Cat. No.: HY-189364

(DL)-3,5-Dimethyltyrosine

Name: (DL)-3,5-Dimethyltyrosine
Brand: MedChemExpress
SKU: HY-189364
Availability: PreOrder

(Synonyms: SMC247-9)

(DL)-3,5-Dimethyltyrosine (SMC247-9) is a selective APOBEC3B inhibitor optimized from SMC247, with an IC₅₀ of 50 pM. (DL)-3,5-Dimethyltyrosine binds to the APOBEC3B protein, reduces intracellular APOBEC3B protein abundance partially through a lysosome-dependent pathway, enhances IL-15 expression in tumor cells, and relieves the suppression of CD8⁺ T cells by tumor cells in an IL-15-dependent manner. (DL)-3,5-Dimethyltyrosine attenuates tumor- and macrophage-derived chemokine-mediated macrophage chemotaxis and inhibits pathological myeloid inflammatory signaling. (DL)-3,5-Dimethyltyrosine inhibits tumor growth in the immune checkpoint blockade-responsive MC38 syngeneic mouse model and produces synergistic effects with anti-PD-L1 in the immune checkpoint blockade-resistant TC-1 tumor model; it also ameliorates anti-PD-1-exacerbated DSS-induced colitis-like intestinal inflammatory injury. (DL)-3,5-Dimethyltyrosine can be used in research related to tumor immunotherapy.

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

CAS No.: 88262-44-6
Formula: C₁₁H₁₅NO₃
Molecular Weight:209.24

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

(DL)-3,5-Dimethyltyrosine Chemical Structure

CAS No.: 88262-44-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

IL-15

IL-6

TNF-α

All Interleukin Related Isoforms :

All TNF Receptor Isoforms :

In Vitro

OthersAdaptive ImmunityCytokines & Chemokines

Others

(DL)-3,5-Dimethyltyrosine (SMC247-9) is a potent inhibitor of recombinant APOBEC3B enzymatic activity with an IC₅₀ of 50 pM; it preferentially targets APOBEC3B with approximately 340-fold selectivity over APOBEC3A; it exhibits strong direct binding affinity for recombinant APOBEC3B with a K_D of 0.3 nM^[1].
(DL)-3,5‑Dimethyltyrosine is competitively inhibited for APOBEC3B binding by ssDNA substrate, yielding a K_D of 5.4 μM in the presence of 100 μM ssDNA^[1].
(DL)-3,5-Dimethyltyrosine (10 μM; 24 h) reduces APOBEC3B protein abundance in KYSE70 cells, potentially through a lysosome-associated turnover process^[1].
(DL)-3,5-Dimethyltyrosine (100 μM; 5 min heating) directly binds APOBEC3B in KYSE70 cell lysates^[1].
(DL)-3,5-Dimethyltyrosine (0.01-100 μM; 24-72 h) shows no cytotoxicity in KYSE70 cells^[1].
(DL)-3,5-Dimethyltyrosine (10 μM; 48 h) decreases APOBEC3B mRNA and increases IL-15 mRNA expression in KYSE70 cells, and promotes IL-15 secretion by KYSE70 cells^[1].

Adaptive Immunity

Cytokines & Chemokines

(DL)-3,5-Dimethyltyrosine (10 μM; 48 h pretreatment, 72 h coculture) reprograms the KYSE70 secretory microenvironment to promote IL-15-related CD8⁺ T cell proliferation and effector function; the induced immune remodeling effect is further enhanced by PD-L1 blockade in a human tumor-conditioned medium model^[1].

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

Western Blot Analysis^[1]

Cell Line:

KYSE70
Concentration:

10 μM
Incubation Time:

24 h
Result:

Reduced APOBEC3B protein levels in KYSE70 cells.
CQ partially restored APOBEC3B protein abundance, whereas MG132 (HY-13259) showed no obvious rescue effect.

Cell Viability Assay^[1]

Cell Line:

KYSE70
Concentration:

0.01, 0.1, 1, 10, 100 μM
Incubation Time:

24, 48, 72 h
Result:

Had no obvious impact on KYSE70 cell viability at concentrations up to 10 μM over 72 h.

Real Time qPCR^[1]

Cell Line:

KYSE70
Concentration:

10 μM
Incubation Time:

48 h
Result:

Reduced APOBEC3B mRNA expression while increasing IL-15 mRNA expression.

ELISA Assay^[1]

Cell Line:

KYSE70
Concentration:

10 μM
Incubation Time:

48 h
Result:

Increased IL-15 secretion after SMC247-9 treatment.

