1. MAPK/ERK Pathway
  2. JNK

CC-930 (Synonyms: Tanzisertib)

Cat. No.: HY-15495 Purity: 99.98%
Handling Instructions

CC-930 is a potent JNK1/JNK2/JNK3 inhibitor with IC50 values of 61/7/6 nM, respectively, and used for the treatment of fibrotic and infammatory indications.

For research use only. We do not sell to patients.

CC-930 Chemical Structure

CC-930 Chemical Structure

CAS No. : 899805-25-5

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 119 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 840 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 1440 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

    CC-930 purchased from MCE. Usage Cited in: Science. 2017 Dec 1;358(6367). pii: eaan4368.

    Kinobead western Blot readout for selected inhibitor:protein combinations.

    CC-930 purchased from MCE. Usage Cited in: Science. 2017 Dec 1;358(6367). pii: eaan4368.

    Immunoblot analysis in MV-4-11 cells and MOLM-13, FLT3-WT and FLT3-ITD transfected HEK293 cells, and Ba/F3 FLT3-ITD cells revealed FLT3 target engagement for Golvatinib and Cabozantinib.

    CC-930 purchased from MCE. Usage Cited in: Nat Cell Biol. 2017 Jun;19(6):698-710.

    Immunoblot analysis of phospho-JNK of splenic XBP1ΔDC CD11c+ cells of XBP1ΔDC mice treated with CC-930 or vehicle. Total JNK and β-tubulin levels serve as loading control. Each lane represents one mouse.

    View All JNK Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    CC-930 is a potent JNK1/JNK2/JNK3 inhibitor with IC50 values of 61/7/6 nM, respectively, and used for the treatment of fibrotic and infammatory indications.

    IC50 & Target[1]

    JNK3

    6 nM (IC50)

    JNK2

    7 nM (IC50)

    JNK1

    61 nM (IC50)

    In Vitro

    CC-930 inhibits the formation of phospho-cJun in human PBMC stimulated by phorbol-12-myristate-13-acetate and phytohemeagglutinin (IC50=1 μM)[1]. CC-930 (1-2 μM) substantially reduces hepatocyte apoptosis and necrosis, abrogates apoptosis and necrosis in FC-loaded WT hepatocytes[2]. CC-930 blocks the JNK pathway that is activated by pro-fibrotic cytokines in systemic sclerosis[3].

    In Vivo

    CC-930 (10 and 30 mg/kg, p.o.) inhibits the production of TNFa by 23% and 77% in the acute rat LPS-induced TNFa production PK-PD model[1]. CC-930 (150 mg/kg) prevents the development of fibrosis in different models, but can also induce the regression of pre-existing fibrosis[3].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.2300 mL 11.1498 mL 22.2995 mL
    5 mM 0.4460 mL 2.2300 mL 4.4599 mL
    10 mM 0.2230 mL 1.1150 mL 2.2300 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [3]

    Systemic sclerosis (SSc) fibroblasts are incubated with 1 µM CC-930 in 96-well plates for 20 h. Then MTT is added at a final concentration of 1 mg/mL, and the cells are further incubated at 37°C for 4 h. Mock-treated fibroblasts are used as controls, and all other results are normalised to untreated cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    To evaluate the regression of fibrosis on inhibition of JNK, a modified model of bleomycin-induced dermal fibrosis is used. In this model, treatment is initiated 3 weeks after the beginning of the challenge with bleomycin, when significant dermal fibrosis is already established. The outcome of six different groups with a total number of 40 mice is analysed. The first group of mice receive subcutaneous injections of NaCl for 6 weeks. The second group is injected for 3 weeks with bleomycin followed by injections of NaCl for another 3 weeks to analyse the degree of fibrosis before treatment, and to control the spontaneous regression of fibrosis. The third group of mice is killed after 6 weeks of injections with bleomycin. The fourth and the fifth group are treated with CC-930 at doses of 50 mg/kg and 150 mg/kg for the last 3 weeks of continuous challenge with bleomycin for 6 weeks. The sixth group is a positive control group consisting of mice challenged with bleomycin for 6 weeks and treated in parallel with imatinib at doses of 50 mg/kg for the last 3 weeks. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    448.44

    Formula

    C₂₁H₂₃F₃N₆O₂

    CAS No.

    899805-25-5

    SMILES

    O[[email protected]]1CC[[email protected]](NC2=NC=C3N=C(NC4=C(F)C=C(F)C=C4F)N([[email protected]@H]5COCC5)C3=N2)CC1

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 33 mg/mL

    CC-930 is dissolved in DMSO at a concentration of 50 mg/mL; a 12.5% solution is made in PEG400[4].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

    Purity: 99.98%

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    Product Name:
    CC-930
    Cat. No.:
    HY-15495
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