Cat. No.: HY-184891

W1307

W1307 is a selective STAT3 inhibitor with a K_D value of 1.74 μM. W1307 inhibits STAT3 Tyr705 phosphorylation, disrupts STAT3 dimerization, and suppresses STAT3 transcriptional activity. W1307 downregulates the expression of STAT3 downstream targets c-Myc, Mcl-1 and Bcl-2. W1307 transcriptionally inhibits SREBP1 and CPT2 expression to disrupt lipid homeostasis. W1307 shows potent anti-leukemic activity and synergizes with Cytarabine (Ara-C) (HY-13605) to overcome chemoresistance in acute myeloid leukemia (AML).

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CAS No.: 3028770-95-5
Formule: C₂₀H₁₅N₃O₃
Masse moléculaire:345.35

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

W1307 Chemical Structure

CAS No.: 3028770-95-5

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Use of MCE Products

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

STAT3

1.74 μM (Kd)

Mcl-1

Bcl-2

Voir tous les produits spécifiques à Isoform STAT :

Voir tous les produits spécifiques à Isoform Bcl-2 Family :

Cellular Effect

Cell Line	Type	Value	Description	References
K562	IC₅₀	2.331 μM	Inhibits the viability of K562 cells. Inhibits the viability of K562 cells.	42310288
MOLM-13	IC₅₀	1.707 μM	Inhibits the viability of MOLM-13 cells. Inhibits the viability of MOLM-13 cells.	42310288

In Vitro

W1307 (0-3 μM; 48 h) significantly suppresses lipid oxidation^[1].
W1307 (0.78-12.5 μM) binds to STAT3 with a K_D of 1.74 μM determined by SPR assay^[1].
W1307 (1 μΜ; 1 h) binds to and stabilizes the STAT3 protein in K562 cells^[1].
W1307 (3 μΜ; 0-24 h) inhibits Tyr 705 phosphorylation of STAT3 in MOLM-13/AR cells^[1].
W1307 (0.3-3 μΜ; 24 h) suppresses the expression of STAT3 downstream targets (c-Myc, Mcl-1, and Bcl-2) and shows no effect on STAT1/STAT5 phosphorylation or AKT phosphorylation in K562/MOLM-13 cells^[1].
W1307 (0-3 μΜ; 12 h) disrupts STAT3-STAT3 dimerization in HEK-293T cells^[1].
W1307 (0-3 μΜ; 24 h) inhibits STAT3 transcriptional activity in HEK-293T cells^[1].
W1307 (0-3 μΜ; 72 h) exhibits attenuated anti-proliferative effects in CRISPR/Cas9-generated stable STAT3-knockout AML cell lines^[1].
W1307 (72 h) inhibits the viability of MOLM-13 (IC₅₀ = 1.707 μΜ), K562 (2.331 μΜ) cells and AML cell lines (IC₅₀ values ranging from 0.549 μΜ to 3.122 μΜ)^[1].
W1307 (0-3 μΜ; 48 h) suppresses the proliferation and exerts pro-apoptotic effects in K562 and MOLM-13 cells^[1].
W1307 (0-1 μM; 48 h) causes cell cycle arrest in K562 and MOLM-13 cells^[1].
W1307 (0-3 μM; 24 h) reduces the mRNA and protein level of lipid biosynthesis-related genes and CPT2 in MOLM-13/AR cells and in shCont and shSTAT3 (#1 and #2) MOLM-13/AR cells^[1].
W1307 (1.5-3 μM; 48 h) disrupts the direct binding of STAT3 to the promoters of SREBP1 and CPT2 in MOLM-13/AR cells^[1].
W1307 (1.5-3 μM; 24 h) suppresses the elevated luciferase activity of pGL3-CPT2 and pGL3-SREBF1 reporter constructs induced by constitutively active STAT3 (STAT3C) in HEK-293T cells^[1].
W1307 (72 h) induces impaired cell viability and excessive intracellular lipid accumulation upon STAT3 inhibition, W1307 and Cytarabine (Ara-C) (HY-13605) potentiates the suppression of cell viability, and the effect can be reversed by exogenous overexpression of either SREBP1 or CPT2 in MOLM-13/AR cells^[1].
W1307 (0-3 μM; 48 h) induces a significant elevation of both total and lipid ROS and reduces mitochondrial membrane potential (MMP) in MOLM-13/AR cells^[1].
W1307 (0-5 μM; 48 h) upregulates intracellular malondialdehyde (MDA) levels in MOLM-13/AR cells^[1].
W1307-induced intracellular neutral lipid accumulation can be attenuated by exogenous Oleic acid (OA) (HY-N1446) supplementation in MOLM-13/AR cells^[1].
W1307 (3 μM; 48 h)-induced cell death is prevented by presence of Acetylcysteine (NAC) (HY-B0215) or OA in MOLM-13/AR cells^[1].
W1307 (3 μM; 48 h) combined with NAC or OA reverses the effects of STAT3 inhibition on ROS formation, MDA accumulation, and MMP reduction in MOLM-13/AR cells^[1].
W1307 induces sensitization to Ara-C, and OA addition reverses this phenotype to reinstate Ara-C resistance in MOLM-13/AR cells^[1].
W1307 (1.5 μM; 72 h) combined with Ara-C shows significantly greater anti-proliferative effects than individual drugs in MOLM-13/AR cells^[1].
W1307 (1.5 μM; 48 h) enhances the apoptosis-inducing effect of Ara-C in MOLM-13/AR cells, consistently with the upregulated apoptotic proteins^[1].
W1307 (1.5 μM; 48 h) combined with Ara-C induces higher ROS accumulation than monotherapy^[1].