Cell Proliferation Assay^[1]

Cell Line:

Human PBMC-derived CD8⁺ T cells, KYSE70 cells
Concentration:

10 μM
Incubation Time:

48 h pretreatment; 72 h coculture (αIL-15, 10 μg/mL)
Result:

Conditioned media from SMC247-9-treated KYSE70 cells partially restored proliferation and increased the IFN-γ⁺ population.
Addition of an IL-15-neutralizing antibody largely abrogated this effect.

Cell Proliferation Assay^[1]

Cell Line:

Human PBMC-derived T cells, KYSE70 cells
Concentration:

10 μM
Incubation Time:

48 h pretreatment; 72 h coculture
Result:

Conditioned media from KYSE70 cells treated with SMC247-9 or anti-PD-L1 each partially alleviated the suppressive effect on T cell proliferation and effector function.
Conditioned media from the combination group supported a stronger proliferative response and higher IFN-γ⁺ CD8⁺ T cell frequency than either single-agent group.

Parmacokinetics

Species	Dose	Route	T_max	T_1/2
Mice^[1]	20 mg/kg	i.p.	0.5 h	1.26 h

In Vivo

Anti-cancerAdaptive ImmunityImmune Tolerance & ImmunosuppressionOxidative Stress

Anti-cancer

Adaptive Immunity

(DL)-3,5-Dimethyltyrosine (SMC247-9) (1 mg/kg; i.p.; daily; 22 days) exerts antitumor activity in the MC38 model, which is associated with enhanced intratumoral CD8⁺ T cell infiltration and systemic activation of CD8⁺ T cell effector function^[1].

Anti-cancer

Adaptive Immunity

Immune Tolerance & Immunosuppression

(DL)-3,5-Dimethyltyrosine (1-3 mg/kg; i.p.; daily; 24 days) dose-dependently inhibits tumor progression in the anti-PD-L1-unresponsive TC-1 model and is associated with increased CD8⁺ T cell infiltration and effector activation in the tumor microenvironment^[1].

Adaptive Immunity

Oxidative Stress

(DL)-3,5-Dimethyltyrosine (1 mg/kg; i.p.; 9 days) alleviates anti-PD-1-exacerbated DSS-induced colitis-like intestinal inflammation^[1].

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

Animal Model:

C57BL/6 (female, 6-8 weeks old, inoculated subcutaneously with 1 × 10⁶ MC38 cells)^[1]
Dosage:

1 mg/kg
Administration:

i.p.; daily; 22 days
Result:

Markedly suppressed tumor growth, as reflected by reduced tumor volume during treatment and lower tumor weight at the study end point.
Increased the proportion of CD3⁺CD8⁺ T cells in tumor tissue.
Significantly elevated the frequency of IFN-γ⁺ CD8⁺ T cells in tumors, spleen, and draining lymph nodes.

Animal Model:

C57BL/6 (female, 6-8 weeks old, inoculated subcutaneously with 2 × 10⁵ TC-1 cells)^[1]
Dosage:

1, 3 mg/kg
Administration:

i.p.; daily; 24 days
Result:

Suppressed tumor progression in a dose-dependent manner.
Increased the proportion of tumor-infiltrating CD3⁺CD8⁺ T cells and IFN-γ⁺ CD8⁺ T cells within tumors.

Animal Model:

C57BL/6 (female, 6-8 weeks old, treated with 3% DSS in drinking water to establish DSS-induced acute colitis aggravated by anti-PD-1 antibody)^[1]
Dosage:

1 mg/kg
Administration:

i.p.; administered on days 1, 4, and 7
Result:

Alleviated body weight loss induced by combined anti-PD-1 and DSS treatment.
Rescued colon shortening and improved colon tissue morphological injury shown by H&E staining.
Reduced M1/M2 macrophage ratio in colorectal tissues.
Decreased levels of proinflammatory cytokines IL-6 and TNF-α in colorectal tissue homogenates.

Related Protocols :

Chemical Information

CAS No. 88262-44-6
Molecular Weight 209.24
Formula C₁₁H₁₅NO₃
SMILES

OC1=C(C)C=C(CC(N)C(O)=O)C=C1C
Synonyms

SMC247-9
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Ning H, et al. Discovery of a Potent APOBEC3B Inhibitor to Augment Antitumor Immunity and Reduce Inflammatory Toxicity. Journal of medicinal chemistry. 2026 Sep 10;69(17):20678-20697.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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(DL)-3,5-Dimethyltyrosine

All Interleukin Related Isoforms

All TNF Receptor Isoforms