroblastoma cell lines with mean IC50 of 307 nM. The growth inhibition of neuroblastoma cell lines is primarily cytostatic and is…

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PYR 41 chemical structureDC7257

PYR 41

PYR-41 is a specific and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with no or little activity at E2.

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SNX-5422(PF04929113) chemical structureDC9948

SNX-5422(PF04929113)

SNX-5422 (PF-04929113), a prodrug of SNX-2112, is an orally active Hsp90 inhibitor, with a Kd of 41 nM, and also induces Her-2 degradation, with an IC50 of 37 nM.

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YM201636 chemical structureDC7343

YM201636

YM-201636 is a potent and selective PIKfyve inhibitor with an IC50 of 33 nM. YM-201636 also inhibits p110α with IC50 of 3.3 μM.

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