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

Western Blot Analysis^[1]

Cell Line:

K562 cells
Concentration:

1 μΜ
Incubation Time:

1 h
Result:

Binded to and stabilized the STAT3 protein.

Western Blot Analysis^[1]

Cell Line:

MOLM-13/AR cells
Concentration:

3 μΜ
Incubation Time:

0-24 h
Result:

Inhibited Tyr705 phosphorylation of STAT3.

Western Blot Analysis^[1]

Cell Line:

K562/MOLM-13 cells
Concentration:

0μΜ, 0.3μΜ, 1μΜ, 3 μΜ
Incubation Time:

24 h
Result:

Suppressed the expression of STAT3 downstream targets (c-Myc, Mcl-1, and Bcl-2).
Showed no effect on STAT1/STAT5 phosphorylation or AKT phosphorylation.

Cell Viability Assay^[1]

Cell Line:

MOLM-13 cells and KO-STAT3-MOLM-13 cells
Concentration:

0 μΜ, 1 μΜ, 3 μM
Incubation Time:

72 h
Result:

Exhibited attenuated anti-proliferative effects in CRISPR/Cas9-generated stable STAT3-knockout AML cell lines.

Cell Viability Assay^[1]

Cell Line:

MOLM-13, K562 cells
Concentration:

0-20 μΜ
Incubation Time:

72 h
Result:

Inhibited the viability of MOLM-13 (IC₅₀ = 1.707 μΜ), K562 (IC₅₀ = 2.331 μΜ) cells.

Cell Viability Assay^[1]

Cell Line:

AML cell lines
Concentration:

0-10 μΜ
Incubation Time:

72 h
Result:

Inhibited the viability of multiple AML cell lines with IC₅₀ values ranging from 0.549 μΜ to 3.122 μΜ.

Cell Proliferation Assay^[1]

Cell Line:

K562 and MOLM-13 cells
Concentration:

0 μΜ, 0.3 μΜ, 1 μΜ, 3 μΜ
Incubation Time:

48 h
Result:

Suppressed the proliferation in K562 and MOLM-13 cells.

Apoptosis Analysis^[1]

Cell Line:

K562 and MOLM-13 cells
Concentration:

0 μΜ, 0.3 μΜ, 1 μΜ, 3 μΜ
Incubation Time:

48 h
Result:

Exerts pro-apoptotic effects.

RT-PCR^[1]

Cell Line:

MOLM-13/AR cells, shCont and shSTAT3 (#1 and #2) MOLM-13/AR cells
Concentration:

0 μΜ, 1.5 μΜ, 3 μΜ
Incubation Time:

24 h
Result:

Reduced the mRNA level of lipid biosynthesis-related genes and CPT2 in MOLM-13/AR cells and in shCont and shSTAT3 (#1 and #2) MOLM-13/AR cells.

Western Blot Analysis^[1]

Cell Line:

MOLM-13/AR cells, shCont and shSTAT3 (#1 and #2) MOLM-13/AR cells
Concentration:

0 μΜ, 1.5 μΜ, 3 μΜ
Incubation Time:

24 h
Result:

Reduced the protein level of lipid biosynthesis-related genes and CPT2 in MOLM-13/AR cells and in shCont and shSTAT3 (#1 and #2) MOLM-13/AR cells.

