2. Apoptosis
    Immunology/Inflammation
    Autophagy
  3. FKBP
    Apoptosis
  4. Rimiducid

Rimiducid  (Synonyms: AP1903)

Cat. No.: HY-16046 Purity: 99.46%
COA Handling Instructions

Rimiducid (AP1903) is a dimerizer agent that acts by cross-linking the FKBP domains. Rimiducid (AP1903) dimerizes the Caspase 9 suicide switch and rapidly induces apoptosis.

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

Rimiducid Chemical Structure

Rimiducid Chemical Structure

CAS No. : 195514-63-7

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2 mg USD 252 In-stock
5 mg USD 384 In-stock
10 mg USD 564 In-stock
50 mg USD 1680 In-stock
100 mg USD 2280 In-stock
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Customer Review

Based on 26 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Rimiducid purchased from MCE. Usage Cited in: Nat Commun. 2020 Apr 2;11(1):1625.  [Abstract]

    Fusion constructs are transiently expressed and treated with DMSO or AP1903 as in the figure. 48 hrs after transfection, cells are immunostained with anti-FLAG (mAire) and anti-PML.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Rimiducid (AP1903) is a dimerizer agent that acts by cross-linking the FKBP domains. Rimiducid (AP1903) dimerizes the Caspase 9 suicide switch and rapidly induces apoptosis.

    IC50 & Target

    EC50: 0.1 nM (FKBP, in HT1080 cells)[1]
    Fas receptor[1]
    In Vitro

    The human fibrosarcoma line HT1080 is engineered to express stably a fusion protein comprising a myristoylation sequence, two copies of F36V-FKBP, and the human first apoptosis signal (Fas) intracellular domain. Rimiducid (AP1903) elicits potent and dose-dependent apoptotic death of these engineered cells in culture, with an EC50 of ≈0.1 nM[1]. Maximal killing occurred in the presence of 3 to 10 nM Rimiducid (AP1903), and the IC50 is approximately 0.2 nM. LV′VFas-transduced T lymphocytes expressing high levels of CD25 (top panel) are eliminated by with 66%±7.5% (n=10) efficiency. When cells are examined after CD25 expression returned to basal levels, 63%±4.7% (n=9) killing is observed after Rimiducid treatment[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    In Vivo

    Rimiducid (AP1903; i.v.,0.01, 0.1, 1, 10, and 100 mg/kg) elicits a dose-dependent decrease in serum human GH levels, with a half-maximal effective dose of 0.4±0.1 mg/kg[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    1411.63

    Appearance

    Solid

    Formula

    C78H98N4O20
    CAS No.
    SMILES

    COC1=CC=C(CC[[email protected]@H](OC([[email protected]@H]2CCCCN2C([[email protected]@H](CC)C3=CC(OC)=C(OC)C(OC)=C3)=O)=O)C4=CC=CC(OCC(NCCNC(COC5=CC([[email protected]@H](CCC6=CC=C(OC)C(OC)=C6)OC([[email protected]@H]7CCCCN7C([[email protected]](C8=CC(OC)=C(OC)C(OC)=C8)CC)=O)=O)=CC=C5)=O)=O)=C4)C=C1OC
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years

    *The compound is unstable in solutions, freshly prepared is recommended.
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (35.42 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 0.7084 mL 3.5420 mL 7.0840 mL
    5 mM 0.1417 mL 0.7084 mL 1.4168 mL
    10 mM 0.0708 mL 0.3542 mL 0.7084 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (1.77 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.81%

    COA (252 KB) LCMS (120 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1][2]

    Cloned HT1080 cell lines (ATCC CCL-121) retrovirally transduced with Fas constructs are prepared. Cell viability after overnight incubation with Rimiducid (0.01 nM, 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM) is measured by Alamar Blue assay[1]. For annexin V assays, sorted LV′VFas-transduced T cells (2×106 cells/mL) are incubated with 10 nM Rimiducid. Analyzed by flow cytometry[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice[1]
    Male nu/nu mice are used. For injection, HTFasGH-3 cells are harvested from tissue culture dishes in PBS/0.1% glucose/10 mM EDTA, washed, and resuspended in PBS/0.1% BSA/0.1% glucose at a concentration of 2×107 cells/mL. Between 2 and 4×106 cells are implanted into two i.m. sites. After 24 h, mice are administered i.v. Rimiducid at 2 mL/kg. After a further 24 h mice are killed and serum human GH concentrations are determined by ELISA.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    Rimiducid195514-63-7AP1903AP 1903AP-1903FKBPApoptosisFK506-binding proteinInhibitorinhibitorinhibit

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