2. Immunology/Inflammation
  3. STING
  4. SB24011

SB24011 is a STING modulator and a TRIM29-STING protein-protein interaction inhibitor. SB24011 blocks TRIM29-induced K48-linked specific ubiquitination by binding to STING, thereby upregulating intracellular STING protein levels. SB24011 enhances inflammatory cytokine expression and STING-mediated immune responses, and exhibits abscopal antitumor activity that promotes tumor regression and activates T cell infiltration. When combined with STING agonists or anti-PD1 antibodies, SB24011 synergistically enhances antitumor responses. SB24011 is suitable for research related to colon cancer and melanoma.

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SB24011

SB24011 Chemical Structure

CAS No. : 1497415-41-4

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SB24011 Related Antibodies

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Description

SB24011 is a STING modulator and a TRIM29-STING protein-protein interaction inhibitor. SB24011 blocks TRIM29-induced K48-linked specific ubiquitination by binding to STING, thereby upregulating intracellular STING protein levels. SB24011 enhances inflammatory cytokine expression and STING-mediated immune responses, and exhibits abscopal antitumor activity that promotes tumor regression and activates T cell infiltration. When combined with STING agonists or anti-PD1 antibodies, SB24011 synergistically enhances antitumor responses. SB24011 is suitable for research related to colon cancer and melanoma[1][2][3].

In Vitro

SB24011 (5-20 μM; 24 h) shows no cytotoxicity in Raw264.7 murine macrophage-like cells[2].
SB24011 (5-20 μM; 18 h; 10 μM; 18, 24 h) upregulates cellular STING protein levels in A431 human skin squamous carcinoma cells[2].
SB24011 (20 μM; 3, 6 h) enhances cGAMP-induced activation of the STING downstream signaling pathway (phosphorylation of STING, TBK1, IRF3) in Raw264.7 murine macrophage-like cells[2].
SB24011 (20 μM; 3, 6 h) augments cGAMP-induced proinflammatory cytokine mRNA expression (ifnb, il6, il15) in Raw264.7 murine macrophage-like cells[2].
SB24011 (5-20 μM) dose-dependently augments cGAMP-induced proinflammatory cytokine mRNA expression (ifnb, il6) in Raw264.7 murine macrophage-like cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SB24011 Related Antibodies

Western Blot Analysis[2]

Cell Line: A431 human skin squamous carcinoma cells
Concentration: 5-20 μM (18 h incubation); 10 μM (18, 24 h incubation)
Incubation Time: 18 h (5,10,20 μM); 18 h, 24 h (10 μM)
Result: Increased cellular STING protein levels in a time- and dose-dependent manner.
Elevated the STING/actin band ratio by 2.1-, 2.9-, and 3.2-fold at 5, 10, and 20 μM, respectively, compared to vehicle.

Western Blot Analysis[2]

Cell Line: Raw264.7 murine macrophage-like cells
Concentration: 20 μM
Incubation Time: 3 h, 6 h
Result: Enhanced cGAMP-induced phosphorylation of STING, TBK1, and IRF3 at both 3 h and 6 h post-treatment.

Real Time qPCR[2]

Cell Line: Raw264.7 murine macrophage-like cells
Concentration: 20 μM
Incubation Time: 3 h, 6 h
Result: Enhanced cGAMP-induced mRNA expression of ifnb (310% increase at 3 h, 30% increase at 6 h), il-6 (1100% increase at 3 h, 3500% increase at 6 h), il-15 (1800% increase at 3 h, 2700% increase at 6 h), and an additional cytokine (800% increase at 3 h, 1500% increase at 6 h) at 3 h compared to cGAMP alone.
Observed similar enhancements at 6 h.
Parmacokinetics
Species Dose Route T1/2 AUC0-∞
Mice[2] 2.5 mg/kg i.v. 0.26 h 340.50 ng·h/mL
Mice[2] 0.15 mg/kg s.c. 3.75 h 24.93 ng·h/mL
In Vivo

SB24011 (1-3 μg per head; intratumoral injection; first and third of four total injections; once every 2 days over 8 days) dose-dependently potentiates cGAMP-mediated anticancer immunity in BALB/c mice with CT26 colorectal tumors, enhancing tumor-infiltrating effector T cell activity and inducing a systemic abscopal effect[2].
SB24011 (1-3 μg per head; intratumoral injection; first and third of four total injections; once every 2 days over 8 days) dose-dependently potentiates cGAMP-mediated anticancer immunity in wild-type C57BL/6J mice with B16F10 melanoma, reducing tumor growth and enhancing effector T cell activity[2].
SB24011 (3 μg per head; intratumoral injection; last two of three total cGAMP injections)-mediated potentiation of cGAMP anticancer efficacy is strictly dependent on functional STING in C57BL/6J mice with B16F10 melanoma[2].
SB24011 (1-3 μg per head; intratumoral injection; once every 4 days) dose-dependently potentiates anti-PD-1 antibody-mediated anticancer immunity in BALB/c mice with CT26 colorectal tumors, producing synergistic tumor growth inhibition[2].
SB24011 promotes tumor regression and T-cell infiltration in syngeneic mouse cancer models, and induces the abscopal effect when combined with anti-PD-1 treatment[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c mice (flanks implanted with CT26 murine colon carcinoma cells, tumors grown to ~100 mm3)[2]
Dosage: 1 μg per head; 3 μg per head
Administration: intratumoral injection; first and third of four total injections (once every 2 days over 8 days)
Result: Reduced tumor volume and mass in a dose-dependent manner.
Increased the proportion of CD3+ T cells (of CD45+ cells) and CD8+ T cells (of CD45+ cells), reduced the proportion of total myeloid-derived suppressor cells (MDSCs, of CD45+ cells), and increased the proportion of CD8+ T cells expressing IFN-γ, granzyme B, and perforin (of CD45+ cells) compared to cGAMP alone.
Increased intracellular STING levels (measured as mean fluorescence intensity) in M1 macrophages and dendritic cells within the tumor microenvironment.
Induced superior distal tumor growth inhibition (abscopal effect).
Molecular Weight

614.69

Formula

C34H38N4O7
CAS No.
Appearance

Solid

Color

Yellow to orange

SMILES

O=C(NC[C@H]1OCCC1)C2=CC=C(N3[C@H](C(C)C)C(N(CC4=CC=C(O)C=C4)C(CC5=CC=C(OC)C=C5)=C3)=O)C([N+]([O-])=O)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation

Purity: 99.7%

SDS (251 KB)

COA (250 KB) Elemental Analysis Report (108 KB)

Handling Instructions (2659 KB)
References
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SB24011 Related Classifications

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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.

Keywords:

SB240111497415-41-4SB 24011SB-24011STINGStimulator of Interferon GenesTMEM173MITAERISMPYSTRIM29-STING protein-protein interactionmelanomacolon carcinomaTRIM29K48 linkage-specific ubiquitinationRaw264.7 cellsanti-PD1 antibodyinflammatory cytokineT-cellInhibitorinhibitorinhibit

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