Cell Viability Assay^[1]

Cell Line:

MOLM-13/AR cells
Concentration:

3 μΜ
Incubation Time:

48 h
Result:

Reduced cell viability, while the presence of NAC or OA restored cell viability.

Apoptosis Analysis^[1]

Cell Line:

MOLM-13/AR cells
Concentration:

3 μΜ
Incubation Time:

48 h
Result:

Induced cell death, while the presence of NAC or OA prevented cell death.

Cell Viability Assay^[1]

Cell Line:

MOLM-13/AR cells
Concentration:

1.5 μM
Incubation Time:

72 h
Result:

Combined with Ara-C shows significantly greater anti-proliferative effects than individual drugs.

Apoptosis Analysis^[1]

Cell Line:

MOLM-13/AR cells
Concentration:

1.5 μΜ
Incubation Time:

48 h
Result:

Enhanced the apoptosis-inducing effect of Ara-C.

Western Blot Analysis^[1]

Cell Line:

MOLM-13/AR cells
Concentration:

1.5 μΜ
Incubation Time:

48 h
Result:

Upregulated the expression of apoptotic proteins.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	MRT_0-t	MRT_0-∞	C_max	AUC_0-t	AUC_0-∞
Mice^[1]	10 mg/kg	i.p.	1.22 h	0.250 h	1.01 h	1.04 h	4300 ng/mL	4800 ng/mL·h	4815 ng/mL·h

In Vivo

W1307 (5 and 15 mg/kg; i.p.; once daily on days 10, 17, 24) exhibits dose-dependent anti-leukemic effects, reduces tumor burden and residual MOLM-13-EGFP/Luc cells in the bone marrow and spleen, lowers immature blast cells in the blood, decreases large basophilic cells in the femoral bone marrow and spleen, suppresses STAT3 signaling and lipid metabolism proteins in tumor tissues in MOLM-13-EGFP/Luc xenograft models in male NOD-SCID mice (5-8 weeks old)^[1].
W1307 (5 mg/kg; i.p.; once daily on days 0, 10, 17, 24) combined with Ara-C exhibits superior anti-leukemic activity, reduces the number of residual MOLM-13/AR-EGFP/Luc cells in the bone marrow and spleen and decreases spleen weight and does not adversely affect non-target tissues in MOLM-13/AR-EGFP/Luc-derived chemo-resistant AML models in male NOD-SCID mice (5-8 weeks old)^[1].

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

Animal Model:

MOLM-13-EGFP/Luc xenograft models in male NOD-SCID mice (5-8 weeks old)^[1]
Dosage:

5 and 15 mg/kg
Administration:

i.p.; once daily on days 10, 17, 24
Result:

Exhibited dose-dependent anti-leukemic effects.
Reduced tumor burden versus vehicle controls.
Reduced residual MOLM-13-EGFP/Luc cells in the bone marrow and spleen.
Reduced the immature blast cells in the blood.
Decreased large basophilic cells in the femoral bone marrow and spleen.
Suppressed STAT3 signaling.
Suppressed lipid metabolism proteins in tumor tissues.

Animal Model:

MOLM-13/AR-EGFP/Luc-derived chemo-resistant AML models in male NOD-SCID mice (5-8 weeks old)^[1]
Dosage:

5 mg/kg
Administration:

i.p.; once daily on days 0, 10, 17, 24
Result:

Combined with Ara-C exhibited superior anti-leukemic activity.
Reduced the number of residual MOLM-13/AR-EGFP/Luc cells in the bone marrow and spleen.
Decreased spleen weight.
Combined with Ara-C did not adversely affect non-target tissues.

Chemical Information

CAS No. 3028770-95-5
Masse moléculaire 345.35
Formule C₂₀H₁₅N₃O₃
SMILES

COC1=CC=C2C(N=C(C3=CC=CC=C3)C=C2C(NC4=NC=CO4)=O)=C1
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Peng K, et al. Targeting STAT3-mediated lipid metabolism reprogramming overcomes chemoresistance in acute myeloid leukemia. Cell Death Dis. 2026 Jun 17. [Content Brief]

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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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W1307

Voir tous les produits spécifiques à Isoform STAT

Voir tous les produits spécifiques à Isoform Bcl-2 Family

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

W1307 Related Classifications

HY-184891 Related Classifications

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